Rilpivirine [500287-72-9]

Referência HY-10574-50mg

Tamanho : 50mg

Marca : MedChemExpress

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Telefone : +1 850 650 7790

Description

Rilpivirine (R278474) is a potent and specific diarylpyrimidine (DAPY) non-nucleoside reverse transcriptase inhibitor (NNRTI). Rilpivirine has high antiviral activity against wild-type HIV (EC50=0.4 nM) and mutant viruses (EC50=0.1-2.0 nM). Rilpivirine has a high genetic barrier to resistance development of HIV[1][2].

IC50 & Target

HIV-1

 

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.5 μM
Compound: 2; RPV
Inhibition of human ERG expressed in HEK293 cells by whole cell electrophysiology assay
Inhibition of human ERG expressed in HEK293 cells by whole cell electrophysiology assay
[PMID: 32293182]
HOS CC50
10 μM
Compound: Rilpivirine
Cytotoxicity against human HOS cells assessed as reduction in cell viability measured after 48 hrs
Cytotoxicity against human HOS cells assessed as reduction in cell viability measured after 48 hrs
[PMID: 35175760]
MT2 CC50
>1 μM
Compound: 39, Rilpivirine, R278474
Cytotoxicity against human MT2 cells infected with HIV1 NL4.3 by MTT assay
Cytotoxicity against human MT2 cells infected with HIV1 NL4.3 by MTT assay
[PMID: 22081993]
MT2 CC50
8 μM
Compound: Rilpivirine
Cytotoxicity against human MT2 cells by MTT assay
Cytotoxicity against human MT2 cells by MTT assay
[PMID: 23899617]
MT2 CC50
8 μM
Compound: Rilpivirine
Cytotoxicity against human MT2 cells assessed as growth inhibition by MTT method
Cytotoxicity against human MT2 cells assessed as growth inhibition by MTT method
[PMID: 27485603]
MT2 CC50
8 μM
Compound: Rilpivirine
Cytotoxicity against human MT2 cells infected with wild-type HIV1 NL4-3 measured 48 hrs by MTT assay
Cytotoxicity against human MT2 cells infected with wild-type HIV1 NL4-3 measured 48 hrs by MTT assay
[PMID: 31281023]
MT2 CC50
8 μM
Compound: Rilpivirine
Cytotoxicity against human MT2 cells assessed as cell growth inhibition after 5 days by MTT assay
Cytotoxicity against human MT2 cells assessed as cell growth inhibition after 5 days by MTT assay
[PMID: 33603971]
MT2 CC50
8 μM
Compound: rpv, 2, rilpivirine, R278474
Cytotoxicity against human MT2 cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against human MT2 cells assessed as reduction in cell viability by MTT assay
[PMID: 25408842]
MT2 CC50
8 μM
Compound: Rilpivirine
Cytotoxicity in human MT2 cells assessed as inhibition of cell growth
Cytotoxicity in human MT2 cells assessed as inhibition of cell growth
[PMID: 23298809]
MT2 CC50
8 μM
Compound: Rilpivirine
Cytotoxicity against human MT2 cells assessed as growth inhibition
Cytotoxicity against human MT2 cells assessed as growth inhibition
[PMID: 23937980]
MT2 CC50
90.7 μM
Compound: 1b, TMC278
Cytotoxicity against human MT2 cells assessed as cell viability
Cytotoxicity against human MT2 cells assessed as cell viability
[PMID: 25042339]
MT2 EC50
0.00065 μM
Compound: Rilpivirine
Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase Y181C mutation infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method
Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase Y181C mutation infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method
[PMID: 23298809]
MT2 EC50
0.00065 μM
Compound: Rilpivirine
Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay
Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay
[PMID: 23937980]
MT2 EC50
0.00065 μM
Compound: rpv, 2, rilpivirine, R278474
Antiviral activity against wild type HIV1 harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay
Antiviral activity against wild type HIV1 harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay
[PMID: 25408842]
MT2 EC50
0.00065 μM
Compound: 39, Rilpivirine, R278474
Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase Y181C mutant infected in human MT2 cells assessed as inhibition of viral infection
Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase Y181C mutant infected in human MT2 cells assessed as inhibition of viral infection
[PMID: 22081993]
MT2 EC50
0.00067 μM
Compound: Rilpivirine
Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method
Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method
[PMID: 23298809]
MT2 EC50
0.00067 μM
Compound: Rilpivirine
Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay
Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay
[PMID: 23937980]
MT2 EC50
0.00067 μM
Compound: rpv, 2, rilpivirine, R278474
Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay
Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay
[PMID: 25408842]
MT2 EC50
0.00067 μM
Compound: 39, Rilpivirine, R278474
Antiviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT2 cells assessed as inhibition of viral infection
Antiviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT2 cells assessed as inhibition of viral infection
[PMID: 22081993]
MT2 EC50
0.001 μM
Compound: Rilpivirine
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against virus-induced cytopathogenicity by MTT assay
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against virus-induced cytopathogenicity by MTT assay
[PMID: 23899617]
MT2 EC50
0.002 μM
Compound: Rilpivirine
Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase K103N and Y181C mutation infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method
Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase K103N and Y181C mutation infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method
[PMID: 23298809]
MT2 EC50
0.002 μM
Compound: Rilpivirine
Antiviral activity against HIV1 3B harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay
Antiviral activity against HIV1 3B harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay
[PMID: 23937980]
MT2 EC50
0.002 μM
Compound: rpv, 2, rilpivirine, R278474
Antiviral activity against wild type HIV1 harboring reverse transcriptase K103N/Y181C mutant infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay
Antiviral activity against wild type HIV1 harboring reverse transcriptase K103N/Y181C mutant infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay
[PMID: 25408842]
MT2 EC50
0.002 μM
Compound: 39, Rilpivirine, R278474
Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase K103N and Y181C double mutant infected in human MT2 cells assessed as inhibition of viral infection
Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase K103N and Y181C double mutant infected in human MT2 cells assessed as inhibition of viral infection
[PMID: 22081993]
MT2 EC50
0.49 nM
Compound: 1b
Antiviral activity against HIV1 3B infected in human MT2 cells measured on day 4 post infection by p24 ELISA method
Antiviral activity against HIV1 3B infected in human MT2 cells measured on day 4 post infection by p24 ELISA method
[PMID: 27070547]
MT2 EC50
0.49 nM
Compound: 1b, TMC278
Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as inhibition of viral replication
Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as inhibition of viral replication
[PMID: 25042339]
MT2 EC50
0.65 nM
Compound: 39, Rilpivirine, R278474
Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase Y181C mutant infected in human MT2 cells assessed as inhibition of viral infection
Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase Y181C mutant infected in human MT2 cells assessed as inhibition of viral infection
[PMID: 22081993]
MT2 EC50
0.65 nM
Compound: Rilpivirine
Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase Y181C mutation infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method
Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase Y181C mutation infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method
[PMID: 23298809]
MT2 EC50
0.65 nM
Compound: Rilpivirine
Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay
Antiviral activity against HIV1 3B harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay
[PMID: 23937980]
MT2 EC50
0.65 nM
Compound: rpv, 2, rilpivirine, R278474
Antiviral activity against wild type HIV1 harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay
Antiviral activity against wild type HIV1 harboring reverse transcriptase Y181C mutant infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay
[PMID: 25408842]
MT2 EC50
0.67 nM
Compound: 39, Rilpivirine, R278474
Antiviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT2 cells assessed as inhibition of viral infection
Antiviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT2 cells assessed as inhibition of viral infection
[PMID: 22081993]
MT2 EC50
0.67 nM
Compound: Rilpivirine
Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method
Antiviral activity against multidrug resistant HIV1 IIIB containing reverse transcriptase infected in human MT2 cells assessed as cytoprotection from infection by MTT colorimetric method
[PMID: 23298809]
MT2 EC50
0.67 nM
Compound: Rilpivirine
Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay
Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection against virus-induced effect by MTT assay
[PMID: 23937980]
MT2 EC50
0.67 nM
Compound: rpv, 2, rilpivirine, R278474
Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay
Antiviral activity against wild type HIV1 3B infected in human MT2 cells assessed as protection from virus-induced cytopathicity by MTT assay
[PMID: 25408842]
MT2 EC50
8 μM
Compound: Rilpivirine
Cytotoxicity against human MT2 cells assessed as cell viability by MTT assay
Cytotoxicity against human MT2 cells assessed as cell viability by MTT assay
[PMID: 35175760]
MT2 EC50
9.03 nM
Compound: 1b
Antiviral activity against multi-NRTI resistant HIV1 A17 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells measured on day 4 post infection by p24 ELISA method
Antiviral activity against multi-NRTI resistant HIV1 A17 harboring reverse transcriptase K103N/Y181C double mutant infected in human MT2 cells measured on day 4 post infection by p24 ELISA method
[PMID: 27070547]
MT2 EC50
9.03 nM
Compound: 1b, TMC278
Antiviral activity against wild type HIV1 A17 expressing K103N/Y181C mutant infected in human MT2 cells assessed as inhibition of viral replication
Antiviral activity against wild type HIV1 A17 expressing K103N/Y181C mutant infected in human MT2 cells assessed as inhibition of viral replication
[PMID: 25042339]
MT4 CC50
>4 μM
Compound: 2
Cytotoxicity against in human MT-4 cells after 5 days by MTT assay
Cytotoxicity against in human MT-4 cells after 5 days by MTT assay
[PMID: 33851529]
MT4 CC50
>4 μM
Compound: RPV; 2
Cytotoxicity against mock infected human MT4 cells by MTT assay
Cytotoxicity against mock infected human MT4 cells by MTT assay
[PMID: 34197708]
MT4 CC50
2 μM
Compound: 1, TMC278
