AM 2394

AM-2394 is a structurally distinct glucokinase activator (GKA). AM-2394 activates glucokinase (GK) with an EC50 of 60 nM.

Signaling Pathways >> Metabolic Enzyme/Protease >> Glucokinase

Research Areas >> Metabolic Disease

EC50: 60 nM (glucokinase)[1]

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].

Mice[1] In order to determine the effect of AM-2394 in an animal model of type 2 diabetes, it was administered per os (PO) to male ob/ob mice 30 minutes prior to performing an oral glucose tolerance test (OGTT). Doses of 1, 3, 10, 30 mg/kg each reduced glucose excursion, with maximal efficacy seen at 3 mg/kg.

[1]. Dransfield PJ, et al. Novel Series of Potent Glucokinase Activators Leading to the Discovery of AM-2394. ACS Med Chem Lett. 2016 May 23;7(7):714-8.

Ro 28-1675 | Palmitelaidic acid | AMG-3969 | LY2608204 | PF 04991532 | PSN-GK1