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Cyclosporin A [59865-13-3]

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Referencia HY-B0579-200mg

embalaje : 200mg

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Marca : MedChemExpress

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Contact local distributor :

Teléfono : +1 850 650 7790

Descripciòn

Cyclosporin A (Cyclosporine A) is an immunosuppressant which binds to the cyclophilin and inhibits phosphatase activity of protein phosphatase 2B (PP2B/calcineurin) with an IC₅₀ of 5 nM^[3]. Cyclosporin A also inhibits CD11a/CD18 adhesion^[8].

IC₅₀ & Target

Cyclophilin D

Cellular Effect

Cell Line	Type	Value	Description	References
2008	IC₅₀	2.7 μM Compound: Cyclosporine A	Inhibition of MRP1 in human 2008 cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay Inhibition of MRP1 in human 2008 cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay	[PMID: 24184213]
2008	IC₅₀	2.81 μM Compound: CsA	Inhibition of MRP1 (unknown origin) expressed in human 2008 cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay Inhibition of MRP1 (unknown origin) expressed in human 2008 cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay	[PMID: 23851114]
2008	IC₅₀	4.78 μM Compound: cyclosporin A	Inhibition of human MRP1 in human 2008 cells Inhibition of human MRP1 in human 2008 cells	[PMID: 18707884]
A2780	GI₅₀	8.94 μM Compound: Cyclosporine A	Cytotoxicity against human A2780 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A2780 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27100033]
A2780	IC₅₀	4.92 μM Compound: cyclosporin A	Inhibition of P-gp in human A2780 cells Inhibition of P-gp in human A2780 cells	[PMID: 18707884]
A2780 ADR	GI₅₀	8.63 μM Compound: Cyclosporine A	Cytotoxicity against human A2780/ADR cells overexpressing ABCB1 assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A2780/ADR cells overexpressing ABCB1 assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 27100033]
A2780 ADR	IC₅₀	0.919 μM Compound: CsA	Inhibition of ABCB1 in human A2780adr cells pre-incubated for 30 mins followed by calcein AM addition and further incubated for 60 mins by calcein AM assay Inhibition of ABCB1 in human A2780adr cells pre-incubated for 30 mins followed by calcein AM addition and further incubated for 60 mins by calcein AM assay	[PMID: 25855895]
A2780 ADR	IC₅₀	0.92 μM Compound: Cyclosporine A	Inhibition of MDR1 in human doxorubicin-resistant A2780adr cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay Inhibition of MDR1 in human doxorubicin-resistant A2780adr cells assessed as Calcein AM accumulation treated 30 mins before Calcein AM addition measured up to 90 mins by fluorescence assay	[PMID: 24184213]
A2780 ADR	IC₅₀	0.99 μM Compound: CsA	Inhibition of p-glycoprotein (unknown origin) expressed in human A2780Adr cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay Inhibition of p-glycoprotein (unknown origin) expressed in human A2780Adr cells assessed as calcein-AM accumulation preincubated for 30 mins before calcein-AM addition measured up to 90 mins by fluorescence assay	[PMID: 23851114]
A2780 ADR	IC₅₀	1.21 μM Compound: Cyclosporine A	Inhibition of ABCB1 in human A2780/ADR cells assessed as reduction in calcien-AM efflux preincubated for 30 mins followed by calcien-AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay Inhibition of ABCB1 in human A2780/ADR cells assessed as reduction in calcien-AM efflux preincubated for 30 mins followed by calcien-AM addition measured immediately at 60 sec time interval for 60 mins by fluorescence assay	[PMID: 27676469]
A2780 ADR	IC₅₀	1.4 μM Compound: Cyclosporin A	Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay Inhibition of P-glycoprotein-mediated multidrug resistance in adriamycin-resistant human A2780/ADR cells by calcein AM assay	[PMID: 19250834]
A2780 ADR	IC₅₀	1.41 μM Compound: Cyclosporine A	Inhibition of ABCB1 in human A2780/ADR cells incubated for 30 mins measured up to 3600 secs with time intervals of 60 secs by calcein accumulation assay Inhibition of ABCB1 in human A2780/ADR cells incubated for 30 mins measured up to 3600 secs with time intervals of 60 secs by calcein accumulation assay	[PMID: 27100033]
B-cell	IC₅₀	0.07 μg/mL Compound: cyclosporin A	Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay	[PMID: 14738397]
B-cell	IC₅₀	0.159 μM Compound: CsA	Inhibition of LPS-induced BALB/c mouse B cell proliferation Inhibition of LPS-induced BALB/c mouse B cell proliferation	[PMID: 17081761]
B-cell	IC₅₀	0.74 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in LPS-induced mouse B-lymphocytes proliferation incubated for 8 hrs by beta scintillation counting based [3H]thymidine incorporation assay Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in LPS-induced mouse B-lymphocytes proliferation incubated for 8 hrs by beta scintillation counting based [3H]thymidine incorporation assay	[PMID: 35678710]
Breast cancer cell line	EC₅₀	0.5 μM Compound: Cyclosporin A	Concentration that reduces the difference in reversal of DOX accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%. Concentration that reduces the difference in reversal of DOX accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%.	[PMID: 11784143]
Breast cancer cell line	EC₅₀	0.6 μM Compound: Cyclosporin A	Concentration that reduces difference in reversal of [3H]VBL accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50% Concentration that reduces difference in reversal of [3H]VBL accumulation between MDA-435/LCC6 and MDA-435/LCC6-MDRI cells by 50%	[PMID: 11784143]
Caco-2	EC₅₀	45.5 μM Compound: Cyclosporin A	Inhibition of P-glycoprotein-mediated [3H]vinblastine transport in human Caco-2 cells Inhibition of P-glycoprotein-mediated [3H]vinblastine transport in human Caco-2 cells	[PMID: 18524592]
Caco-2	EC₅₀	80 μM Compound: cyclosporin A	Inhibition of human Pgp mediated [3H]vinblastine transport in human Caco-2 cells Inhibition of human Pgp mediated [3H]vinblastine transport in human Caco-2 cells	[PMID: 17936633]
Caco-2	EC₅₀	80 μM Compound: cyclosporin A	Inhibition of human P-glycoprotein mediated [3H]vinblastine transport in human Caco-2 cells Inhibition of human P-glycoprotein mediated [3H]vinblastine transport in human Caco-2 cells	[PMID: 18257545]
Caco-2	EC₅₀	80 μM Compound: cyclosporin A	Inhibition of human P-gp mediated [3H]vinblastine transport activity in human Caco-2 cells Inhibition of human P-gp mediated [3H]vinblastine transport activity in human Caco-2 cells	[PMID: 18276145]
Caco-2	IC₅₀	1.3 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 5 uM) in Caco-2 cells	[PMID: 10820137]
Caco-2	IC₅₀	2.9 μM Compound: CsA	Inhibition of P-gp in human Caco2 cells assessed as reduction in digoxin efflux Inhibition of P-gp in human Caco2 cells assessed as reduction in digoxin efflux	[PMID: 23382458]
Cancer cell lines	IC₅₀	1 μM Compound: Cyclosporin A	Growth inhibitory activity on MDA-435/LCC6 (Pgp-positive) human breast cancer cells. Growth inhibitory activity on MDA-435/LCC6 (Pgp-positive) human breast cancer cells.	[PMID: 11784143]
Cancer cell lines	IC₅₀	1.1 μM Compound: Cyclosporin A	Growth inhibitory activity on MDA-435/LCC6-MDRI (Pgp-negative) human breast cancer cells. Growth inhibitory activity on MDA-435/LCC6-MDRI (Pgp-negative) human breast cancer cells.	[PMID: 11784143]
