Integrase-LEDGF/p75 allosteric inhibitor 1

Names

[ CAS No. ]:
1431738-14-5

[ Name ]:
Integrase-LEDGF/p75 allosteric inhibitor 1

Biological Activity

[Description]:

Integrase-LEDGF/p75 allosteric inhibitor 1 (Compound 31h) is an orally active integrase-LEDGF/p75 (IN-LEDGF/p75) allosteric inhibitor. Integrase-LEDGF/p75 allosteric inhibitor 1 inhibits HIV-1 DNA integration and shows antiviral activity with an EC50 of 3.9 nM against HIV-1 recombinant molecular clone NL432[1].

[Related Catalog]:

Research Areas >> Infection
Signaling Pathways >> Metabolic Enzyme/Protease >> HIV Integrase

[Target]

EC50: 3.9 nM (NL432)[1]


[In Vivo]

Integrase-LEDGF/p75 allosteric inhibitor 1 (Compound 31h) has moderate metabolic stability (HLM MS = 59%, RLM MS = 61%), exhibits good clearance (CLt = 6.99 mL/min/kg) and good bioavailability (F = 36%) in rats[1].

[References]

[1]. Sugiyama S, et al. Discovery of novel integrase-LEDGF/p75 allosteric inhibitors based on a benzene scaffold. Bioorg Med Chem. 2020 Sep 1;28(17):115643.

Chemical & Physical Properties

[ Molecular Formula ]:
C33H41NO6S

[ Molecular Weight ]:
579.75

Related Compounds