Indinavir sulfate

  • Chemical Properties
CAS No. 157810-81-6 Cat. No. BCP13525
Name Indinavir sulfate
Synonyms Crixivan sulfate;MK-639 sulfate;L-735524 sulfate;MK639 sulfate;L735524 sulfate;MK 639 sulfate;L 735524 sulfate;
Formula C36H49N5O8S M. Wt 711.87
  • Biological Activity
Description 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.
Pathways Protease/Metabolic Enzyme 
Targets HIV Protease 

Structure

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