CCRF-CEM	IC₅₀	3.4 μM Compound: 1	Inhibitory activity against Human MDR1 P-Glycoprotein ABC Transporter using leukemia CEM cells Inhibitory activity against Human MDR1 P-Glycoprotein ABC Transporter using leukemia CEM cells	[PMID: 12361387]
CEM/VLB100	IC₅₀	3.41 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of Calcein-AM efflux (Calcein-AM: 0.25 uM) in CEM/VLB100 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux (Calcein-AM: 0.25 uM) in CEM/VLB100 cells	[PMID: 10891114]
EMT6	IC₅₀	440 nM Compound: Cyclosporin A	Reversal effect on the accumulation of [3H]- daunorubicin in mouse mammary carcinoma cell line EMT6/AR 1.0 Reversal effect on the accumulation of [3H]- daunorubicin in mouse mammary carcinoma cell line EMT6/AR 1.0	[PMID: 10098671]
HEK293	IC₅₀	0.7 μM Compound: Cyclosporine A	Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estradiol-17beta-glucuronide substrate	[PMID: 22587986]
HEK293	IC₅₀	0.7 μM Compound: Cyclosporine A	Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using pitavastatin substrate	[PMID: 22587986]
HEK293	IC₅₀	1.2 μM Compound: Cyclosporine A	Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate Inhibition of OATP1B1 (unknown origin) expressed in HEK293 cells using estrone-3-sulfate substrate	[PMID: 22587986]
HEK293	IC₅₀	1.3 μM Compound: Cyclosporin A	Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting Inhibition of human liver OATP1B3 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E17-betaG uptake incubated for 5 mins by scintillation counting	[PMID: 22541068]
HEK293	IC₅₀	1.4 μM Compound: Cyclosporin A	Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting Inhibition of human liver OATP1B1 expressed in HEK293 Flp-In cells assessed as reduction in E17-betaG uptake by scintillation counting	[PMID: 22541068]
HEK293	IC₅₀	37 μM Compound: Cyclosporin A	Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting Inhibition of human liver OATP2B1 expressed in HEK293 Flp-In cells assessed as reduction in [3H]E3S uptake incubated for 5 mins by scintillation counting	[PMID: 22541068]
HeLa	IC₅₀	>8.3 μM Compound: Cs	Antiviral activity against RSV infected in human HeLa cells assessed as inhibition of viral replication Antiviral activity against RSV infected in human HeLa cells assessed as inhibition of viral replication	[PMID: 18212100]
HeLa	IC₅₀	1 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of Taurocholate uptake in NTCP-expressing HeLa cells TP_TRANSPORTER: inhibition of Taurocholate uptake in NTCP-expressing HeLa cells	[PMID: 10565843]
HeLa	IC₅₀	6.6 μM Compound: Cs	Antiviral activity against HPV-18 infected in human HeLa cells assessed as inhibition of viral replication after 3 days Antiviral activity against HPV-18 infected in human HeLa cells assessed as inhibition of viral replication after 3 days	[PMID: 18212100]
HepG2	IC₅₀	>50 μM Compound: 92125416	HARVARD: Cytotoxicity in HepG2 cell line HARVARD: Cytotoxicity in HepG2 cell line	[PMID: 22586124]
HepG2	IC₅₀	0.00165 μM Compound: 92125416	HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells	[PMID: 22586124]
HFF	IC₅₀	>10000 nM Compound: CSA	Inhibition of fetal calf serum-induced proliferation of human foreskin fibroblast assessed as [3H]thymidine incorporation after 4 days by scintillation counting Inhibition of fetal calf serum-induced proliferation of human foreskin fibroblast assessed as [3H]thymidine incorporation after 4 days by scintillation counting	[PMID: 14593182]
HFF	IC₅₀	>10 μM Compound: CSA	Inhibition of fetal calf serum-induced proliferation of human foreskin fibroblast assessed as [3H]thymidine incorporation after 4 days by scintillation counting Inhibition of fetal calf serum-induced proliferation of human foreskin fibroblast assessed as [3H]thymidine incorporation after 4 days by scintillation counting	[PMID: 14593182]
HL-60	IC₅₀	>10 μM Compound: 1	Inhibitory activity against human formylpeptide receptor (FPR) of human leukemia HL-60 cells Inhibitory activity against human formylpeptide receptor (FPR) of human leukemia HL-60 cells	[PMID: 12361388]
Huh-5-2	CC₅₀	4.4 μM Compound: CsA	Cytostatic activity against human Huh5-2 cells assessed as decrease in cell proliferation after 3 days by MTS method Cytostatic activity against human Huh5-2 cells assessed as decrease in cell proliferation after 3 days by MTS method	10.1039/C1MD00227A
Huh-5-2	CC₅₀	6 μM Compound: Cyclosporine A	Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay	[PMID: 18625766]
Huh-5-2	EC₅₀	0.3 μM Compound: Cyclosporine A	Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay	[PMID: 18625766]
Huh-5-2	EC₅₀	306 nM Compound: CsA	Antiviral activity against Hepatitis C virus genotype 1b I389luc-ubi-neo/NS3-3'/5.1 subgenomic replicon infected in human Huh5-2 cells after 4 days by luciferase assay Antiviral activity against Hepatitis C virus genotype 1b I389luc-ubi-neo/NS3-3'/5.1 subgenomic replicon infected in human Huh5-2 cells after 4 days by luciferase assay	10.1039/C1MD00227A
Huh-7	CC₅₀	5.62 μM Compound: CsA	Antiviral activity against Hepatitis C virus infected in human Huh7ET cells assessed as inhibition of viral replication after 72 hrs by luciferase reporter gene assay Antiviral activity against Hepatitis C virus infected in human Huh7ET cells assessed as inhibition of viral replication after 72 hrs by luciferase reporter gene assay	[PMID: 19933795]
Huh-7	EC₅₀	>10 μM Compound: CsA	Antiviral activity against cyclosporine A/NIM-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay Antiviral activity against cyclosporine A/NIM-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay	[PMID: 20176894]
Huh-7	EC₅₀	0.21 μM Compound: CsA	Antiviral activity against HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay Antiviral activity against HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay	[PMID: 20176894]
Huh-7	EC₅₀	137 nM Compound: CsA	Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis Antiviral activity against Hepatitis C virus genotype 1b Con1 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis	10.1039/C1MD00227A
Huh-7	EC₅₀	198 nM Compound: CsA	Antiviral activity against Hepatitis C virus genotype 1a H77 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis Antiviral activity against Hepatitis C virus genotype 1a H77 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis	10.1039/C1MD00227A
Huh-7	EC₅₀	3.39 μM Compound: CsA	Antiviral activity against cyclosporine A-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay Antiviral activity against cyclosporine A-resistant HCV subtype 1b Con1 infected in human HuH7 cells assessed as reduction in viral RNA level after 48 hrs by MTS assay	[PMID: 20176894]
Huh-7	EC₅₀	455 nM Compound: CsA	Antiviral activity against Hepatitis C virus genotype 2a JFH-1 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis Antiviral activity against Hepatitis C virus genotype 2a JFH-1 infected in human Huh7 cells assessed as decrease in subgenomic RNA level after 72 hrs by RT-PCR analysis	10.1039/C1MD00227A
Huh-7	IC₅₀	5810 nM Compound: 1, CsA	Cytotoxicity against human HuH7 cells assessed as release of lactate dehydrogenase Cytotoxicity against human HuH7 cells assessed as release of lactate dehydrogenase	[PMID: 20943390]
