2133364-01-7
中文名稱
2133364-01-7
英文名稱
Vildagliptin dihydrate
CAS
2133364-01-7
分子式
C17H27N3O3
分子量
321.42
MOL 文件
2133364-01-7.mol
2133364-01-7 結(jié)構(gòu)式
常見(jiàn)問(wèn)題列表
生物活性
Vildagliptin dihydrate (LAF237 dihydrate) 是一種有效且穩(wěn)定的選擇性二肽基肽酶IV (DPP-IV) 抑制劑，在人 Caco-2 細(xì)胞中抑制 DPP-IV 的 IC50 為 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。靶點(diǎn)
IC50: 3.5 nM (DPP-IV, in human Caco-2 cells)
體外研究
Vildagliptin promotes beta cell survival by inhibiting cell apoptosis. Vildagliptin also promotes cell proliferation.
體內(nèi)研究
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. |