GKA50

GKA50 is a potent glucokinase activator (EC₅₀=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 Ca²⁺-dependent modulator of insulin secretion. GKA50 shows significant glucose lowering in high fat fed female rats^[1][2][3][4]. In Vitro: GKA50 (0.01-100 μM; 24 hours) enhances INS-1 cell proliferation with EC₅₀values ranging from 1 to 2 μM^[2].
GKA50 (1.2 μM+40 μM glucose; 2-4 days) treatment reduces apoptosis induced by chronic high glucose in INS-1 cells^[2].
GKA50 activates human glucokinase enzymatic activity with an EC₅₀ of 0.022 μM. GKA50 stimulates insulin secretion in the pancreatic insulinoma cell line, INS-1, with an EC₅₀ of 0.065 μM. GKA50 reduces chronic-high-glucose-induced apoptosis via modulation of glucokinase and apoptotic protein BAD^[2]. In Vivo: GKA50 (1-30 mg/kg; p.o.) gives significant glucose lowering in an oral glucose tolerance test^[1].