Jurkat	EC₅₀	0.005 μM Compound: CsA	Antiinflammatory activity in human Jurkat cells assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay Antiinflammatory activity in human Jurkat cells assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay	[PMID: 19933795]
Jurkat	EC₅₀	6.7 nM Compound: 1, CsA	Immunosuppressive activity against human Jurkat cells assessed as inhibition of phytohemagglutinin-M/phorbol myristate acetate-induced IL2 production Immunosuppressive activity against human Jurkat cells assessed as inhibition of phytohemagglutinin-M/phorbol myristate acetate-induced IL2 production	[PMID: 20943390]
Jurkat	IC₅₀	>1 μM Compound: cyclosporin-A	Inhibition of production of beta-galactosidase thymidine kinase RGA in Jurkat cells Inhibition of production of beta-galactosidase thymidine kinase RGA in Jurkat cells	[PMID: 11881984]
Jurkat	IC₅₀	>10 μM Compound: CsA	Cytotoxicity against human Jurkat cells after 4 days by MTT assay Cytotoxicity against human Jurkat cells after 4 days by MTT assay	[PMID: 22984987]
Jurkat	IC₅₀	>10 μM Compound: CsA	In vitro inhibition of Jurkat cell proliferation. In vitro inhibition of Jurkat cell proliferation.	[PMID: 11384243]
Jurkat	IC₅₀	>10 μM Compound: CsA	In vitro inhibitory activity against Jurkat cell proliferation In vitro inhibitory activity against Jurkat cell proliferation	[PMID: 9719606]
Jurkat	IC₅₀	0.007 μM Compound: cyclosporin-A	Inhibition of production of IL-2 secretion in Jurkat cells Inhibition of production of IL-2 secretion in Jurkat cells	[PMID: 11881984]
Jurkat	IC₅₀	0.008 μM Compound: Cyclosporin A	Effect on the transcription and release of IL-2 in a reporter-gene assay (RGA) Effect on the transcription and release of IL-2 in a reporter-gene assay (RGA)	10.1016/S0960-894X(97)10005-1
Jurkat	IC₅₀	0.008 μM Compound: cyclosporin-A	Inhibition of production of beta-galactosidase IL-2 RGA in Jurkat cells Inhibition of production of beta-galactosidase IL-2 RGA in Jurkat cells	[PMID: 11881984]
Jurkat	IC₅₀	1.4 nM Compound: 1	Inhibition of NFAT activation in PMA/ionomycin-stimulated human Jurkat T cells incubated for 30 mins prior to PMA/ionomycin stimulation measured after 5 hrs by luciferase reporter gene assay Inhibition of NFAT activation in PMA/ionomycin-stimulated human Jurkat T cells incubated for 30 mins prior to PMA/ionomycin stimulation measured after 5 hrs by luciferase reporter gene assay	[PMID: 23964991]
Jurkat	IC₅₀	1.9 μM Compound: CsA	Immunosuppressive activity in human Jurkat cells assessed as reduction in PHA + PMA-induced IL-2 production after 48 hrs by ELISA Immunosuppressive activity in human Jurkat cells assessed as reduction in PHA + PMA-induced IL-2 production after 48 hrs by ELISA	[PMID: 30579802]
Jurkat	IC₅₀	11 nM Compound: 1; CyA	Immunosuppressive activity in human PMA/ionomycin stimulated Jurkat T cells assessed as suppression of IL2 production pretreated with cells followed by PMA/ionomycin stimulation measured after 13 hrs by ELISA Immunosuppressive activity in human PMA/ionomycin stimulated Jurkat T cells assessed as suppression of IL2 production pretreated with cells followed by PMA/ionomycin stimulation measured after 13 hrs by ELISA	[PMID: 27647370]
Jurkat	IC₅₀	12 nM Compound: CsA	The compound was tested in vitro for inhibition of IL-2 release stimulated with PMA/ionomycin by Jurkat cells. The compound was tested in vitro for inhibition of IL-2 release stimulated with PMA/ionomycin by Jurkat cells.	[PMID: 7473543]
Jurkat	IC₅₀	2 nM Compound: CsA	Immunosuppressive activity was measured by inhibition of the IL-2 production in Jurkat cells. Immunosuppressive activity was measured by inhibition of the IL-2 production in Jurkat cells.	[PMID: 14643337]
K562/R7	IC₅₀	0.7 μM Compound: cyclosporin A	Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay	[PMID: 25634041]
KB	IC₅₀	0.6 μM Compound: CSA (cyclosporin A)	Inhibitory activity against KB cell line after 72 h of drug exposure Inhibitory activity against KB cell line after 72 h of drug exposure	[PMID: 15481991]
KB 3-1	EC₅₀	1.2 μM Compound: CSA (cyclosporin A)	Concentration that causes 50% of maximum vinblastine accumulation in KB/MDR cells in 1 h Concentration that causes 50% of maximum vinblastine accumulation in KB/MDR cells in 1 h	[PMID: 15481991]
KB 3-1	IC₅₀	1.5 μM Compound: CSA (cyclosporin A)	Inhibitory activity against KB/MDR cell line after 72 hr of drug exposure Inhibitory activity against KB/MDR cell line after 72 hr of drug exposure	[PMID: 15481991]
KB 3-1	IC₅₀	23.9 μM Compound: Cyclosporine A	Cytotoxicity against human KB 3-1 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay Cytotoxicity against human KB 3-1 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay	[PMID: 35751979]
KB-V1	IC₅₀	7.95 μM Compound: Cyclosporine A	Cytotoxicity against human KB-V1 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay Cytotoxicity against human KB-V1 cells assessed as cell growth inhibition incubated for 72 hrs by MTS assay	[PMID: 35751979]
L929	IC₅₀	29.9 μM Compound: Cyclosporin A	Cytotoxicity against mouse L929 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay Cytotoxicity against mouse L929 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay	[PMID: 34597896]
L929	IC₅₀	30 μM Compound: cyclosporin A	Cytotoxicity against mouse L929 cells after 3 days by MTS assay Cytotoxicity against mouse L929 cells after 3 days by MTS assay	[PMID: 25985195]
L929	IC₅₀	33.9 μM Compound: 2	Cytotoxicity against mouse L929 cells after 72 hrs Cytotoxicity against mouse L929 cells after 72 hrs	[PMID: 22320402]
L929	IC₅₀	33.9 μM Compound: cyclosporine A	Cytotoxicity against mouse L929 cells assessed as growth inhibition after 3 days by MTS assay Cytotoxicity against mouse L929 cells assessed as growth inhibition after 3 days by MTS assay	[PMID: 24171478]
LLC-PK1	IC₅₀	0.7 μM Compound: Cyclosporin a	Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, mouse L-mdr1b expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	0.7 μM Compound: Cyclosporin a	TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1b-expressing LLC-PK1 cells	[PMID: 12699389]
LLC-PK1	IC₅₀	0.8 μM Compound: Cyclosporin a	Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, human L-MDR1 expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	0.8 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in MDR1-expressing LLC-PK1 cells	[PMID: 12699389]
LLC-PK1	IC₅₀	3.66 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of Doxorubicin transepithelial transport (basal to apical) (Digoxin: 0.8 uM) in MDR1-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Doxorubicin transepithelial transport (basal to apical) (Digoxin: 0.8 uM) in MDR1-expressing LLC-PK1 cells	[PMID: 9914792]
LLC-PK1	IC₅₀	4.8 μM Compound: Cyclosporin a	Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay Inhibition of P-glycoprotein, mouse L-mdr1a expressed in LLC-PK1 epithelial cells using calcein-AM polarisation assay	[PMID: 12699389]
LLC-PK1	IC₅₀	4.8 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in Mdr1a-expressing LLC-PK1 cells	[PMID: 12699389]
Lymphocyte	CC₅₀	43.2 μM Compound: CsA	Cytotoxicity against lymphocytes (unknown origin) assessed as decrease in cell viability Cytotoxicity against lymphocytes (unknown origin) assessed as decrease in cell viability	[PMID: 29292227]
