中文同义词:
依曲韦林;依曲韦林-D6;依曲韦林合成工艺;依曲韦林;伊曲韦林;4 - ((6-氨基-5-溴-2 - ((4-氰基苯基)氨基)嘧啶-4-基)氧基)-3,5-二甲基苄腈;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;4-((6-氨基-5-溴-2-((4-氰基苯基)氨基)嘧啶-4-基)氧基)-3,5-二甲基苯甲腈
英文名称:
4-[[6-amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3, 5 –dimethylbenzonitrile
英文同义词:
4-[[6-amino-5-bromo-2-[(4-cyanophenyl)amino]-4-pyrimidinyl]oxy]-3, 5 –dimethylbenzonitrile;Etravirine;Etravirine（TMC-125）;R 165335;TMC 125;4-(6-amino-5-bromo-2-(4-cyanobenzyl)pyrimidin-4-yloxy)-3,5-dimethylbenzonitrile, Etravirine;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/Etravirine
相关类别:
原料药;新型抗HIV药;信号转导通路激酶抑制剂;杂环类;原料药中间体;微生物Microbiology;小分子抑制剂;All Inhibitors;Inhibitors;Intermediates Fine Chemicals;Non-nucleoside Reverse Transcriptase;Pharmaceuticals;Other APIs;小分子抑制剂，天然产物;有机原料;试剂;化工原料
沸点
637.4±65.0 °C(Predicted)
储存条件
Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
酸度系数(pKa)
1.23±0.10(Predicted)
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.
生物活性
Etravirine (TMC125, R-165335) 是一种非核苷类逆转录酶抑制剂(NNRTI)，用于治疗HIV。
靶点
Target Value
Reverse transcriptase
体外研究
Etravirine (TMC125)，对野生型HIV-1高度有效，EC50为1.4 nM到4.8 nM，对HIV-2也表现出一定的活性，EC50 为3.5 μM。TMC125也会抑制一系列HIV-1 M型亚基和循环重组形式以及O型病毒。
体内研究
Etravirine对抗性发展具有高的基因屏障。在IIb期试验，多次治疗的患者中，包括感染耐NNRTIs和耐蛋白酶抑制剂(PIs)病毒的患者，TMC125对现有NNRTIs耐药的HIV具有活性，与对照组具有相似的耐受性。
