Gemigliptin (tartrate)

DPP-4抑制剂(IC50=0.01µM)；对DPP-4的选择性优于DPP-8、DPP-9和FAP-α（IC50s分别为277.28、233.72、418.43µM）；抑制分离的人血浆中的DPP-4活性(IC50=11.5nM)；体外清除甲基乙二醛并抑制BSA和甲基乙二醛之间的AGE形成以及AGE-BSA与大鼠尾腱胶原的交联（IC50s分别为1.15、11.69和1.39mM）；在100mg/kg剂量下降低db/db糖尿病小鼠的循环AGE水平和红细胞IgG含量；降低血糖和糖化血红蛋白水平，减少STZ和高脂饮食诱发的糖尿病小鼠模型中的胰腺β细胞损伤；诱导SW1736和TPC-1细胞的细胞毒性。A DPP-4 inhibitor (IC50 = 0.01 µM); selective for DPP-4 over DPP-8, DPP-9, and FAP- α (IC50s = 277.28, 233.72, 418.43 µM, respectively); inhibits DPP-4 activity in isolated human plasma (IC50 = 11.5 nM); scavenges methylglyoxal in vitro and inhibits AGE formation between BSA and methylglyoxal and cross-linking of AGE-BSA with rat tail tendon collagen (IC50s = 1.15, 11.69, and 1.39 mM, respectively); reduces the levels of circulating AGE and red blood cell IgG content in db/db diabetic mice at 100 mg/kg; decreases blood glucose and HbA1c levels and reduces pancreatic β-cell damage in a mouse model of STZ- and high-fat diet-induced diabetes; induces cytotoxicity in SW1736 and TPC-1 cells.分子式C18H19F8N5O2 • XC4H6O6分子量489.4FC(F)(C1=C2C(CN(CC2)C(C[C@H](N)CN3CC(F)(CCC3=O)F)=O)=NC(C(F)(F)F)=N1)F.OC([C@H](O)[C@@H](O)C(O)=O)=O