硫酸茚地那韦
| CAS号 | 157810-81-6 | 货号 | BCP13525 |
| 中文名 | 硫酸茚地那韦 | ||
| 英文名 | Indinavir sulfate | ||
| 中文别名 | |||
| 英文别名 | Crixivan sulfate;MK-639 sulfate;L-735524 sulfate;MK639 sulfate;L735524 sulfate;MK 639 sulfate;L 735524 sulfate; | ||
| 分子式 | C36H49N5O8S | 分子量 | 711.87 |
| 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 | ||
| 靶 点 | HIV Protease | ||
结构式
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