Cytotoxicity against human MT4 cells after 3 days by EGFP based replication assay
Cytotoxicity against human MT4 cells after 3 days by EGFP based replication assay
[PMID: 17223230]
MT4 CC50
2000 nM
Compound: 1, TMC278
Cytotoxicity against human MT4 cells after 3 days by EGFP based replication assay
Cytotoxicity against human MT4 cells after 3 days by EGFP based replication assay
[PMID: 17223230]
MT4 CC50
3.98 μM
Compound: 2; RPV
Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay
[PMID: 32293182]
MT4 CC50
3.98 μM
Compound: RPV
Cytotoxicity in mock-infected human MT4 assessed as reduction in cell viability incubated for 5 days by MTT assay
Cytotoxicity in mock-infected human MT4 assessed as reduction in cell viability incubated for 5 days by MTT assay
[PMID: 33734714]
MT4 CC50
3.98 μM
Compound: RPV
Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability by MTT assay
[PMID: 34432448]
MT4 CC50
3.98 μM
Compound: RPV
Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay
Cytotoxicity against mock-infected human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay
[PMID: 34496571]
MT4 CC50
3.98 μM
Compound: RPV
Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay
[PMID: 35061384]
MT4 CC50
3.98 μM
Compound: RPV
Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by MTT assay
[PMID: 36411036]
MT4 CC50
3.98 μM
Compound: RPV
Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by MTT assay
[PMID: 36996328]
MT4 CC50
4.38 μM
Compound: RPV, TMC278; 2
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 5 days by MTT assay
[PMID: 30721060]
MT4 CC50
6.5 μM
Compound: RPV
Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by Cell Titer Glo luminescent assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability incubated for 5 days by Cell Titer Glo luminescent assay
[PMID: 36652602]
MT4 CC50
8 μM
Compound: 39, Rilpivirine, R278474
Cytotoxicity against human MT4 cells infected with HIV1 NL4.3 by MTT assay
Cytotoxicity against human MT4 cells infected with HIV1 NL4.3 by MTT assay
[PMID: 22081993]
MT4 EC50
0.0004 μM
Compound: TMC278
Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
[PMID: 23707918]
MT4 EC50
0.0004 μM
Compound: 39, Rilpivirine, R278474
Antiviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT4 cells assessed as inhibition of viral infection
Antiviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT4 cells assessed as inhibition of viral infection
[PMID: 22081993]
MT4 EC50
0.0005 μM
Compound: TMC-278
Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of viral replication
Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of viral replication
[PMID: 19666220]
MT4 EC50
0.00052 μM
Compound: TMC-278
Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 V370A mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA
Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 V370A mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA
[PMID: 22818973]
MT4 EC50
0.00055 μM
Compound: TMC-278
Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA
Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA
[PMID: 22818973]
MT4 EC50
0.001 μM
Compound: TMC278
Antiviral activity against HIV1 RES056 expressing RT K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
Antiviral activity against HIV1 RES056 expressing RT K103N/Y181C mutant infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
[PMID: 23707918]
MT4 EC50
0.001 μM
Compound: 39, Rilpivirine, R278474
Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase K103N and Y181C double mutant infected in human MT4 cells assessed as inhibition of viral infection
Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase K103N and Y181C double mutant infected in human MT4 cells assessed as inhibition of viral infection
[PMID: 22081993]
MT4 EC50
0.0013 μM
Compound: 39, Rilpivirine, R278474
Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral infection
Antiviral activity against Human immunodeficiency virus 1 NL4.3 reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral infection
[PMID: 22081993]
MT4 EC50
0.1 nM
Compound: 1, TMC278
Antiviral activity against HIV1 LAI with RT K103N mutation in MT4 cells by EGFP based replication assay
Antiviral activity against HIV1 LAI with RT K103N mutation in MT4 cells by EGFP based replication assay
[PMID: 17223230]
MT4 EC50
0.13 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype AG infected in human MT4 cells assessed as reduction in virus induced cytopathicity
Antiviral activity against Human immunodeficiency virus 1 subtype AG infected in human MT4 cells assessed as reduction in virus induced cytopathicity
[PMID: 19933797]
MT4 EC50
0.14 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype G infected in human MT4 cells assessed as reduction in virus induced cytopathicity
Antiviral activity against Human immunodeficiency virus 1 subtype G infected in human MT4 cells assessed as reduction in virus induced cytopathicity
[PMID: 19933797]
MT4 EC50
0.21 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype AE infected in human MT4 cells assessed as reduction in virus induced cytopathicity
Antiviral activity against Human immunodeficiency virus 1 subtype AE infected in human MT4 cells assessed as reduction in virus induced cytopathicity
[PMID: 19933797]
MT4 EC50
0.21 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype F1 infected in human MT4 cells assessed as reduction in virus induced cytopathicity