Lymphocyte	EC₅₀	60 nM Compound: 1, CSA	Immunosuppressive activity in lymphocytes (unknown origin) by mixed lymphocyte reaction assay Immunosuppressive activity in lymphocytes (unknown origin) by mixed lymphocyte reaction assay	[PMID: 24831536]
Lymphocyte	IC₅₀	0.054 μM Compound: CsA	Immunosuppressive activity in lymphocytes by mixed lymphocyte reaction assay Immunosuppressive activity in lymphocytes by mixed lymphocyte reaction assay	[PMID: 20064721]
Lymphocyte	IC₅₀	0.054 μM Compound: CsA	Immunosuppressive activity in peripheral blood lymphocytes isolated from two individuals assessed as proliferation using [methyl-3H]thymidine by mixed lymphocyte reaction assay Immunosuppressive activity in peripheral blood lymphocytes isolated from two individuals assessed as proliferation using [methyl-3H]thymidine by mixed lymphocyte reaction assay	[PMID: 21171614]
Lymphocyte	IC₅₀	0.2 μg/mL Compound: Cyclosporin A	Immunosuppressive activity in human lymphocytes by mixed lymphocyte reaction assay Immunosuppressive activity in human lymphocytes by mixed lymphocyte reaction assay	[PMID: 3373220]
Lymphocyte	IC₅₀	89 nM Compound: CsA	Immunosuppressive activity in lymphocytes by MLR assay Immunosuppressive activity in lymphocytes by MLR assay	[PMID: 24900866]
MDCK	IC₅₀	>14.8 μM Compound: Cs	Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as inhibition of viral replication Antiviral activity against Influenza A virus H1N1 infected in MDCK cells assessed as inhibition of viral replication	[PMID: 18212100]
MDCK	IC₅₀	>14.8 μM Compound: Cs	Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as inhibition of viral replication Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as inhibition of viral replication	[PMID: 18212100]
MDCK	IC₅₀	>14.8 μM Compound: Cs	Antiviral activity against influenza B virus infected in MDCK cells assessed as inhibition of viral replication Antiviral activity against influenza B virus infected in MDCK cells assessed as inhibition of viral replication	[PMID: 18212100]
MDCK	IC₅₀	>9.9 μM Compound: Cs	Antiviral activity against BVDV infected in MDCK cells assessed as inhibition of viral replication Antiviral activity against BVDV infected in MDCK cells assessed as inhibition of viral replication	[PMID: 18212100]
MDCK-II	IC₅₀	13.6 μM Compound: cyclosporin A	Inhibition of human MRP2 expressed in dog MDCK2 cells Inhibition of human MRP2 expressed in dog MDCK2 cells	[PMID: 18707884]
MDCK-II	IC₅₀	25.6 μM Compound: Cyclosporine A	Inhibition of ABCC2 (unknown origin) expressed in MDCK2 cells assessed as inhibition of calcein-AM efflux measured after 30 mins in presence of ABCB1 inhibitor GF120918 and ABCC1 inhibitor MK-571 by flow cytometry Inhibition of ABCC2 (unknown origin) expressed in MDCK2 cells assessed as inhibition of calcein-AM efflux measured after 30 mins in presence of ABCB1 inhibitor GF120918 and ABCC1 inhibitor MK-571 by flow cytometry	[PMID: 27393949]
MDCK-II	IC₅₀	9.34 μM Compound: CsA	Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells Inhibition of human MDR1-dependent accumulation of calcein-AM expressed in MDCK2 cells	[PMID: 17664327]
MT4	CC₅₀	5608 nM Compound: CSA	Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by cell-titer glo assay Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by cell-titer glo assay	[PMID: 30074795]
MT4	EC₅₀	450 nM Compound: 1, CsA	Antiviral activity against HIV1 3B infected in human MT4 cells coinfected with HTLV1 assessed as reduction in virus-induced cytopathogenicity after 4 days by MTT assay Antiviral activity against HIV1 3B infected in human MT4 cells coinfected with HTLV1 assessed as reduction in virus-induced cytopathogenicity after 4 days by MTT assay	[PMID: 23849880]
MT4	IC₅₀	>0.83 μM Compound: Cs	Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect by MTT assay Antiviral activity against HIV-1 3B infected in human MT4 cells assessed as inhibition of virus induced cytopathic effect by MTT assay	[PMID: 18212100]
NCI/ADR-RES	IC₅₀	0.29 μM Compound: Cyclosporin	Reversal of P-gp mediated multidrug resistance in doxorubicin-resistant human MCF-7/ADR cells assessed as doxorubicin IC50 incubated for 48 hrs by CCK-8 assay (Rvb = 12.66 +/- 1.45 microM) Reversal of P-gp mediated multidrug resistance in doxorubicin-resistant human MCF-7/ADR cells assessed as doxorubicin IC50 incubated for 48 hrs by CCK-8 assay (Rvb = 12.66 +/- 1.45 microM)	[PMID: 38364715]
NCI/ADR-RES	IC₅₀	0.518 μM Compound: Cyclosporin A	Cytotoxicity against DOX-resistant human MCF7/ADR cells assessed as doxorubicin IC50 incubated for 48 hrs in presence of doxorubicin by CCK8 assay Cytotoxicity against DOX-resistant human MCF7/ADR cells assessed as doxorubicin IC50 incubated for 48 hrs in presence of doxorubicin by CCK8 assay	[PMID: 36645980]
NCI/ADR-RES	IC₅₀	0.86 μM Compound: CyclosporinA	Cytotoxicity against human MCF7ADR cells assessed as doxorubicin IC50 at 5 uM incubated for 48 hrs by CCK8 assay Cytotoxicity against human MCF7ADR cells assessed as doxorubicin IC50 at 5 uM incubated for 48 hrs by CCK8 assay	[PMID: 37229830]
Neutrophil	IC₅₀	0.047 nM Compound: CSA	Reduction of chemotaxis in human neutrophils assessed as inhibition of fMLP-OMe-induced cell migration pretreated 10 mins before fMLP-OMe challenge Reduction of chemotaxis in human neutrophils assessed as inhibition of fMLP-OMe-induced cell migration pretreated 10 mins before fMLP-OMe challenge	[PMID: 19362486]
NIH-3T3-G185	IC₅₀	1.4 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Daunorubicin efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	1.7 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of Calcein-AM efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Calcein-AM efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	1.7 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Rhodamine 123 efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	1.8 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of LDS-751 efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	2.1 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of Tetramethylrosamine efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Tetramethylrosamine efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	2.4 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of Fluo-3-AM efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of Fluo-3-AM efflux in NIH-3T3-G185 cells	[PMID: 11716514]
NIH-3T3-G185	IC₅₀	4.3 μM Compound: Cyclosporin A	TP_TRANSPORTER: inhibition of JC-1 efflux in NIH-3T3-G185 cells TP_TRANSPORTER: inhibition of JC-1 efflux in NIH-3T3-G185 cells	[PMID: 11716514]
PBMC	EC₅₀	0.0031 μM Compound: CsA	Antiinflammatory activity in human PBMC assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay Antiinflammatory activity in human PBMC assessed as inhibition of anti-CD3/CD28 antibody-induced IL-2 production treated for 1 hr before anti-CD3/CD28 antibody challenge measured after 6 hrs by immunosuppression assay	[PMID: 19933795]
PBMC	IC₅₀	0.056 μM Compound: Cs	Antiproliferative activity against mouse PBMC with MLR assessed as inhibition of [3H]thymidine incorporation after 18 hrs Antiproliferative activity against mouse PBMC with MLR assessed as inhibition of [3H]thymidine incorporation after 18 hrs	[PMID: 18212100]
