Vildagliptin

Research use only, not for human use.

Vildagliptin, previously identified as LAF237, is a new oral anti-hyperglycemic agent (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs.

Vildagliptin, previously identified as LAF237, is a new oral anti-hyperglycemic agent (anti-diabetic drug) of the new dipeptidyl peptidase-4 (DPP-4) inhibitor class of drugs. Vildagliptin inhibits the inactivation of GLP-1 and GIP by DPP-4, allowing GLP-1 and GIP to potentiate the secretion of insulin in the beta cells and suppress glucaon release by the alpha cells of the islets of Langerhans in the pancreas. It is currently in clinical trials in the U.S. and has been shown to reduce hyperglycemia in type 2 diabetes mellitus. While the drug is still not approved for use in the US, it was approved in Feb 2008 by European Medicines Agency for use within the EU and is listed on the Australian PBS with certain restrictions. (In Vitro):Vildagliptin promotes beta cell survival by inhibiting cell apoptosis. Vildagliptin also promotes cell proliferation.(In Vivo):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.

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.

LAF-237

Metabolic Enzyme/Protease

DPP

DPP-4

Metabolic Disease

——

274901-16-5

303.4

C17H25N3O2

>98% (HPLC)

Ethanol: 60 mg/mL (197.75 mM); Water: 60 mg/mL (197.75 mM); DMSO: 60 mg/mL (197.75 mM)

N#C[C@H]1N(C(CN[C@@]23C[C@@]4(O)C[C@](C3)([H])C[C@@](C4)([H])C2)=O)CCC1

(S)-1-(2-(((1s,3R,5R,7S)-3-hydroxyadamantan-1-yl)amino)acetyl)pyrrolidine-2-carbonitrile

(-20℃)

With Ice Pack

≥ 2 years