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。

Vildagliptin dihydrate (LAF237 dihydrate) is a potent, stable, selective dipeptidyl peptidase IV ( DPP-IV ) inhibitor with an IC 50 of 3.5 nM in human Caco-2 cells. Vildagliptin dihydrate possesses excellent oral bioavailability and potent antihyperglycemic activity [1].

Vildagliptin promotes beta cell survival by inhibiting cell apoptosis. Vildagliptin also promotes cell proliferation [2].

Vildagliptin (35 mg/kg; once daily by oral gavage) increases plasma active GLP-1 levels in islets of db/db mice [2]. Vildagliptin (10 μmol/kg; orally) significantly decreases glucose excursions and stimulate insulin secretion in obese male Zucker rats [1]. Animal Model: Male db/db mice (BKS) and wildtype mice [2] 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 [1] Dosage: 10 μmol/kg (Pharmacokinetic Analysis) Administration: Orally Result: Significantly decreased glucose excursions and stimulate insulin secretion.

2133364-01-7

C17H29N3O4

339.43

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years