Home Microbiology Reverse Transcriptase inhibitor Rilpivirine For research use only.

Rilpivirine

Synonyms: R278474, TMC278, DB08864

Rilpivirine (R278474, TMC27, DB08864) is a non-nucleoside reverse transcriptase inhibitor (NNRTI), and used to treat HIV-1 infection.

Rilpivirine Chemical Structure

Rilpivirine Chemical Structure

CAS: 500287-72-9

Selleck's Rilpivirine has been cited by 15 publications

Purity & Quality Control

Batch: Purity: 99.97%
99.97

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
MT4 cells Function assay Antiviral activity against wild type HIV1 LAI infected in MT4 cells by EGFP based replication assay, EC50=0.001 μM 17223230
MT4 cells Cytotoxicity assay 3 days Cytotoxicity against human MT4 cells after 3 days by EGFP based replication assay, CC50=2 μM 17223230
human PBMC cells Function assay Antiviral activity against Human immunodeficiency virus 1 subtype D isolate 92UG001 infected in human PBMC cells by cell based assay, EC50=0.00026 μM 19933797
human TZM-bl cells Cytotoxicity assay 4 days Cytotoxicity against human TZM-bl cells after 4 days by XTT assay, CC50=19.4 μM 22856541
human MT4 cells Function assay 72 h 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, EC50=0.0037 μM 23137340
MT2 cells Cytotoxicity assay Cytotoxicity in human MT2 cells assessed as inhibition of cell growth, CC50=8 μM 23298809
MT2 cells Function assay 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, EC50=0.002 μM 22081993
Click to View More Cell Line Experimental Data

Biological Activity

Description Rilpivirine (R278474, TMC27, DB08864) is a non-nucleoside reverse transcriptase inhibitor (NNRTI), and used to treat HIV-1 infection.
Features Approved anti-HIV drug with longer half-life and reduced side-effect profile than older NNRTIs.
Targets
Reverse transcriptase [1]
In vitro
In vitro Rilpivirine shows antiviral activity with EC50 ranging from 0.1 nM to 2 nM against wild-type and selected site-directed single and double mutants of HIV-1. [1] Rilpivirine inhibits viral replication at concentrations at which first-generation NNRTIs could not suppress replication, and produces a high genetic barrier to resistance development. [2]
In Vivo
In vivo After iv administration of Rilpivirine, Elimination half-life ranges from 4.4 h in rat to 31 h in dog. After oral administration of Rilpivirine in PEG 400, half-life ranges between 2.8 h in rat and 39 h in dog. [1]
Animal Research Animal Models Sprague−Dawley rat, beagle dog, white New Zealand rabbit, and cynomolgus monkey.
Dosages 4 mg/kg ( rat); 1.25 mg/kg (other species)
Administration i.v., p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06104306 Recruiting HIV-1-infection Gilead Sciences December 13 2023 Phase 4
NCT05601128 Recruiting HIV-1-infection|HIV Infections|HIV I Infection Allegheny Singer Research Institute (also known as Allegheny Health Network Research Institute) January 1 2023 Phase 3
NCT05112939 Active not recruiting Healthy Janssen Research & Development LLC November 16 2021 Phase 1
NCT05358756 Completed Healthy Subject Aptorum International Limited October 9 2021 Phase 1

Chemical lnformation & Solubility

Molecular Weight 366.42 Formula

C22H18N6
CAS No. 500287-72-9 SDF Download Rilpivirine SDF
Smiles CC1=CC(=CC(=C1NC2=NC(=NC=C2)NC3=CC=C(C=C3)C#N)C)C=CC#N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 73 mg/mL ( (199.22 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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