Repaglinide 是一种能够用于2 型糖尿病的胰岛素促分泌剂。

Repaglinide is a benzoic acid derivative that stimulates insulin secretion from the pancreas and is used in the therapy of type 2 diabetes. Repaglinide has been linked to rare instances of clinically apparent acute liver injury.

在喂食和饥饿的正常大鼠中,Repaglinide比给予降血糖磺脲类药物后更大更快速地增加血浆胰岛素浓度和较早地下降血糖.

Repaglinide以钙依赖方式结合NCS蛋白质,但不与CAM或S100蛋白结合。Repaglinide以钙依赖方式紧密结合CCaMK和PpCaMK,拮抗结构域的调节功能,对CCaMK和PpCaMK域的IC 50值为55 mM和4 mM。Repaglinide以低亲和力（K（D）= 59 nM）结合单独的SUR1,但以高亲和力结合SUR1与Kir6.2共表达,增加了大约150倍。Repaglinide在视紫红质激酶测定中,拮抗恢复蛋白的抑制作用,IC50值为400 mM。

135062-02-1

C27H36N2O4

452.59

瑞格列奈;AG-EE 623ZW;AG-EE 388 ZW

Ethanol:84 mg/mL (185.6 mM)
DMSO:84 mg/mL (185.6 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years