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Indinavir sulfate

CAS No. : 157810-81-6

MCE 站：Indinavir sulfate

产品活性：Indinavir(MK-639; L735524)硫酸盐是HIV蛋白酶抑制剂，具有很好的口服生物相容性。Amprenavir 也是 SARS-CoV 3CL^pro 的抑制剂，IC₅₀ 为 1.71 μM。

研究领域：Anti-infection  |  Metabolic Enzyme/Protease

作用靶点：HIV  |  HIV Protease  |  SARS-CoV

In Vitro: 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 [1]. 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 [2].

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