Integrase-LEDGF/p75 allosteric inhibitor 1

Modify Date: 2024-01-12 10:29:07

Integrase-LEDGF/p75 allosteric inhibitor 1 Structure
Integrase-LEDGF/p75 allosteric inhibitor 1 structure
Common Name Integrase-LEDGF/p75 allosteric inhibitor 1
CAS Number 1431738-14-5 Molecular Weight 579.75
Density N/A Boiling Point N/A
Molecular Formula C33H41NO6S Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Integrase-LEDGF/p75 allosteric inhibitor 1


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].

 Names

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
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