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Indinavir sulfate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Indinavir sulfate图片
CAS NO:157810-81-6
规格:98%
分子量:711.87
包装与价格:
包装价格(元)
200mg电议
500mg电议
50mg电议
100mg电议

产品介绍
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。
CAS:157810-81-6
分子式:C36H49N5O8S
分子量:711.87
纯度:98%
存储:Store at -20°C

Background:

Indinavir sulfate(MK-639 sulfate; L735524 sulfate ) is a potent and specific HIV protease inhibitor that appears to have good oral bioavailability.Target: HIV ProteaseIndinavir(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].




[1]. Stein, D.S., et al., A 24-week open-label phase I/II evaluation of the HIV protease inhibitor MK-639 (indinavir). AIDS, 1996. 10(5): p. 485-92. [2]. Liu, F., et al., Kinetic, stability, and structural changes in high-resolution crystal structures of HIV-1 protease with drug-resistant mutations L24I, I50V, and G73S. J Mol Biol, 2005. 354(4): p. 789-800.