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MK-0941 is a glucokinase activator with EC50 values of 0.24 and 0.065 μM at low (2.5 mM) and high (10 mM) concentrations of glucose, respectively. It increases insulin secretion from isolated rat islets of Langerhans and glucose uptake by hepatocytes in vitro. MK-0941 reduces blood glucose levels in high-fat diet-fed db/db mice and in high-fat diet-fed mice with diabetes induced by streptozotocin .

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