Product Data Sheet

GSK3739936

Catalog No. A51384

main product photo
GSK3739936 is a potent allosteric inhibitor of HIV-1 integrase, exhibiting an IC50 value of 11.1 nM and an EC50 of 1.7 nM. In addition to its inhibitory effects, GSK3739936 demonstrates weak inhibition of cytochrome P450 enzymes (IC50 > 24.3 μM). This compound also showcases favorable pharmacokinetic properties in preclinical models, characterized by rapid absorption, low to moderate clearance rates, and excellent oral bioavailability, making it a promising candidate for further research in HIV therapeutics.
Chemical Information
Catalog NumA51384
M. Wt562.71
FormulaC34H43FN2O4
Purity>98%
Storageat -20 °C 3 years (powder form); at -20 °C 6 months (Solution base)
CAS No.1803444-21-4
SynonymsBMS-986180
SMILESCC1=NC(C)=C(C(N2CCC(C)(CC2)C)=C1[C@@H](C(O)=O)OC(C)(C)C)C3=CC=C(C=C3)OCCC4=CC=C(C=C4)F
Biological Activity
DescriptionGSK3739936 is a potent allosteric inhibitor of HIV-1 integrase, exhibiting an IC50 value of 11.1 nM and an EC50 of 1.7 nM. In addition to its inhibitory effects, GSK3739936 demonstrates weak inhibition of cytochrome P450 enzymes (IC50 > 24.3 μM). This compound also showcases favorable pharmacokinetic properties in preclinical models, characterized by rapid absorption, low to moderate clearance rates, and excellent oral bioavailability, making it a promising candidate for further research in HIV therapeutics.
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