TM-N1324

GPR39激动剂；浓度为1µM时，对165个GPCR（包括GHS-R和胃动素受体）中的GPR39具有选择性；在表达人类GPR39的HEK293细胞中诱导肌醇磷酸积累（在有和没有锌的情况下，EC50s分别为2和201nM）并在表达人类GPR39的COS-7细胞中诱导cAMP积累（在有锌的情况下，EC50=17nM）；在1µM时减少小鼠胃粘膜分离细胞中的生长素释放肽分泌并增加生长抑素分泌；在高脂饮食引起的肥胖小鼠模型中，减少黑暗期的食物摄入量和体重。A GPR39 agonist; selective for GPR39 over a panel of 165 GPCRs, including GHS-R and the motilin receptor, at 1 µM; induces inositol phosphate accumulation in HEK293 cells expressing human GPR39 (EC50s = 2 and 201 nM in the presence and absence of zinc, respectively) and cAMP accumulation in COS-7 cells expressing human GPR39 (EC50 = 17 nM in the presence of zinc); decreases ghrelin secretion and increases somatostatin secretion in isolated mouse gastric mucosa cells at 1 µM; decreases food intake during the dark period and body weight in a mouse model of high-fat diet-induced obesity.分子式C18H13ClFN7O分子量397.8O=C1NC2=C(C(C1)C3=CC=C(C=C3Cl)F)C(C)=NN2C4=NC=NC5=C4NC=N5