A-769662

A-769662 is a **potent, reversible, direct activator of AMP-activated protein kinase (AMPK)**, specifically binding to heterotrimers containing the β1 regulatory subunit. Unlike indirect AMPK activators such as metformin and AICAR, A-769662 binds at a site distinct from AMP, allosterically activating AMPK and inhibiting its dephosphorylation. It acts via the carbohydrate-binding module of the β subunit and the kinase domain interface, promoting phosphorylation of downstream AMPK targets, notably acetyl-CoA carboxylase (ACC). This leads to metabolic effects such as inhibition of fatty acid synthesis and anti-inflammatory effects in rodent models of endotoxemia and inflammatory arthritis[1][3][4][5][6][7]. Developed as a **synthetic research tool**, it has demonstrated efficacy in vitro and in preclinical animal models but is not intended for therapeutic or diagnostic human use.

Other names

A 769662A769662A-769662thienopyridone derivative