Saxagliptin (hydrochloride) (BMS-477118 hydrochloride) 是一种有效的、选择性的、可逆的、竞争性的和具有口服活性的二肽基肽酶-4 (DPP-4) (Ki \u003d 0.6-1.3 nM) 抑制剂。
| Cas No. | 709031-78-7 |
| 别名 | 沙克列汀中间体,BMS-477118 hydrochloride |
| Canonical SMILES | O=C(N1[C@H](C#N)C[C@H]2[C@@H]1C2)[C@H]([C@@]3(C[C@H](C4)C5)C[C@H]5C[C@@]4(O)C3)N.Cl |
| 分子式 | C18H25N3O2•HCl |
| 分子量 | 351.9 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 10 mg/ml,PBS (pH 7.2): 2 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | Saxagliptin is a potent inhibitor of dipeptidyl peptidase 4 (DPP-4; Ki = 0.6 nM). It inhibits DPP-4 ex vivo (ED50 = 0.12 μmol/kg) in plasma from normal fasted rats. Saxagliptin (0.3-3 mg/kg) reduces plasma glucose levels in Zuckerfa/fa diabetic rats in a dose-dependent manner. Oral administration at doses ranging from 1-10 μmol/kg increases plasma insulin levels and improves glucose clearance in ob/ob mice, a transgenic model of obesity. Saxagliptin induces systolic and diastolic dysfunction, reduces contractile force, and exacerbates ischemia-reperfusion injury-induced cardiac dysfunction in isolated guinea pig hearts. Formulations containing saxagliptin have been used for the treatment of type 2 diabetes. |
