维格列汀二水合物
| 中文名称 | 维格列汀二水合物 |
|---|---|
| 中文同义词 | 维格列汀二水合物;维达列汀二水合物;化合物 VILDAGLIPTIN DIHYDRATE |
| 英文名称 | Vildagliptin dihydrate |
| 英文同义词 | Vildagliptin dihydrate |
| CAS号 | 2133364-01-7 |
| 分子式 | C17H27N3O3 |
| 分子量 | 321.42 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 2133364-01-7.mol |
| 结构式 |  |
维格列汀二水合物 性质
| 储存条件 | Store at -20°C |
|---|---|
| 溶解度 | 溶于二甲基亚砜 |
Vildagliptin dihydrate (LAF237 dihydrate) 是一种有效且稳定的选择性二肽基肽酶IV (DPP-IV) 抑制剂，在人 Caco-2 细胞中抑制 DPP-IV 的 IC50 为 3.5 nM。Vildagliptin dihydrate 具有出色的口服生物利用度和有效的降血糖活性。
IC50: 3.5 nM (DPP-IV, in human Caco-2 cells)
Vildagliptin promotes beta cell survival by inhibiting cell apoptosis. Vildagliptin also promotes cell proliferation.
Vildagliptin (35 mg/kg; once daily by oral gavage) increases plasma active GLP-1 levels in islets of db/db mice.
Vildagliptin (10 µmol/kg; orally) significantly decreases glucose excursions and stimulate insulin secretion in obese male Zucker rats.
| Animal Model: | Male db/db mice (BKS) and wildtype mice |
| Dosage: | 35 mg/kg |
| Administration: | Oral gavage; once daily; for 6 weeks |
| Result: | Increased plasma active GLP-1 levels (22.63±1.19 vs. 11.69±0.44). |
| Animal Model: | Obese male Zucker rats |
| Dosage: | 10 µmol/kg (Pharmacokinetic Analysis) |
| Administration: | Orally |
| Result: | Significantly decreased glucose excursions and stimulate insulin secretion. |