Etravirine

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

用于治疗 HIV-1 感染的第二代非核苷逆转录酶抑制剂 (NNRTI)。

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.

——

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