Antiviral activity against Human immunodeficiency virus 1 subtype F1 infected in human MT4 cells assessed as reduction in virus induced cytopathicity
[PMID: 19933797]
MT4 EC50
0.22 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype BG infected in human MT4 cells assessed as reduction in virus induced cytopathicity
Antiviral activity against Human immunodeficiency virus 1 subtype BG infected in human MT4 cells assessed as reduction in virus induced cytopathicity
[PMID: 19933797]
MT4 EC50
0.24 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype (H) infected in human MT4 cells assessed as reduction in virus induced cytopathicity
Antiviral activity against Human immunodeficiency virus 1 subtype (H) infected in human MT4 cells assessed as reduction in virus induced cytopathicity
[PMID: 19933797]
MT4 EC50
0.3 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype C infected in human MT4 cells assessed as reduction in virus induced cytopathicity
Antiviral activity against Human immunodeficiency virus 1 subtype C infected in human MT4 cells assessed as reduction in virus induced cytopathicity
[PMID: 19933797]
MT4 EC50
0.3 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype D infected in human MT4 cells assessed as reduction in virus induced cytopathicity
Antiviral activity against Human immunodeficiency virus 1 subtype D infected in human MT4 cells assessed as reduction in virus induced cytopathicity
[PMID: 19933797]
MT4 EC50
0.3 nM
Compound: TMC-278, RPV
Antiviral activity against HIV1 harboring reverse transcriptase K101N mutant infected in human MT4 cells
Antiviral activity against HIV1 harboring reverse transcriptase K101N mutant infected in human MT4 cells
[PMID: 24581546]
MT4 EC50
0.4 nM
Compound: 39, Rilpivirine, R278474
Antiviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT4 cells assessed as inhibition of viral infection
Antiviral activity against Human immunodeficiency virus 1 NL4.3 infected in human MT4 cells assessed as inhibition of viral infection
[PMID: 22081993]
MT4 EC50
0.4 nM
Compound: TMC278
Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of virus-induced cytopathic effect after 5 days by MTT assay
[PMID: 23707918]
MT4 EC50
0.44 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype A1 infected in human MT4 cells assessed as reduction in virus induced cytopathicity
Antiviral activity against Human immunodeficiency virus 1 subtype A1 infected in human MT4 cells assessed as reduction in virus induced cytopathicity
[PMID: 19933797]
MT4 EC50
0.5 nM
Compound: 1, TMC278
Antiviral activity against HIV1 LAI with RT F227C and V106A mutation in MT4 cells by EGFP based replication assay
Antiviral activity against HIV1 LAI with RT F227C and V106A mutation in MT4 cells by EGFP based replication assay
[PMID: 17223230]
MT4 EC50
0.5 nM
Compound: 1, TMC278
Antiviral activity against HIV1 LAI with RT F227C mutation in MT4 cells by EGFP based replication assay
Antiviral activity against HIV1 LAI with RT F227C mutation in MT4 cells by EGFP based replication assay
[PMID: 17223230]
MT4 EC50
0.5 nM
Compound: 1, TMC278
Antiviral activity against HIV1 LAI with RT L100I mutation in MT4 cells by EGFP based replication assay
Antiviral activity against HIV1 LAI with RT L100I mutation in MT4 cells by EGFP based replication assay
[PMID: 17223230]
MT4 EC50
0.5 nM
Compound: TMC278
Antiviral activity against HIV1 expressing wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay
Antiviral activity against HIV1 expressing wild type reverse transcriptase infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay
[PMID: 23137340]
MT4 EC50
0.5 nM
Compound: TMC278
Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay
Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase K103N mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay
[PMID: 23137340]
MT4 EC50
0.5 nM
Compound: TMC-278
Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of viral replication
Antiviral activity against HIV1 3B infected in human MT4 cells assessed as inhibition of viral replication
[PMID: 19666220]
MT4 EC50
0.5 nM
Compound: TMC-278, RPV
Antiviral activity against HIV1 harboring wild type reverse transcriptase infected in human MT4 cells
Antiviral activity against HIV1 harboring wild type reverse transcriptase infected in human MT4 cells
[PMID: 24581546]
MT4 EC50
0.52 nM
Compound: TMC-278
Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 V370A mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA
Antiviral activity against bevirimat-resistant HIV1 NL4-3 harboring QVT motif of Gag SP1 V370A mutant infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA
[PMID: 22818973]
MT4 EC50
0.55 nM
Compound: TMC-278
Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA
Antiviral activity against wild type HIV1 NL4-3 infected in human MT4 cells assessed as reduction of viral p24 level cells by fluorescence assay relative to wild type HIV1 NL4-3 after 4 days by ELISA
[PMID: 22818973]
MT4 EC50
0.73 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as reduction in virus induced cytopathicity
Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT4 cells assessed as reduction in virus induced cytopathicity
[PMID: 19933797]
MT4 EC50
1 nM
Compound: 1, TMC278
Antiviral activity against wild type HIV1 LAI infected in MT4 cells by EGFP based replication assay
