GKA50 is a potent glucokinase activator ( EC 50 =33 nM at 5 mM glucose). GKA50 stimulates insulin release from mouse islets of Langerhans. GKA50 is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca 2+ -dependent modulator of insulin secretion. GKA50 shows significant glucose lowering in high fat fed female rats.
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