AM-2394 is an effective and specific Glucokinase agonist (GKA, EC50: 60 nM), which catalyzes the phosphorylation of glucose to glucose-6-phosphate. AM-2394(AM2394) increases the affinity of 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.

GKA:60 nM(EC50)

AM-2394, a novel glucokinase activator, prominently reduces plasma glucose levels in ob/ob mice during an oral glucose tolerance test (OGTT) at a 3 mg/kg dosage. It enhances glucokinase's (GK) glucose affinity by roughly 10-fold, showing moderate clearance and favorable oral bioavailability across various animal models. Additionally, AM-2394 significantly improves glucose control following an OGTT in an ob/ob mouse model of diabetes. It demonstrates suitable cross-species plasma clearance, distribution volume, and oral bioavailability, supporting its potential for further investigation in animal studies[1].

Kinase screen: Briefly, all assays (25.5 μl at 21°C for 30 min) are performed using a Biomek 2000 Laboratory Automation Workstation in a 96-well format. Reactions contains 5–20 mU purified kinase along with substrate peptide or protein and are initiated by the addition of 10 mM MgAcetate and 5, 20, or 50 μM ATP ([γ-33P]-ATP, 800 cpm/pmol).