Antiviral activity against wild type HIV1 LAI infected in MT4 cells by EGFP based replication assay
[PMID: 17223230]
MT4 EC50
1 nM
Compound: TMC-278, RPV
Antiviral activity against HIV1 harboring reverse transcriptase K101N/Y181C double mutant infected in human MT4 cells
Antiviral activity against HIV1 harboring reverse transcriptase K101N/Y181C double mutant infected in human MT4 cells
[PMID: 24581546]
MT4 EC50
1.2 nM
Compound: 1, TMC278
Antiviral activity against HIV1 LAI with RT Y188L mutation in MT4 cells by EGFP based replication assay
Antiviral activity against HIV1 LAI with RT Y188L mutation in MT4 cells by EGFP based replication assay
[PMID: 17223230]
MT4 EC50
1.3 nM
Compound: 1, TMC278
Antiviral activity against HIV1 LAI with RT Y181C mutation in MT4 cells by EGFP based replication assay
Antiviral activity against HIV1 LAI with RT Y181C mutation in MT4 cells by EGFP based replication assay
[PMID: 17223230]
MT4 EC50
1.3 nM
Compound: TMC278
Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay
Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay
[PMID: 23137340]
MT4 EC50
1.3 nM
Compound: TMC-278, RPV
Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells
Antiviral activity against HIV1 harboring reverse transcriptase Y181C mutant infected in human MT4 cells
[PMID: 24581546]
MT4 EC50
3.2 nM
Compound: 1, TMC278
Antiviral activity against HIV1 LAI with RT K103N and Y181C mutation in MT4 cells by EGFP based replication assay
Antiviral activity against HIV1 LAI with RT K103N and Y181C mutation in MT4 cells by EGFP based replication assay
[PMID: 17223230]
MT4 EC50
3.7 nM
Compound: TMC278
Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay
Antiviral activity against NNRTI-resistant HIV1 harboring reverse transcriptase Y188L mutant infected in human MT4 cells assessed as inhibition of viral replication after 72 hrs by HeLa-CD4-LTR-beta-gal assay
[PMID: 23137340]
MT4 EC50
5.22 μM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 2 ROD infected in human MT4 cells assessed as reduction in virus induced cytopathicity
Antiviral activity against Human immunodeficiency virus 2 ROD infected in human MT4 cells assessed as reduction in virus induced cytopathicity
[PMID: 19933797]
MT4 EC50
7.5 nM
Compound: 1, TMC278
Antiviral activity against HIV1 LAI with RT L100I and K103N mutation in MT4 cells by EGFP based replication assay
Antiviral activity against HIV1 LAI with RT L100I and K103N mutation in MT4 cells by EGFP based replication assay
[PMID: 17223230]
Neuron EC50
4.4 μM
Compound: RPV
Neurotoxicity in mouse primary neurons assessed as loss of MAP-2 intensity incubated for 48 hrs by imaging analysis
Neurotoxicity in mouse primary neurons assessed as loss of MAP-2 intensity incubated for 48 hrs by imaging analysis
[PMID: 37130343]
PBMC EC50
0.07 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92RW020 infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92RW020 infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
0.07 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG035 infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG035 infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
0.07 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype E isolate 93TH073 infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype E isolate 93TH073 infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
0.08 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype B isolate WEJO infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype B isolate WEJO infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
0.08 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype E isolate 92TH006 infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype E isolate 92TH006 infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
0.11 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 93MW959 infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 93MW959 infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
0.16 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR020 infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR020 infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
0.19 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR029 infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR029 infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
0.23 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype B isolate 93BR021 infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype B isolate 93BR021 infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
0.24 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92UG037 infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92UG037 infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
0.25 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype G isolate G3 infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype G isolate G3 infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
0.26 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG001 infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG001 infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
0.26 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype G isolate JV1083 infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype G isolate JV1083 infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