PBMC	IC₅₀	12 nM Compound: cyclosporin A	Antiproliferative activity against human PBMC Antiproliferative activity against human PBMC	[PMID: 15679309]
PBMC	IC₅₀	3 nM Compound: CsA	Immunosuppressive activity in human PBMC isolated from two individuals assessed as inhibition of proliferation using [3H]thymidine by mixed lymphocyte reaction assay Immunosuppressive activity in human PBMC isolated from two individuals assessed as inhibition of proliferation using [3H]thymidine by mixed lymphocyte reaction assay	10.1039/C1MD00227A
RD	CC₅₀	>10 μM Compound: CsA	Cytotoxicity against human RD cells after 24 hrs by WST-1 assay Cytotoxicity against human RD cells after 24 hrs by WST-1 assay	[PMID: 26564266]
RD	EC₅₀	3.66 μM Compound: CsA	Antiviral activity against EV71 infected in RD cells after 24 hrs by luciferase assay Antiviral activity against EV71 infected in RD cells after 24 hrs by luciferase assay	[PMID: 26564266]
Sf21	IC₅₀	0.5 μM Compound: Cyclosporine	Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]
Sf21	IC₅₀	0.6 μM Compound: Cyclosporine	Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]
Splenocyte	CC₅₀	>2.5 μM Compound: CsA	Cytotoxicity in BALB/c mouse Splenocyte assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay Cytotoxicity in BALB/c mouse Splenocyte assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay	[PMID: 35104138]
Splenocyte	CC₅₀	0.88 μM Compound: CsA	Cytotoxicity against splenocytes after 48 hrs by MTT assay Cytotoxicity against splenocytes after 48 hrs by MTT assay	[PMID: 19481938]
Splenocyte	CC₅₀	1.2 μM Compound: CsA	Cytotoxicity against BALB/c mouse splenocytes after 48 hrs by CCK-8 assay Cytotoxicity against BALB/c mouse splenocytes after 48 hrs by CCK-8 assay	[PMID: 30500185]
Splenocyte	CC₅₀	1.2 μM Compound: CsA	Cytotoxicity against BALB/c mouse splenocytes assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay Cytotoxicity against BALB/c mouse splenocytes assessed as reduction in cell viability incubated for 48 hrs by CCK8 assay	[PMID: 31253536]
Splenocyte	CC₅₀	5.5 μM Compound: CsA	Cytotoxicity against BALB/c mouse splenocytes incubated for 48 hrs by MTT assay Cytotoxicity against BALB/c mouse splenocytes incubated for 48 hrs by MTT assay	[PMID: 37307145]
Splenocyte	CC₅₀	7.33 μM Compound: CsA	Cytotoxicity in BALB/c mouse Splenocyte assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxicity in BALB/c mouse Splenocyte assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 35678710]
Splenocyte	EC₅₀	0.03 μM Compound: Cyclosporine A	Immunosuppressive activity in BALB/c mouse splenocyte assessed as reduction in ConA-induced mouse T-lymphocytes proliferation incubated for 48 hrs by MTT assay Immunosuppressive activity in BALB/c mouse splenocyte assessed as reduction in ConA-induced mouse T-lymphocytes proliferation incubated for 48 hrs by MTT assay	[PMID: 36596229]
Splenocyte	IC₅₀	0.01 μg/mL Compound: Cyclosporine A	Antiproliferative activity against concanavalin A-stimulated BALB/c mouse splenocytes after 72 hrs by AlamarBlue assay Antiproliferative activity against concanavalin A-stimulated BALB/c mouse splenocytes after 72 hrs by AlamarBlue assay	[PMID: 23167554]
Splenocyte	IC₅₀	0.01 μM Compound: CsA	Immunosuppressive activity in splenocytes assessed as inhibition of concanavalin A-induced proliferation after 48 hrs by [3H]thymidine incorporation assay Immunosuppressive activity in splenocytes assessed as inhibition of concanavalin A-induced proliferation after 48 hrs by [3H]thymidine incorporation assay	[PMID: 19481938]
Splenocyte	IC₅₀	0.01 μM Compound: CsA	Immunosuppressive activity in mouse splenocytes assessed as inhibition of allogenic mixed lymphocyte reaction Immunosuppressive activity in mouse splenocytes assessed as inhibition of allogenic mixed lymphocyte reaction	[PMID: 19502058]
Splenocyte	IC₅₀	0.02 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of ConA-induced T cell proliferation by measuring [3H]-thymidine uptake by beta scintillation counter analysis Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of ConA-induced T cell proliferation by measuring [3H]-thymidine uptake by beta scintillation counter analysis	[PMID: 37307145]
Splenocyte	IC₅₀	0.03 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse Splenocyte assessed as inhibition of concanavalin A induced T-cell proliferation by [3H]-thymidine incorporation based beta scintillation counter analysis Immunosuppressive activity in BALB/c mouse Splenocyte assessed as inhibition of concanavalin A induced T-cell proliferation by [3H]-thymidine incorporation based beta scintillation counter analysis	[PMID: 35104138]
Splenocyte	IC₅₀	0.04 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A stimulated T-cell proliferation by measuring [3H]-thymidine uptake preincubated for 48 hrs followed by concanavalin A stimulation and [3H]-thymidine addition f Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A stimulated T-cell proliferation by measuring [3H]-thymidine uptake preincubated for 48 hrs followed by concanavalin A stimulation and [3H]-thymidine addition f	[PMID: 30500185]
Splenocyte	IC₅₀	0.04 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A-stimulated T-cell proliferation by measuring [3H]-thymidine uptake preincubated before concanavalin A stimulation for 48 hrs followed by [3H]-thymidine additio Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A-stimulated T-cell proliferation by measuring [3H]-thymidine uptake preincubated before concanavalin A stimulation for 48 hrs followed by [3H]-thymidine additio	[PMID: 31253536]
Splenocyte	IC₅₀	0.07 μM Compound: CsA	Immunosuppressive activity in splenocytes assessed as inhibition of LPS-induced proliferation after 48 hrs by [3H]thymidine incorporation assay Immunosuppressive activity in splenocytes assessed as inhibition of LPS-induced proliferation after 48 hrs by [3H]thymidine incorporation assay	[PMID: 19481938]
Splenocyte	IC₅₀	0.07 μg/mL Compound: Cyclosporine A	Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in ConA-induced mouse T-lymphocytes proliferation Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in ConA-induced mouse T-lymphocytes proliferation	[PMID: 38441877]
Splenocyte	IC₅₀	0.1 μM Compound: Cyclosporin A	Immunosupressive activity in OVA323-339 peptide-stimulated OT-2 T cell receptor transgenic mouse splenocytes assessed as inhibition of T cell proliferation after 3 days by MTT assay Immunosupressive activity in OVA323-339 peptide-stimulated OT-2 T cell receptor transgenic mouse splenocytes assessed as inhibition of T cell proliferation after 3 days by MTT assay	[PMID: 25537268]
Splenocyte	IC₅₀	0.17 μM Compound: Cyclosporine A	Immunosuppressive activity in mouse splenocyte assessed as reduction in ConA-induced mouse T-cell proliferation Immunosuppressive activity in mouse splenocyte assessed as reduction in ConA-induced mouse T-cell proliferation	[PMID: 38128907]
Splenocyte	IC₅₀	0.3 μM Compound: Cyclosporine A	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A-stimulated T-cell proliferation incubated for 48 hrs by MTT assay Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of concanavalin A-stimulated T-cell proliferation incubated for 48 hrs by MTT assay	[PMID: 33544615]
