1431738-14-5

1431738-14-5 structure
1431738-14-5 structure
  • Name: Integrase-LEDGF/p75 allosteric inhibitor 1
  • Chemical Name: Integrase-LEDGF/p75 allosteric inhibitor 1
  • CAS Number: 1431738-14-5
  • Molecular Formula: C33H41NO6S
  • Molecular Weight: 579.75
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease HIV Integrase
  • Create Date: 2022-06-27 19:59:48
  • Modify Date: 2024-01-12 10:29:07
  • 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].

Name Integrase-LEDGF/p75 allosteric inhibitor 1
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
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.

Molecular Formula C33H41NO6S
Molecular Weight 579.75