0.33 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 92BR025 infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 92BR025 infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
0.38 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG024 infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG024 infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
0.44 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92UG029 infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype A isolate 92UG029 infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
0.51 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype B isolate JR-CSF infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype B isolate JR-CSF infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
0.51 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype G isolate RU132 infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype G isolate RU132 infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
0.53 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 93IN101 infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype C isolate 93IN101 infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
0.95 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR019 infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype F isolate 93BR019 infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
1.01 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype E isolate CMU08 infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype E isolate CMU08 infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
2.88 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype O isolate BCF02 infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype O isolate BCF02 infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
3.13 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype O misolate BCF01 infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype O misolate BCF01 infected in human PBMC cells by cell based assay
[PMID: 19933797]
PBMC EC50
8.45 nM
Compound: TMC278, rilpivirine
Antiviral activity against Human immunodeficiency virus 1 subtype O isolate BCF03 infected in human PBMC cells by cell based assay
Antiviral activity against Human immunodeficiency virus 1 subtype O isolate BCF03 infected in human PBMC cells by cell based assay
[PMID: 19933797]
T-cell CC50
8 μM
Compound: Rilpivirine
Cytotoxicity against human CD4-positive T cells
Cytotoxicity against human CD4-positive T cells
[PMID: 26487915]
T-cell EC50
1142 nM
Compound: Rilpivirine
Antiviral activity against HIV-1 X4 expressing reverse transcriptase K101P mutant infected in human CD4+ T cells for 3 days by FACS analysis
Antiviral activity against HIV-1 X4 expressing reverse transcriptase K101P mutant infected in human CD4+ T cells for 3 days by FACS analysis
[PMID: 26487915]
T-cell EC50
13 nM
Compound: Rilpivirine
Antiviral activity against HIV-1 X4 expressing reverse transcriptase K103N mutant infected in human CD4+ T cells for 3 days by FACS analysis
Antiviral activity against HIV-1 X4 expressing reverse transcriptase K103N mutant infected in human CD4+ T cells for 3 days by FACS analysis
[PMID: 26487915]
T-cell EC50
13 nM
Compound: Rilpivirine
Antiviral activity against HIV-1 X4 expressing wild-type reverse transcriptase infected in human CD4+ T cells for 3 days by FACS analysis
Antiviral activity against HIV-1 X4 expressing wild-type reverse transcriptase infected in human CD4+ T cells for 3 days by FACS analysis
[PMID: 26487915]
T-cell EC50
51 nM
Compound: Rilpivirine
Antiviral activity against HIV-1 X4 expressing reverse transcriptase Y181C mutant infected in human CD4+ T cells for 3 days by FACS analysis
Antiviral activity against HIV-1 X4 expressing reverse transcriptase Y181C mutant infected in human CD4+ T cells for 3 days by FACS analysis
[PMID: 26487915]
TZM CC50
>273 nM
Compound: 2
Cytotoxicity against human TZM-bl cells infected with HIV1 NL4-3
Cytotoxicity against human TZM-bl cells infected with HIV1 NL4-3
[PMID: 28465101]
TZM CC50
>30 μM
Compound: 1b
Cytotoxicity against human TZM-bl cells assessed as reduction in cell viability after 1 day by CytoTox-Glo assay
Cytotoxicity against human TZM-bl cells assessed as reduction in cell viability after 1 day by CytoTox-Glo assay
[PMID: 27070547]
TZM CC50
>341 nM
Compound: RPV; TMC278
Cytotoxicity against human TZM-bl cells by CytoTox-Glo reagent-based assay
Cytotoxicity against human TZM-bl cells by CytoTox-Glo reagent-based assay
[PMID: 29635166]
TZM CC50
>5 μM
Compound: RPV
Cytotoxicity against human TZM-bl cells assessed as reduction in cell viability by MTS assay
Cytotoxicity against human TZM-bl cells assessed as reduction in cell viability by MTS assay
[PMID: 37130343]
TZM CC50
>5 μM
Compound: RPV
Cytotoxicity against human TZM-bl cells assessed as reduction in viability incubated for 48 hrs by MTT assay
Cytotoxicity against human TZM-bl cells assessed as reduction in viability incubated for 48 hrs by MTT assay
[PMID: 37130343]
TZM CC50
19.4 μM
Compound: 2
Cytotoxicity against human TZM-bl cells after 4 days by XTT assay
Cytotoxicity against human TZM-bl cells after 4 days by XTT assay
[PMID: 22856541]
TZM CC50
19.4 μM
Compound: 2, TMC278
Cytotoxicity against human TZM-bl cells
Cytotoxicity against human TZM-bl cells
[PMID: 22406117]
In Vitro

