GKA50

851884-87-2

464.51

10 mM in DMSO

Metabolic Enzyme/Protease

GKA50 is a potent glucokinase activator (EC₅₀=33 nM at 5 mM glucose). GKA50 stimulates insulin release from mouse islets of Langerhans and MIN6 cells. GKA50 shows significant glucose lowering in high fat fed female rats^[1][2]. In Vitro: GKA50 (0.01-100 uM; 24 hours) enhances INS-1 cell proliferation with EC₅₀values ranging from 1 to 2 uM^[2].
GKA50 (1.2 uM+40 uM 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 uM. GKA50 stimulates insulin secretion in the pancreatic insulinoma cell line, INS-1, with an EC₅₀ of 0.065 uM. 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].