gka-50

GKA50 stimulates insulin release from mouse islets of Langerhans and MIN6 cells. GKA50 shows significant glucose lowering in high fat fed female rats. GKA50 is a potent glucokinase activator (EC50=33 nM at 5 mM glucose).

GKA50 quarterhydrate is a potent glucokinase activator with an EC50 value of 33 nM. This glucose-like activator of β-cell metabolism in rodent and human pancreatic islets is a Ca2+-dependent regulator of insulin secretion. It stimulates insulin secretion in mouse islets and significantly reduces blood glucose in high-fat-fed female rats.