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PSN-GK1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
PSN-GK1图片
CAS NO:745051-61-0
规格:98%
分子量:438.54
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议
20mg电议

产品介绍
PSN-GK1是有效的葡萄糖激酶(glucokinase)活化剂,EC50值为0.13μM。
CAS:745051-61-0
分子式:C20H23FN2O4S2
分子量:438.54
纯度:98%
存储:Store at -20°C

Background:

PSN-GK1 is a potent glucokinase activator with an EC50 of 0.13 μM.



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[1]. 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[2].


[1]. Bertram LS, et al. SAR, pharmacokinetics, safety, and efficacy of glucokinase activating 2-(4-sulfonylphenyl)-N-thiazol-2-ylacetamides: discovery of PSN-GK1. J Med Chem. 2008 Jul 24;51(14):4340-5. [2]. Fyfe MC, et al. Glucokinase activator PSN-GK1 displays enhanced antihyperglycaemic and insulinotropic actions. Diabetologia. 2007 Jun;50(6):1277-87.