[CAS NO. 500287-72-9] Rilpivirine

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PRODUCTS SPECIFICATIONS [500287-72-9]

Catelog

SLK-S7303

Brand

Selleck

CAS

500287-72-9

DESCRIPTION [500287-72-9]

Overview

MDL	MFCD11046372
Molecular Weight	366.42
Molecular Formula	C22H18N6
SMILES	N(C1=C(C)C=C(/C=C/C#N)C=C1C)C2=NC(NC3=CC=C(C#N)C=C3)=NC=C2

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume 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
10 mM	0.2729 mL	1.3646 mL	2.7291 mL
50 mM	0.0546 mL	0.2729 mL	0.5458 mL

Description

Rilpivirine (R278474, TMC27, DB08864) is a , 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

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. Rilpivirine inhibits viral replication at concentrations at which first-generation NNRTIs could not suppress replication, and produces a high genetic barrier to resistance development.

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.

References

[1] Janssen PA, et al. J Med Chem. 2005, 48(6), 1901-1909.
[2] Azijn H, et al. Antimicrob Agents Chemother. 2010, 54(2), 718-727.

Synonyms

Benzonitrile, 4-[[4-[[4-[(1E)-2-cyanoethenyl]-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]-

4-[[4-[[4-[(1E)-2-Cyanoethenyl]-2,6-dimethylphenyl]amino]-2-pyrimidinyl]amino]benzonitrile

Rilpivirine

R 278474

TMC 278

Rekambys