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是一种结构独特的葡萄糖激酶激活剂，在ob/ob小鼠进行口服葡萄糖耐量测试（OGTT）时，以3 mg/kg的剂量显著降低血浆葡萄糖水平。AM-2394使葡萄糖激酶（GK）对葡萄糖的亲和力提高了大约10倍，并在多种动物模型中表现出适中的清除率和良好的口服生物利用度，降低了ob/ob小鼠糖尿病模型在口服葡萄糖耐量测试后的葡萄糖波动。AM-2394在跨物种血浆清除率、分布体积和口服生物利用度方面展现出良好到适中的效果，允许在动物模型中进一步评估[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).