MK-0941 free base

MK-0941 free base is an orally active glucokinase activator, with EC50s of 240 and 65 nM for recombinant human glucokinase in the presence of 2.5 and 10 mM glucose, respectively. MK-0941 free base exhibits strong glucose-lowering activity and is a potential therapeutic agent for treatment of type 2 diabetes[1][2].

Signaling Pathways >> Metabolic Enzyme/Protease >> Glucokinase

Research Areas >> Metabolic Disease

Glucokinase[1][2].

MK-0941 free base (3 or 10 mg/kg, sing oral dose) treatment reduced blood glucose significantly in db/db diabetic mouse[1]. Animal Model: Male db/db and db/+ (lean) mice (9-10 weeks of age, weighing 43-45 g) [1]. Dosage: 3 or 10 mg/kg. Administration: Oral gavage, single dose. Result: Resulted in significant reduction in blood glucose. These two doses lowered blood glucose similarly at 1 h after dosing, suggesting that saturation of effect was approached.

[1]. Eiki J, et al. Pharmacokinetic and pharmacodynamic properties of the glucokinase activator MK-0941 in rodent models of type 2 diabetes and healthy dogs. Mol Pharmacol. 2011 Dec;80(6):1156-65.

[2]. Meininger GE, et al. Effects of MK-0941, a novel glucokinase activator, on glycemic control in insulin-treated patients with type 2 diabetes. Diabetes Care. 2011 Dec;34(12):2560-6.