Splenocyte	IC₅₀	0.32 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse Splenocyte assessed as inhibition of LPS induced B-cell proliferation by [3H]-thymidine incorporation based beta scintillation counter analysis Immunosuppressive activity in BALB/c mouse Splenocyte assessed as inhibition of LPS induced B-cell proliferation by [3H]-thymidine incorporation based beta scintillation counter analysis	[PMID: 35104138]
Splenocyte	IC₅₀	0.4 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-stimulated B-cell proliferation by measuring [3H]-thymidine uptake preincubated for 48 hrs followed by LPS stimulation and [3H]-thymidine addition for 8 hrs measured afte Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-stimulated B-cell proliferation by measuring [3H]-thymidine uptake preincubated for 48 hrs followed by LPS stimulation and [3H]-thymidine addition for 8 hrs measured afte	[PMID: 30500185]
Splenocyte	IC₅₀	0.4 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-stimulated B-cell proliferation by measuring [3H]-thymidine uptake preincubated before LPS stimulation for 48 hrs followed by [3H]-thymidine addition for 8 hrs by beta-sc Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-stimulated B-cell proliferation by measuring [3H]-thymidine uptake preincubated before LPS stimulation for 48 hrs followed by [3H]-thymidine addition for 8 hrs by beta-sc	[PMID: 31253536]
Splenocyte	IC₅₀	0.55 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-induced B cell proliferation by measuring [3H]-thymidine uptake by beta scintillation counter analysis Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of LPS-induced B cell proliferation by measuring [3H]-thymidine uptake by beta scintillation counter analysis	[PMID: 37307145]
Splenocyte	IC₅₀	10 nM Compound: Cyclosporine A	Immunosuppressive activity in human splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay Immunosuppressive activity in human splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay	[PMID: 19827831]
Splenocyte	IC₅₀	10.15 μM Compound: CsA	Cytotoxicity against BALB/c mouse splenocyte assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay Cytotoxicity against BALB/c mouse splenocyte assessed as reduction in cell viability measured after 72 hrs by CCK-8 assay	[PMID: 33973788]
Splenocyte	IC₅₀	17 nM Compound: Cyclosporine A	Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay Immunosuppressive activity in BALB/c mouse splenocytes assessed as inhibition of [3H]thymidine incorporation after 4 days by allogenic mixed lymphocyte reaction assay	[PMID: 19827831]
Splenocyte	IC₅₀	30 nM Compound: 1, CsA	Immunosuppressant activity in mouse splenocytes by mixed-leukocyte reaction assay Immunosuppressant activity in mouse splenocytes by mixed-leukocyte reaction assay	[PMID: 23017885]
T cell line	CC₅₀	9.8 μM Compound: CsA	Cytotoxicity against BALB/c mouse T cell assessed as reduction in cell viability after 48 hrs by CCK8 assay Cytotoxicity against BALB/c mouse T cell assessed as reduction in cell viability after 48 hrs by CCK8 assay	[PMID: 32822186]
T cell line	IC₅₀	26 nM Compound: CsA	Antiproliferative activity against Con A-induced BALB/c mouse T cell after 48 hrs by CCK8 assay Antiproliferative activity against Con A-induced BALB/c mouse T cell after 48 hrs by CCK8 assay	[PMID: 32822186]
T-cell	CC₅₀	13.78 μM Compound: CsA	Cytotoxicity against lymph node T cell after 24 hrs by MTT assay Cytotoxicity against lymph node T cell after 24 hrs by MTT assay	[PMID: 22300886]
T-cell	CC₅₀	15.82 μM Compound: CsA	Cytotoxicity against BALB/c mouse T cells after 48 hrs by MTT assay Cytotoxicity against BALB/c mouse T cells after 48 hrs by MTT assay	[PMID: 21131104]
T-cell	CC₅₀	4.5 μM Compound: Cyclosporin A	Cytotoxic activity against BALB/c mouse T-lymphocytes assessed as reduction in cell viability incubated for 48 hrs by MTT assay Cytotoxic activity against BALB/c mouse T-lymphocytes assessed as reduction in cell viability incubated for 48 hrs by MTT assay	[PMID: 28294615]
T-cell	EC₅₀	6.4 nM Compound: CsA	Immunosuppressive activity in human PBMC assessed as inhibition of anti-human CD3-induced T-cell proliferation after 4 days by CellTrace violet cell proliferation dye based FACS analysis Immunosuppressive activity in human PBMC assessed as inhibition of anti-human CD3-induced T-cell proliferation after 4 days by CellTrace violet cell proliferation dye based FACS analysis	[PMID: 28075591]
T-cell	ED₅₀	50 nM Compound: Cyclosporin A	Inhibition of T-cell proliferation Inhibition of T-cell proliferation	[PMID: 15357990]
T-cell	IC₅₀	>10000 nM Compound: CSA	Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting	[PMID: 14593182]
T-cell	IC₅₀	>10 μM Compound: CSA	Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting	[PMID: 14593182]
T-cell	IC₅₀	0.00137 μM Compound: CsA	Inhibition of ConA-induced BALB/c mouse T cell proliferation Inhibition of ConA-induced BALB/c mouse T cell proliferation	[PMID: 17081761]
T-cell	IC₅₀	0.007 μM Compound: Cyclosporin A	Compound was tested for inhibition of IL-2 secretion in mouse T cell line Compound was tested for inhibition of IL-2 secretion in mouse T cell line	10.1016/S0960-894X(97)10005-1
T-cell	IC₅₀	0.011 μM Compound: CsA	Immunosuppressive activity in mouse T cells assessed as inhibition of two way mixed lymphocyte reaction after 4 days by MTT assay Immunosuppressive activity in mouse T cells assessed as inhibition of two way mixed lymphocyte reaction after 4 days by MTT assay	[PMID: 22984987]
T-cell	IC₅₀	0.03 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in ConA-induced mouse T-lymphocytes proliferation incubated for 8 hrs by beta scintillation counting based [3H]thymidine incorporation assay Immunosuppressive activity in BALB/c mouse splenocytes assessed as reduction in ConA-induced mouse T-lymphocytes proliferation incubated for 8 hrs by beta scintillation counting based [3H]thymidine incorporation assay	[PMID: 35678710]
T-cell	IC₅₀	0.04 μg/mL Compound: cyclosporin A	Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay	[PMID: 14738397]
T-cell	IC₅₀	0.04 μg/mL Compound: cyclosporin A	Immunosuppressant activity in mouse T cells assessed as inhibition of concanavalin A-induced cell proliferation Immunosuppressant activity in mouse T cells assessed as inhibition of concanavalin A-induced cell proliferation	[PMID: 11575965]
T-cell	IC₅₀	0.046 μg/mL Compound: Cyclosporin A	Immunosuppressive activity in guinea pig T cell assessed as inhibition of mitogenesis Immunosuppressive activity in guinea pig T cell assessed as inhibition of mitogenesis	[PMID: 3373220]
T-cell	IC₅₀	0.06 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of anti-CD3/anti-CD28-stimulated cell proliferation after 72 hrs by MTT assay Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of anti-CD3/anti-CD28-stimulated cell proliferation after 72 hrs by MTT assay	[PMID: 21131104]
T-cell	IC₅₀	0.07 μM Compound: CsA	Immunosuppressive activity in lymph node T cell assessed as inhibition of ConA-stimulated cell proliferation after 72 hrs by MTT assay Immunosuppressive activity in lymph node T cell assessed as inhibition of ConA-stimulated cell proliferation after 72 hrs by MTT assay	[PMID: 22300886]
