MK-0941

Research use only, not for human use.

MK-0941 (MK0941) is a novel potent, orally active Glucokinase (GK) activator with EC50 of 0.240 and 0.065 uM in 2.5 and 10 mM glucose, respectively.

MK-0941 (MK0941) is a novel potent, orally active Glucokinase (GK) activator with EC50 of 0.240 and 0.065 uM in 2.5 and 10 mM glucose, respectively; increases insulin secretion by 17-fold and glucose uptake up to 18-fold, respectively, in isolated rat islets of Langerhans and hepatocytes at 10 uM; exhibits strong glucose-lowering activity in rodent models of type 2 diabetes and healthy dogs.Diabetes Phase 2 Discontinued.

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MK-0941 free base (3 or 10 mg/kg, sing oral dose) treatment reduced blood glucose significantly in db/db diabetic mouse. Animal Model:Male db/db and db/+ (lean) mice (9-10 weeks of age, weighing 43-45 g) .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.

MK0941

Cytoskeleton/Cell Adhesion Molecules

Glucokinase

Glucokinase

Metabolic Disease

Diabetes

752240-01-0

460.5

C21H24N4O6S

>98% (HPLC)

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CCS(=O)(=O)C1=NC=C(C=C1)OC2=CC(=CC(=C2)C(=O)NC3=NN(C=C3)C)OC(C)CO

3-[[6-(ethylsulfonyl)-3-pyridinyl]oxy]-5-[(1S)-2-hydroxy-1-methylethoxy]-N-(1-methyl-1H-pyrazol-3-yl)benzamide

(-20℃)

With Ice Pack

≥ 2 years