Cat. No.: HY-10574

Rilpivirine

(Synonyms: R278474; TMC278; DB08864)

11 Cited Publications

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Based on 11 publication(s) in Google Scholar

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.

For research use only. We do not sell to patients.

Purity: 99.67%
CAS No.: 500287-72-9
Formula: C₂₂H₁₈N₆
Molecular Weight:366.42

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Rilpivirine Chemical Structure

CAS No.: 500287-72-9

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
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- IC₅₀ & Target
- Cellular Effect
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- In Vivo
- Clinical Trial
Chemical Information
Publications (11)
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Bioz

Biological Activity

Description

IC₅₀ & Target

HIV-1

All HIV Isoforms :

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	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	0.00065 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: 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	0.65 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	0.67 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	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	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	0.00065 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	0.00067 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	0.65 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	0.67 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	CC₅₀	8 μM Compound: Rilpivirine	Cytotoxicity against human MT2 cells by MTT assay Cytotoxicity against human MT2 cells by MTT assay	[PMID: 23899617]
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	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	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	0.00065 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	0.00067 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	0.65 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	0.67 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	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	0.49 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	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]
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	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	0.00065 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	0.00067 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	0.65 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: 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	0.49 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	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	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	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]
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	0.5 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	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	1.2 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	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	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]
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	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	0.5 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	0.13 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	0.44 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	0.73 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	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	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	0.001 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	0.0004 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	0.4 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	0.00052 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	0.52 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	0.5 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	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	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	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	0.0004 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	0.4 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	0.3 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	0.5 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	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	1.3 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	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	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	>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	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	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	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]
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	19.4 μM Compound: 2, TMC278	Cytotoxicity against human TZM-bl cells Cytotoxicity against human TZM-bl cells	[PMID: 22406117]
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	>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	>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	>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]

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.

In Vivo

Rilpivirine (10-160 mg/kg; p.o. for 1 month) does not produce abnormal effects in rat, apart from liver weight increase and species-specific thyroid hypertrophy, both at the higher dose levels^[1].
Rilpivirine (i.v.) exhibits elimination half-life ranges from 4.4 h in rat to 31 h in dog, and exposure (AUC_inf) amounts to 3.1 μg·h/mL (4 mg/kg) in rat, 8.7 μg·h/mL (1.25 mg/kg) in dog, 1.4 μg·h/mL (1.25 mg/ kg) in monkey, and 44 μg·h/mL (1.25 mg/kg) in rabbit^[1].
Rilpivirine (p.o.) exhibits half-life ranges between 2.8 h in rat and 39 h in dog, and oral bioavailability of 32% and 31% in rat and dog^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 500287-72-9
Appearance Solid
Molecular Weight 366.42
Formula C₂₂H₁₈N₆
Color Light yellow to yellow
SMILES

CC1=CC(/C=C/C#N)=CC(C)=C1NC2=CC=NC(NC3=CC=C(C=C3)C#N)=N2
Synonyms

R278474; TMC278; DB08864
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (11)

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Journal Impact Factor

J Med Chem

Selective and Orally Bioavailable Dipeptidyl Peptidase 9 Inhibitors with Potent Pyroptosis Induction Properties. [Abstract]

2025 Oct 29. PMID: 41160575
Br J Cancer

Transcriptome analysis of newly established carboplatin-resistant ovarian cancer cell model reveals genes shared by drug resistance and drug-induced EMT. [Abstract]

2023 Mar;128(7):1344-1359. PMID: 36717670
Pharmaceuticals (Basel)

Combined In Silico and In Vitro Evidence Supporting an Aurora A Kinase Inhibitory Role of the Anti-Viral Drug Rilpivirine and an Anti-Proliferative Influence on Cancer Cells. [Abstract]

2022 Sep 25;15(10):1186. PMID: 36297298
Int J Antimicrob Agents

Efficacy of antiretroviral compounds against Toxoplasma gondii in vitro. [Abstract]

2019 Dec;54(6):814-819. PMID: 31479744
Sci Rep

NMR characterization of HIV-1 reverse transcriptase binding to various non-nucleoside reverse transcriptase inhibitors with different activities. [Abstract]

2015 Oct 29;5:15806. PMID: 26510386
PLoS One

Development of a novel in vitro assay to screen for neuroprotective drugs against iatrogenic neurite shortening. [Abstract]

2021 Mar 10;16(3):e0248139. PMID: 33690613
Biol Pharm Bull

Mass Spectrometric Characterization of HIV-1 Reverse Transcriptase Interactions with Non-nucleoside Reverse Transcriptase Inhibitors. [Abstract]

2016;39(3):450-4. PMID: 26934936
chemRxiv

2026 Apr 6.
SSRN

2023 Sep 8.
University of Rijeka

2023.
University of Oxford

2019 Jul.

Solvent & Solubility

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.7291 mL

13.6455 mL

27.2911 mL

5 mM

0.5458 mL

2.7291 mL

5.4582 mL

10 mM

0.2729 mL

1.3646 mL

2.7291 mL

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.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

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

This protocol yields a clear solution of ≥ 3 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 (30.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (272 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Janssen PAJ, et, al. In search of a novel anti-HIV drug: multidisciplinary coordination in the discovery of 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2- pyrimidinyl]amino]benzonitrile (R278474, rilpivirine). J Med Chem. 2005 Mar 24;48(6):1901-9. [Content Brief]

[2]. Azijn H, et, al. TMC278, a next-generation nonnucleoside reverse transcriptase inhibitor (NNRTI), active against wild-type and NNRTI-resistant HIV-1. Antimicrob Agents Chemother. 2010 Feb;54(2):718-27. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7291 mL	13.6455 mL	27.2911 mL	68.2277 mL
	5 mM	0.5458 mL	2.7291 mL	5.4582 mL	13.6455 mL
	10 mM	0.2729 mL	1.3646 mL	2.7291 mL	6.8228 mL
	15 mM	0.1819 mL	0.9097 mL	1.8194 mL	4.5485 mL
	20 mM	0.1365 mL	0.6823 mL	1.3646 mL	3.4114 mL
	25 mM	0.1092 mL	0.5458 mL	1.0916 mL	2.7291 mL
	30 mM	0.0910 mL	0.4549 mL	0.9097 mL	2.2743 mL
	40 mM	0.0682 mL	0.3411 mL	0.6823 mL	1.7057 mL

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Rilpivirine

Anti-Infection Compound Library

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Antiviral Compound Library

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Publications Citing Use of MedChemExpress (MCE) Rilpivirine

All HIV Isoforms

Biological Activity

Chemical Information

Publications (11)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Rilpivirine

Anti-Infection Compound Library

FDA-Approved Drug Library

Antiviral Compound Library

Drug Repurposing Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Rare Diseases Drug Library

Pediatric Drug Library

EMA-Approved Drug Library

Human Metabolite Library

Heterocyclic Compound Library

Off-patent Drug Library

Cysteine Targeted Covalent Library

Highly Selective Inhibitors Library

Anti-Drug-Resistant Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Nephrotoxicity Compound Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Rilpivirine

All HIV Isoforms

Biological Activity

Chemical Information

Publications (11)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Rilpivirine Related Classifications

Cat. No.: HY-10574