Name: Rilpivirine
Brand: Selleck Chemicals
SKU: S7303
Rating: 5 (15 reviews)

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

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

Rilpivirine Related Products

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Signaling Pathway

Reverse Transcriptase Signaling Pathway

Choose Selective Reverse Transcriptase Inhibitors

Cell Data

Cell Lines	Assay Type	Incubation Time	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

References

Chemical Information & 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

In vitro
Batch:

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

Water : Insoluble

Ethanol : Insoluble

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

Preparing Stock Solutions

Molarity Calculator

Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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

Tel: +1-832-582-8158 Ext:3
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