AM-2394

AM-2394 is a structurally distinct glucokinase activator (GKA). AM-2394 activates glucokinase (GK) with an EC₅₀ of 60 nM. IC50 & Target: EC50: 60 nM (glucokinase)^[1] In Vivo: AM-2394, a structurally distinct glucokinase activator that displays a robust reduction in plasma glucose during an oral glucose tolerance test (OGTT) in ob/ob mice at a dose of 3 mg/kg. AM-2394 increases the affinity of glucokinase (GK) for glucose by approximately 10-fold, exhibits moderate clearance and good oral bioavailability in multiple animal models, and lowers glucose excursion following an oral glucose tolerance test in an ob/ob mouse model of diabetes. AM-2394 exhibits good-to-moderate cross species plasma clearance, volume of distribution, and oral bioavailability, allowing for further evaluation in animal models^[1].