MK-0941

MK-0941 is a selective, orally active, and allosteric 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 activates hexokinase subtype IV. MK-0941 can increase insulin secretion and glucose uptake. MK-0941 can be studied in research for type 2 diabetes^[1][2]. IC50 & Target:EC50: 240 nM (Recombinant human glucokinase, 2.5 mM glucose), 65 nM (Recombinant human glucokinase, 10 mM glucose)^[1] In Vitro:MK-0941 (1 μM) decreases the enzyme’s S_0.5 for glucose from 6.9 to 1.4 mM^[1].
MK-0941 (0.1-10 μM, 1.5 h) increases insulin secretion of isolated hepatocytes, dependent on MK-0941 and glucose concentrations^[1].
MK-0941 (0.1-30 μM, 3 h) increases the phosphorylation by 18-fold with 30 μM concentration in hepatocytes^[1]. In Vivo:MK-0941 (1-30 mg/kg, p.o., single dose) significantly reduces the blood glucose dose-dependently in HFD mice model^[1].
MK-0941 (2-60 mg/kg, p.o., twice daily for 14 d) retains the glucose-lowering efficacy in HFD mice^[1].
MK-0941 (3-10 mg/kg, p.o., single dose) reduces blood glucose and increases total plasma cholesterol in the db/db diabetic HFD/STZ mice^[1].
MK-0941 (0.3-3 mg/kg, p.o., single dose) significantly reduces the plasma glucose concentration in healthy dogs dose-dependently^[1].