A 769662 is a potent and reversible AMP-activated protein kinase (AMPK) allosteric activator with an EC50 of 0.8 µM, that displays selectivity towards beta1 subunit-containing heterotrimers, activating AMPK by binding to the beta and gamma subunits and not the AMP binding site. AMPK is a key cellular energy sensor and regulator of metabolic homeostasis and activation of AMPK provides beneficial outcomes in fighting against metabolic disorders such as insulin resistance and type 2 diabetes. In vivo, A 769662 inhibits fatty acid biosynthesis in rat hepatocytes and decreases plasma glucose and triglyceride levels. In ob/ob mice, A-769662 inhibits the rate of whole-body fatty acid oxidation, decreases body weight gain, reduces triglycerides and lowers glucose levels. A 769662 also inhibits proliferation of mesenchymal stem cells and impedes reprogramming of mouse embryonic fibroblasts to induced pluripotent stem cells (iPSCs).
