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编 号:F272301
分子式:C17H29N3O4
分子量:339.43
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Vildagliptin dihydrate (LAF237 dihydrate) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin dihydrate possesses excellent oral bioavailability and potent antihyperglycemic activity.

体内研究:
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.

体外研究:
Vildagliptin promotes beta cell survival by inhibiting cell apoptosis. Vildagliptin also promotes cell proliferation.
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