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Reagentes e instrumentos para imunologia, biologia celular e biologia molecular.

Tacrolimus [104987-11-3]

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Referência HY-13756-10mg

Tamanho : 10mg

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Marca : MedChemExpress

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Telefone : +1 850 650 7790

Description

Tacrolimus (FK506), a macrocyclic lactone, binds to FK506 binding protein (FKBP) to form a complex. Tacrolimus inhibits calcineurin phosphatase, which inhibits T-lymphocyte signal transduction and IL-2 transcription. Immunosuppressive properties^[1].

IC₅₀ & Target

Macrolide

Cellular Effect

Cell Line	Type	Value	Description	References
B-cell	IC₅₀	1.6 ng/mL Compound: FK-506	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	1.6 x 10^-3μg/mL Compound: FK-506	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]
CD4+ve Th	IC₅₀	0.034 nM Compound: 1; FK506	Immunosuppressive activity in C57BL/6J mouse CD4+ve T cells assessed as inhibition of CD3/CD28-stimulated CD4+ve T cell proliferation incubated for 72 hrs by CellTrace-violet staining based flow cytometry analysis Immunosuppressive activity in C57BL/6J mouse CD4+ve T cells assessed as inhibition of CD3/CD28-stimulated CD4+ve T cell proliferation incubated for 72 hrs by CellTrace-violet staining based flow cytometry analysis	[PMID: 33534559]
HEK293	IC₅₀	3.7 μM Compound: FK506	TP_TRANSPORTER: inhibition of Phalloidin uptake (Phalloidin: 1 uM) in OATP-C-expressing HEK293 cells TP_TRANSPORTER: inhibition of Phalloidin uptake (Phalloidin: 1 uM) in OATP-C-expressing HEK293 cells	[PMID: 14530907]
HepG2	IC₅₀	>100 μM Compound: 1; FK-506	Cytotoxicity against human HepG2 cells Cytotoxicity against human HepG2 cells	[PMID: 28412204]
Jurkat	IC₅₀	0.056 nM Compound: 1, FK506	Inhibition of calcineurin in human Jurkat cells assessed as inhibition of NFAT-mediated IL-2 production after 8 hrs by beta-lactamase reporter gene assay Inhibition of calcineurin in human Jurkat cells assessed as inhibition of NFAT-mediated IL-2 production after 8 hrs by beta-lactamase reporter gene assay	10.1039/C2MD20266B
Jurkat	IC₅₀	0.19 nM Compound: FK-506	Inhibitory activity against IL-2 receptor in human T-cell jurkat cell line stimulated by phytohemagglutininin and phorbol myristate acetate Inhibitory activity against IL-2 receptor in human T-cell jurkat cell line stimulated by phytohemagglutininin and phorbol myristate acetate	[PMID: 15369399]
Jurkat	IC₅₀	0.36 μM Compound: 1; FK-506	Immunosuppressive activity in PMA/ionomycin stimulated human Jurkat T cells assessed as suppression of IL2 production pretreated for 15 to 30 mins followed by PMA/ionomycin addition measured after 18 to 20 hrs by ELISA Immunosuppressive activity in PMA/ionomycin stimulated human Jurkat T cells assessed as suppression of IL2 production pretreated for 15 to 30 mins followed by PMA/ionomycin addition measured after 18 to 20 hrs by ELISA	[PMID: 28412204]
Jurkat	IC₅₀	5.8 μM Compound: FK506	Anti-inflammatory activity in PMA/ionomycin stimulated human Jurkat T cells assessed as reduction in IL-2 secretion preincubated for 20 mins followed by PMA/ionomycin stimulation measured after 12 hrs by ELISA Anti-inflammatory activity in PMA/ionomycin stimulated human Jurkat T cells assessed as reduction in IL-2 secretion preincubated for 20 mins followed by PMA/ionomycin stimulation measured after 12 hrs by ELISA	[PMID: 28509552]
PBMC	IC₅₀	0.29 nM Compound: FK-506	Inhibitory activity against murine mixed lymphocyte reaction Inhibitory activity against murine mixed lymphocyte reaction	[PMID: 15369399]
RBL-2H3	IC₅₀	0.25 nM Compound: FK506	Inhibition of TNF-alpha production in rat RBL2H3 cells after 16 hrs by ELISA Inhibition of TNF-alpha production in rat RBL2H3 cells after 16 hrs by ELISA	[PMID: 23791076]
RBL-2H3	IC₅₀	0.25 nM Compound: FK-506	Antiinflammatory activity in rat RBL2H3 cells assessed as inhibition of DNP-BSA-induced TNF-alpha production preincubated for 15 mins prior DNP-BSA challenge measured after 30 mins by ELISA Antiinflammatory activity in rat RBL2H3 cells assessed as inhibition of DNP-BSA-induced TNF-alpha production preincubated for 15 mins prior DNP-BSA challenge measured after 30 mins by ELISA	[PMID: 22410084]
RBL-2H3	IC₅₀	0.25 nM Compound: FK-506	Inhibition of DNP7-BSA antigen-induced TNFalpha release in rat RBL-2H3 cells Inhibition of DNP7-BSA antigen-induced TNFalpha release in rat RBL-2H3 cells	[PMID: 16901696]
T-cell	IC₅₀	0.18 nM Compound: 1 (FK-506)	Agonistic activity in a murine splenic T-cell proliferation assay was calculated by measurement of [3H]thymidine uptake relative to control Agonistic activity in a murine splenic T-cell proliferation assay was calculated by measurement of [3H]thymidine uptake relative to control	10.1016/S0960-894X(01)81248-8
T-cell	IC₅₀	0.29 nM Compound: 1 (FK-506)	In vitro evaluation for immunosuppressive activity against proliferation of antigen stimulated murine splenic T cells In vitro evaluation for immunosuppressive activity against proliferation of antigen stimulated murine splenic T cells	10.1016/S0960-894X(01)80264-X
T-cell	IC₅₀	0.29 nM Compound: 1 (FK-506)	In vitro immunosuppressive activity against proliferation of antigen stimulated murine splenic T cells In vitro immunosuppressive activity against proliferation of antigen stimulated murine splenic T cells	10.1016/S0960-894X(01)80265-1
T-cell	IC₅₀	0.5 nM Compound: FK-506	In vitro inhibitory activity against human T-cell proliferation. In vitro inhibitory activity against human T-cell proliferation.	[PMID: 7537331]
T-cell	IC₅₀	0.9 nM Compound: FK-506	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	1.5 x 10^-5μg/mL Compound: FK-506	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	1.5 x 10^-5μg/mL Compound: FK-506	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	1.5*10^-5μg/mL Compound: FK-506	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	1.5*10^-5μg/mL Compound: FK-506	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]
U-251	IC₅₀	13.8 nM Compound: 1	Inhibition of SAP130 in VEGF-stimulated human U251 cells by PLAP reporter gene assay Inhibition of SAP130 in VEGF-stimulated human U251 cells by PLAP reporter gene assay	[PMID: 17643112]
Vero 76	IC₅₀	>100 μM Compound: 1; FK-506	Cytotoxicity against African green monkey Vero 76 cells Cytotoxicity against African green monkey Vero 76 cells	[PMID: 28412204]
WiDr	IC₅₀	10.9 nM Compound: 1	Inhibition of SAP130 mediated cell growth in human WiDr cells Inhibition of SAP130 mediated cell growth in human WiDr cells	[PMID: 17643112]