Rilpivirine is active against wild-type HIV-1 (EC50=0.4 nM) and all single and double mutants tested (EC50=0.1-2.0 nM)[1].
Rilpivirine (10-5000 nM; 30 d) does not observe the sign of wild-type HIV-1 breakthrough at 1 μM within 30 days[1].
Rilpivirine inhibits 81% of clinical isolates (about 1200 recombinant clinical isolates) at a 50% inhibitory concentration (EC50) less than 1 nM, and inhibits 94% at EC50 less than 10 nM[1].
Rilpivirine shows subnanomolar EC50s against wild-type HIV-1 group M isolates (0.07-1.01 nM) and nanomolar EC50s against group O isolates (2.88-8.45 nM) in MT4 T-cells[2].

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

Solvant et solubilité
In Vitro: 

DMSO : 18.18 mg/mL (49.62 mM; ultrasonic and warming and adjust pH to 2 with 1 M HCl and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7291 mL 13.6455 mL 27.2911 mL
5 mM 0.5458 mL 2.7291 mL 5.4582 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 3 mg/mL (8.19 mM); Clear solution

    This protocol yields a clear solution of ≥ 3 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (30.0 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 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 3 mg/mL (8.19 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 3 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 (30.0 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.
Pureté et documentation
Références

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Referência
Descrição
Cond.
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A11542-10
 10mg 
A11542-25
 25mg