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PSN-GK1

CAS No. : 745051-61-0

MCE 站：PSN-GK1

产品活性：PSN-GK1是有效的葡萄糖激酶 (glucokinase) 活化剂，EC₅₀ 值为0.13 μM。

研究领域：Metabolic Enzyme/Protease

作用靶点：Glucokinase

In Vivo: PSN-GK1 exhibits an excellent pharmacokinetic profile, with high oral bioavailability, in the rat. PSN-GK1 can markedly reduce blood glucose which accompanied by a trend toward increased pancreatic insulin release. Separately, the antihyperglycemic actions of PSN-GK1 have been shown to be a result of both pancreatic ａnd hepatic effects. In addition, PSN-GK1 engenders potent antihyperglycemic effects in diabetic rodents without causing hypoglycemia. At 5 mM glucose, PSN-GK1 activates glucokinase (4.3-fold, EC₅₀=130 nM), increases MIN6 insulin secretion (26-fold, EC₅₀=267 nM) ａnd 2-DG hepatocytic uptake (3-fold, EC₅₀=1 μM). In C57Bl/6 mice, PSN-GK1 reduces blood glucose at 1 ａnd 10 mg/kg (by mouth), but insulin is increased significantly at only the higher dose. In hyperinsulinaemic 10-mM glucose clamps, PSN-GK1 increases2-DG incorporation into liver glycogen sixfold, directly demonstrating liver effects.

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