GKA50 (1-30 mg/kg; p.o.) gives significant glucose lowering in an oral glucose tolerance test. Animal Model: High-fat-fed obese female Zucker (fa/fa) rats Dosage: 1, 3, 10, 30 mg/kg Administration: Oral administration Result: Significant percentage glucose lowering.

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 glucokinase enzymatic activity with an EC 50 of 0.022 μM. GKA50 stimulates insulin secretion in the pancreatic insulinoma cell line, INS-1, with an EC 50 of 0.065 μM. GKA50 reduces chronic-high-glucose-induced apoptosis via modulation of glucokinase and apoptotic protein BAD. Cell Proliferation Assay Cell Line: INS-1 cells (starved overnight with 3 μM glucose) Concentration: 0.01-100 μM Incubation Time: 24 hours Result: Stimulated cell proliferation in a dose-dependent manner, with EC 50 values ranging from 1 to 2 μM.

GKA50 是一种有效的葡萄糖激酶 (glucokinase) 激活剂 (EC50=33 nM)。GKA50 刺激小鼠胰岛和 MIN6 细胞分泌胰岛素。GKA50 对高脂高脂脂肪雌性大鼠有显著的降糖作用。