[CAS NO. 269055-15-4] Etravirine (TMC125)

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Catalog:	SLK-S3080
Brand:	Selleck
CAS:	269055-15-4

Overview

MDL	MFCD09837879
Molecular Weight	435.28
Molecular Formula	C20H15BrN6O
SMILES	O(C1=NC(NC2=CC=C(C#N)C=C2)=NC(N)=C1Br)C3=C(C)C=C(C#N)C=C3C

For research use only.

Storage

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

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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	2.2974 mL	11.4869 mL	22.9737 mL
5 mM	0.4595 mL	2.2974 mL	4.5947 mL
10 mM	0.2297 mL	1.1487 mL	2.2974 mL
50 mM	0.0459 mL	0.2297 mL	0.4595 mL

Description

Etravirine (TMC125, R-165335) is a non-nucleoside reverse transcriptase inhibitor () used for the treatment of HIV.

Targets

Reverse transcriptase ^[1]

In vitro

Etravirine (TMC125), is highly active against wild-type HIV-1 with EC50 of 1.4 nM to 4.8 nM and shows some activity against HIV-2 with EC50 of 3.5 μM. TMC125 also inhibits a series of HIV-1 group M subtypes and circulating recombinant forms and a group O virus.

In vivo

Etravirine has a high genetic barrier to the development of resistance. In phase IIb trials in treatment-experienced patients, including those infected with virus resistant to NNRTIs and protease inhibitors (PIs), TMC125 is active against HIV resistant to currently available NNRTIs, with a similar tolerability profile to that of the control group.

References

[1] Das K, et al. J Med Chem, 2004, 47(10), 2550-2560.
[2] Andries K, et al. Antimicrob Agents Chemother, 2004, 48(12), 4680-4686.
[3] Lazzarin A, et al. Lancet, 2007, 370(9581), 39-48.

Synonyms

Benzonitrile, 4-[[6-amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethyl-

4-[[6-Amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3,5-dimethylbenzonitrile

TMC 125

Etravirine

R 165335

Intelence

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