SB-756050

TGR5激动剂（人类受体的EC50=1.3μM）；对TGR5相较于FXR以及其他一系列受体、通道和转运蛋白具有选择性；在糖尿病Goto Kakizaki大鼠中，剂量为10-100mg/kg时，可降低空腹血糖水平，增加葡萄糖处置率和胰岛素分泌。A TGR5 agonist (EC50 = 1.3 μM for the human receptor); selective for TGR5 over FXR and panel of other receptors, channels, and transporters; decreases fasting glucose levels and increases glucose disposal rate and insulin secretion in diabetic Goto Kakizaki rats from 10-100 mg/kg.