茚地那韦

  • 化学数据
CAS号 150378-17-9 货号 BCP05711
中文名 茚地那韦
英文名 Indinavir
中文别名 吲地那韦;吲地纳韦;
英文别名 Crixivan;MK-639;L-735524;MK639;L735524;MK 639;L 735524;L 735 524;
分子式 C36H47N5O4 分子量 613.36
  • 用途
生物活性 Indinavir(MK-639) is a protease inhibitor used as a component of highly active antiretroviral therapy (HAART) to treat HIV infection and AIDS.MK-639 appears to have significant dose-related antiviral activity and is well tolerated. Inhibition constants (K(i)) of the antiviral drug indinavir for the reaction catalyzed by the mutant enzymes were about threefold and 50-fold higher for PR(L24I) and PR(I50V), respectively, relative to PR and PR(G73S). The dimer dissociation constant (K(d)) was estimated to be approximately 20 nM for both PR(L24I) and PR(I50V), and below 5 nM for PR(G73S) and PR. Crystal structures of the mutants PR(L24I), PR(I50V) and PR(G73S) were determined in complexes with indinavir, or the p2/NC substrate analog at resolutions of 1.10-1.50 Angstrom .
信号通路 Protease/Metabolic Enzyme Microbiology/Virology 
靶 点 HIV Protease HIV 

结构式

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