Etravirine

Research use only, not for human use.

A second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) for treatment of HIV-1 infection.

A second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI) for treatment of HIV-1 infection.HIV Infection Approved(In Vitro):TMC125 is highly active against wild-type HIV-1 (50% effective concentration [EC50]=1.4 to 4.8 nM) and shows some activity against HIV-2 (EC50=3.5 μM). TMC125 also inhibits a series of HIV-1 group M subtypes and circulating recombinant forms and a group O virus. TMC125 has activity for 19 viruses with EC50 of < 5 nM.(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.

TMC125 is highly active against wild-type HIV-1 (50% effective concentration [EC50]=1.4 to 4.8 nM) and shows some activity against HIV-2 (EC50=3.5 μM). TMC125 also inhibits a series of HIV-1 group M subtypes and circulating recombinant forms and a group O virus.?TMC125 has activity for 19 viruses with EC50 of < 5 nM.

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R-165335 | TMC-125

Microbiology/Virology

HIV

ReverseTranscriptase

Infection

HIV Infection

269055-15-4

435.2767

C20H15BrN6O

>98% (HPLC)

10 mM in DMSO

N#CC1=CC(C)=C(OC2=NC(NC3=CC=C(C#N)C=C3)=NC(N)=C2Br)C(C)=C1

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

(-20℃)

With Ice Pack

≥ 2 years