| Identification | Back Directory | [Name]
GS-9822 | [CAS]
2219362-41-9 | [Synonyms]
GS-9822
GS-9822;GS 9822;GS9822
6-Benzothiazoleacetic acid, 7-(4-chlorophenyl)-α-(1,1-dimethylethoxy)-5-methyl-2-[1-methyl-3-[1-(3-oxetanyl)-4-piperidinyl]-1H-indazol-5-yl]-, (αS)- | [Molecular Formula]
C36H39ClN4O4S | [MOL File]
2219362-41-9.mol | [Molecular Weight]
659.24 |
| Hazard Information | Back Directory | [Description]
GS-9822 is a novel LEDGIN, an inhibitor that targets the binding pocket of LEDGF/p75 which is a cellular cofactor that substantially contributes to HIV integration site selection, displaying a block-and-lock phenotype in cell culture. | [Uses]
GS-9822 is a potent antivira agent with nanomolar activity against wild-type HIV-1 viruses. GS-9822 potently inhibits the LEDGF/p75-integrase interaction with an IC50 of 0.07 μM. GS-9822 has high in vitro metabolic stability and favorable oral pharmacokinetic profiles with low systemic clearance in rats, dogs, and monkeys[1]. | [References]
[1] Bruggemans A, et al. GS-9822, a preclinical LEDGIN candidate, displays a block-and-lock phenotype in cell culture. Antimicrob Agents Chemother. 2023 May 1;65(5):e02328-20. DOI:10.1128/AAC.02328-20 |
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