Mitiglinide (calcium salt)

SUR1/Kir6.2抑制剂(IC50=4nM)；对SUR1/Kir6.2具有选择性，优于SUR2A/Kir6.2和SUR2B/Kir6.2通道（IC50s分别为3µM和5µM）；在100µM时诱导HIT-T15胰岛素瘤细胞和分离的小鼠胰岛中的胰岛素释放；在STZ诱发的糖尿病大鼠模型中，增加餐后血浆胰岛素水平并抑制餐后血浆葡萄糖水平的升高。A SUR1/Kir6.2 inhibitor (IC50 = 4 nM); selective for SUR1/Kir6.2 over SUR2A/Kir6.2 and SUR2B/Kir6.2 channels (IC50s = 3 and 5 µM, respectively); induces insulin release in HIT-T15 insulinoma cells and isolated mouse pancreatic islets at 100 µM; increases postprandial plasma insulin levels and inhibits postprandial increases in plasma glucose levels in an STZ-induced rat model of diabetes.分子式C19H24NO3 • 1/2Ca分子量334.4O=C(C[C@H](CC1=CC=CC=C1)C([O-])=O)N2C[C@@]3([H])CCCC[C@@]3([H])C2.O=C(C[C@H](CC4=CC=CC=C4)C([O-])=O)N5C[C@@]6([H])CCCC[C@@]6([H])C5.[Ca+2]