4-[[2-[(4-氰基苯基)氨基]-5-溴-6-氨基]-4-嘧啶基氧基

发布者：信康浏览次数：

产品名称:4-[[2-[(4-氰基苯基)氨基]-5-溴-6-氨基]-4-嘧啶基氧基]-3,5-二甲基苯腈

CAS:269055-15-4

别名：4-[[2-[(4-氰基苯基)氨基]-5-溴-6-氨基]-4-嘧啶基氧基]-3,5-二甲基苯腈;依曲韦林;依曲韦林;依曲韦林-D6;依曲韦林合成工艺

英文名：4-[[6-amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3, 5 –dimethylbenzonitrile

[]

生物活性Etravirine (TMC125)是一种非核苷类逆转录酶抑制剂(NNRTI)，用于治疗HIV。
体外研究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.
体内研究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.