In Vitro

Tacrolimus (FK506) inhibits calcium-dependent events, such as IL-2 gene transcription, NO synthase activation, cell degranulation, and apoptosis. Tacrolimus also potentiates the actions of glucocorticoids and progesterone by binding to FKBPs contained within the hormone receptor complex, preventing degradation. The agent may enhance expression of the TGFβ-1 gene in a fashion analogous to that demonstrated for CsA. T cell proliferation in response to ligation of the T cell receptor is inhibited by Tacrolimus^[1]. Treatment with a low concentration of Tacrolimus (FK506,10 μg/L) does not significantly affect the proliferation of MH3924A cells (P=0.135). Upon treatment with higher concentrations of Tacrolimus (100-1,000 μg/L), the proliferation of MH3924A cells is significantly enhanced (P<0.01). Treatment with AMD3100 at any concentration (10, 50 or 100 μg/L), has no obvious effect on MH3924A cell proliferation (P>0.05). However, when different concentrations of AMD3100 are combined with 100 μg/L Tacrolimus, the in vitro proliferation of MH3924A cells is increased (P<0.01)^[3].

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

Solvant et solubilité

In Vitro:

DMSO : 125 mg/mL (155.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 12.5 mg/mL (15.55 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.2438 mL	6.2188 mL	12.4375 mL
5 mM	0.2488 mL	1.2438 mL	2.4875 mL
10 mM	0.1244 mL	0.6219 mL	1.2438 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: 2.75 mg/mL (3.42 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (3.11 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2.5 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 (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (3.11 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Pureté et documentation

Purity: 99.93%

Fiche technique (288 KB) SDS (644 KB)

COA (262 KB) HNMR (300 KB) RP-HPLC (260 KB) LCMS (100 KB) Elemental Analysis Report (118 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Thomson AW, et al. Mode of action of Tacrolimus (FK506): molecular and cellular mechanisms. Ther Drug Monit. 1995 Dec;17(6):584-91. [Content Brief]

[2]. Vogel KR, et al. mTOR inhibitors rescue premature lethality and attenuate dysregulation of GABAergic/glutamatergic transcription in murine succinate semialdehyde dehydrogenase deficiency (SSADHD), a disorder of GABA metabolism. J Inherit Metab Dis. 2016 Nov;39(6):877-886. [Content Brief]

[3]. Zhu H, et al. Tacrolimus promotes hepatocellular carcinoma and enhances CXCR4/SDF 1α expression in vivo. Mol Med Rep. 2014 Aug;10(2):585-92. [Content Brief]

[4]. Okada Y, et al. Tacrolimus ameliorates dextran sulfate sodium-induced colitis in mice: implication of interleukin-1β suppression. Biol Pharm Bull. 2011;34(12):1823-7. [Content Brief]

[5]. Yuwei He, et al. Drug targeting through platelet membrane-coated nanoparticles for the treatment of rheumatoid arthritis. Nano Res. 30 June 2018.

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Tacrolimus [104987-11-3]

Referência HY-13756-10mg

Contactar o distribuidor local :

Marca : MedChemExpress

Contactar o distribuidor local :

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