T-cell	IC₅₀	0.08 μM Compound: Cyclosporin A	Inhibition of ConA-induced cell proliferation of BALB/c mouse T-lymphocytes assessed as reduction in [3H]thymidine incorporation incubated for 48 hrs by beta scintillation counting method Inhibition of ConA-induced cell proliferation of BALB/c mouse T-lymphocytes assessed as reduction in [3H]thymidine incorporation incubated for 48 hrs by beta scintillation counting method	[PMID: 28294615]
T-cell	IC₅₀	0.1 μM Compound: CsA	Immunosuppressive activity in BALB/c mouse T cells assessed as reduction in ConA-induced cell proliferation Immunosuppressive activity in BALB/c mouse T cells assessed as reduction in ConA-induced cell proliferation	[PMID: 32323537]
T-cell	IC₅₀	0.2 μM Compound: CsA	Immunosuppressant activity in human T lymphocytes assessed as inhibition of anti-human CD3 and anti-human CD28 monoclonal antibody-induced T lymphocyte proliferation incubated for 72 hrs by FACS analysis Immunosuppressant activity in human T lymphocytes assessed as inhibition of anti-human CD3 and anti-human CD28 monoclonal antibody-induced T lymphocyte proliferation incubated for 72 hrs by FACS analysis	[PMID: 31181920]
T-cell	IC₅₀	0.26 μM Compound: CsA	Inhibition of ConA-induced T lymphocytes (unknown origin) proliferation Inhibition of ConA-induced T lymphocytes (unknown origin) proliferation	[PMID: 29292227]
T-cell	IC₅₀	0.28 μg/mL Compound: Cyclosporin A	Immunosuppressive activity in human T cell assessed as inhibition of mitogenesis Immunosuppressive activity in human T cell assessed as inhibition of mitogenesis	[PMID: 3373220]
T-cell	IC₅₀	0.34 μM Compound: cyclosporin A	Inhibition of PHA-induced human T cell proliferation after 24 hrs by MTT assay Inhibition of PHA-induced human T cell proliferation after 24 hrs by MTT assay	[PMID: 11678649]
T-cell	IC₅₀	0.57 μM Compound: CsA	Inhibition of PI3K-gamma in mouse lymph node cells assessed as inhibition of ConA-stimulated T cell proliferation Inhibition of PI3K-gamma in mouse lymph node cells assessed as inhibition of ConA-stimulated T cell proliferation	[PMID: 26720154]
T-cell	IC₅₀	1.05 μM Compound: Cyclosporine A	Immunomodulatory activity in C57BL/6 mouse mesenteric lymph node T cells assessed as inhibition of concanavalin A stimulated T-cell proliferation incubated for 68 hrs by CCK-8 assay Immunomodulatory activity in C57BL/6 mouse mesenteric lymph node T cells assessed as inhibition of concanavalin A stimulated T-cell proliferation incubated for 68 hrs by CCK-8 assay	[PMID: 37017305]
T-cell	IC₅₀	1.34 M Compound: Cyclosporine A	In vitro concentration of compound required to inhibit ConA-induced T cell proliferation to 50% in BALB/c mice In vitro concentration of compound required to inhibit ConA-induced T cell proliferation to 50% in BALB/c mice	[PMID: 15999998]
T-cell	IC₅₀	1.34 x 10^-7M Compound: Cyclosporine A	In vitro concentration of compound required to inhibit ConA-induced T cell proliferation to 50% in BALB/c mice In vitro concentration of compound required to inhibit ConA-induced T cell proliferation to 50% in BALB/c mice	[PMID: 15999998]
T-cell	IC₅₀	13.7 nM Compound: CsA	In vitro inhibitory activity against human T-cell proliferation. In vitro inhibitory activity against human T-cell proliferation.	[PMID: 7537331]
T-cell	IC₅₀	14 nM Compound: cyclosporin A	Immunosuppressive activity in BALB/c/C57BL/6 mouse T cells assessed as inhibition of alloantigen-induced cell proliferation after 96 hrs by measuring [3H]thymidine uptake by mixed lymphocyte reaction assay Immunosuppressive activity in BALB/c/C57BL/6 mouse T cells assessed as inhibition of alloantigen-induced cell proliferation after 96 hrs by measuring [3H]thymidine uptake by mixed lymphocyte reaction assay	[PMID: 21456524]
T-cell	IC₅₀	2.12 μM Compound: csa	Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of ConA-induced T cell proliferation incubated 24 hrs post ConA-induction for 72 hrs by MTT assay Immunosuppressive activity in BALB/c mouse T cells assessed as inhibition of ConA-induced T cell proliferation incubated 24 hrs post ConA-induction for 72 hrs by MTT assay	[PMID: 22727369]
T-cell	IC₅₀	32 nM Compound: CSA	Inhibition of allogenic cells-stimulated proliferation in mouse T cells by mixed lymphocyte reaction method Inhibition of allogenic cells-stimulated proliferation in mouse T cells by mixed lymphocyte reaction method	[PMID: 14593182]
T-cell	IC₅₀	550 nM Compound: CsA	Immunosuppressive activity in concanavalin A-activated T cell assessed as inhibition of lymphoproliferation after 3 days by beta-scintillation counting Immunosuppressive activity in concanavalin A-activated T cell assessed as inhibition of lymphoproliferation after 3 days by beta-scintillation counting	[PMID: 19502058]
T-cell	IC₅₀	74 nM Compound: CSA	Inhibition of allogenic cells-stimulated proliferation in human T cells by mixed lymphocyte reaction method Inhibition of allogenic cells-stimulated proliferation in human T cells by mixed lymphocyte reaction method	[PMID: 14593182]
T-cell	IC₅₀	8.1 nM Compound: CsA	In vitro inhibitory activity against human T-cell production of lymphokine IL-2 In vitro inhibitory activity against human T-cell production of lymphokine IL-2	[PMID: 7537331]
T-cell	IC₅₀	8.97 μM Compound: CYA	Inhibition of CD4 expression in human CD4+ T cells Inhibition of CD4 expression in human CD4+ T cells	[PMID: 22101135]
Ventricular myocyte	IC₅₀	2 μM Compound: Cyclosporin A	Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes	[PMID: 22761000]
Vero	CC₅₀	>50 μM Compound: Cyclosporine	Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr	10.1101/2020.03.20.999730
Vero	IC₅₀	<=0.5 μM Compound: Cs	Antiviral activity against Dengue virus 1 infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay Antiviral activity against Dengue virus 1 infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay	[PMID: 19451286]
Vero	IC₅₀	>16.6 μM Compound: Cs	Antiviral activity against Yellow fever virus 17D infected in african green monkey Vero cells assessed as inhibition of viral replication Antiviral activity against Yellow fever virus 17D infected in african green monkey Vero cells assessed as inhibition of viral replication	[PMID: 18212100]
Vero	IC₅₀	>25 μM Compound: Cs	Antiviral activity against Coxsackie B3 infected in african green monkey Vero cells assessed as inhibition of viral replication Antiviral activity against Coxsackie B3 infected in african green monkey Vero cells assessed as inhibition of viral replication	[PMID: 18212100]
Vero	IC₅₀	>8.3 μM Compound: Cs	Antiviral activity against SARS coronavirus infected in african green monkey Vero cells assessed as inhibition of viral replication Antiviral activity against SARS coronavirus infected in african green monkey Vero cells assessed as inhibition of viral replication	[PMID: 18212100]
Vero	IC₅₀	≤ 0.5 μM Compound: Cs	Antiviral activity against Dengue virus 1 infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay Antiviral activity against Dengue virus 1 infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay	[PMID: 19451286]
Vero	IC₅₀	5.82 μM Compound: Cyclosporine	Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr	10.1101/2020.03.20.999730
Vero	IC₅₀	8 μM Compound: Cs	Antiviral activity against West Nile virus infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay Antiviral activity against West Nile virus infected in african green monkey Vero cells assessed as decrease in viral RNA synthesis after 24 hrs by luciferase reporter gene assay	[PMID: 19451286]

