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GKA50 quarterhydrate is a potent glucokinase activator ( EC 50 =33 nM at 5 mM glucose) and stimulates insulin release from mouse islets of Langerhans. GKA50 quarterhydrate is a glucose-like activator of beta-cell metabolism in rodent and human islets and
Appearance:Solid
In Vitro:GKA50 (0.01-100 μM; 24 hours) enhances INS-1 cell proliferation with EC 50 values ranging from 1 to 2 μM. GKA50 (1.2 μM+40 μM glucose; 2-4 days) treatment reduces apoptosis induced by chronic high glucose in INS-1 cells. GKA50 activates human gl
In Vivo:GKA50 (1-30mg/kg; p.o.) gives significant glucose lowering in an oral glucose tolerance test. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: High-fat-fed obese female Zucker (fa/fa) rats
Biological Activity:GKA50 quarterhydrate is a potent glucokinase activator ( EC 50 =33 nM at 5 mM glucose) and stimulates insulin release from mouse islets of Langerhans. GKA50 quarterhydrate is a glucose-like activator of beta-cell metabolism in rodent and human islets and