In Vitro

Cyclosporin A is able to bind with the cyclophilin in T cells^[1].
Cyclosporin A works by forming a Cyclophilin-Cyclosporin A complex to inhibit calcineurin^[2].
Cyclosporin A inhibits calcineurin in stimulated cells with an IC₅₀ value of 7 nM^[3].
Cyclosporin A suppresses the nuclear translocation of NF-AT^[4]. Cyclosporin A shows an effect on mitochondria via preventing the MTP from opening with an IC₅₀ of 39 nM^[5].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvente y solubilidad

In Vitro:

DMSO : 62.5 mg/mL (51.97 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 50 mg/mL (41.58 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	0.8315 mL	4.1576 mL	8.3152 mL
5 mM	0.1663 mL	0.8315 mL	1.6630 mL
10 mM	0.0832 mL	0.4158 mL	0.8315 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: 2.62 mg/mL (2.18 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.08 mg/mL (1.73 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (1.73 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

Pureza y Documentación

Purity: 99.94%

Ficha de datos (293 KB) SDS (419 KB)

COA (261 KB) HNMR (329 KB) RP-HPLC (235 KB) LCMS (92 KB)

Instrucciones de manejo (2659 KB)

Referencias

[1]. Handschumacher RE, et al. Cyclophilin: a specific cytosolic binding protein for cyclosporin A. Science. 1984 Nov 2;226(4674):544-7. [Content Brief]

[2]. Liu J, et al. Calcineurin is a common target of cyclophilin-cyclosporin A and FKBP-FK506 complexes. Cell. 1991 Aug 23;66(4):807-15. [Content Brief]

[3]. Fruman DA, et al. Calcineurin phosphatase activity in T lymphocytes is inhibited by FK 506 and cyclosporin A. Proc Natl Acad Sci U S A. 1992 May 1;89(9):3686-90. [Content Brief]

[4]. Flanagan WM, et al. Nuclear association of a T-cell transcription factor blocked by FK-506 and cyclosporin A. Nature. 1991 Aug 29;352(6338):803-7. [Content Brief]

[5]. Nicolli A, et al. Interactions of cyclophilin with the mitochondrial inner membrane and regulation of the permeability transition pore, and cyclosporin A-sensitive channel. J Biol Chem. 1996 Jan 26;271(4):2185-92. [Content Brief]

[6]. Borel JF, et al. Effects of the new anti-lymphocytic peptide cyclosporin A in animals. Immunology. 1977 Jun;32(6):1017-25. [Content Brief]

[7]. Williams, R, et al. Randomised trial comparing FK506 and cyclosporin in prevention of liver allograft rejection. European FK506 Multicentre Liver Study Group. Lancet, 1994, 344(8920), 423-428. [Content Brief]

[8]. Dalmarco EM, et al. Cyclosporin A inhibits CD11a/CD18 adhesion molecules due to inhibition of TNFalpha and IL-1 beta levels in the mouse model of pleurisy induced by carrageenan. Cell Adh Migr. 2008 Oct-Dec;2(4):231-5. [Content Brief]

[9]. Medeiros M, et al. Increased cyclosporine bioavailability induced by experimental nephrotic syndrome in rats. Can J Physiol Pharmacol. 2007 May;85(5):502-6. [Content Brief]

[10]. Nguyen LT, et al. Lysyl oxidase inhibitors attenuate cyclosporin A-induced nephropathy in mouse. Sci Rep. 2021 Jun 14;11(1):12437. [Content Brief]

[11]. Ling H, et al. Therapeutic role of TGF-beta-neutralizing antibody in mouse cyclosporin A nephropathy: morphologic improvement associated with functional preservation. J Am Soc Nephrol. 2003 Feb;14(2):377-88. [Content Brief]

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