product name Vildagliptin (LAF-237)
Description: Vildagliptin, also known as LAF237, is an potent and orally available inhibitor of DPP-4 with IC50 of 2.3 nM. 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 glucagon release by the alpha cells of the islets of Langerhans in the pancreas. Vildagliptin has been shown to reduce hyperglycemia in type 2 diabetes mellitus. Vildagliptin was approved in Feb 2008 by in EU.
References: J Med Chem. 2003 Jun 19;46(13):2774-89; Eur J Pharmacol. 2011 Jan 15;650(2-3):703-7.
303.4
Formula
C17H25N3O2
CAS No.
274901-16-5
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 60 mg/mL (197.8 mM)
Water:
Ethanol: 60 mg/mL (197.8 mM)
Solubility (In vivo)
Saline: 30 mg/mL
Synonyms
LAF237
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19414842
| In Vitro |
In vitro activity: Vildagliptin is the most stable DPP-IV inhibitor, binding in the S1- and S2-catalytic sites of DPP-IV, possessing a P-1 site transition-state mimetic. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Vildagliptin(orally dosed with 10 μmol/kg) is a potent, orally active inhibitor of plasma DPP-IV activity that provides increased levels of GLP-1 in an oral glucose tolerance test (OGTT) with Obese male Zucker rats. Vildagliptin orally dosed with 10 μmol/kg both significantly decreases glucose excursions and stimulates insulin secretion in Obese male Zucker rats. Maximum inhibition of plasma DPP-IV activity (95%) is observed approximately 2 hours postdose of Vildagliptin (1 μmol/kg, po) while >50% inhibition of DPP-IV is observed within 30 min postdose and persisted for >10 hours in normal Cynomolgus monkeys. Vildagliptin(60 mg/kg) increases pancreatic beta cell mass through enhanced beta cell replication and reduced apoptosis, and the increased beta cell mass is sustained for 12 days after vildagliptin washout. Vildagliptin administrated at doses of 10 mg/kg for 32 weeks protects nerve fiber loss in streptozotocin (STZ)-induced diabetic adult male Sprague Dawley rats. |
| Animal model | Obese male Zucker rats |
| Formulation & Dosage | Dissolved in 0.5% carboxymethylcellulose (CMC) and 0.2% Tween 80; 10 μmol/kg; p.o. administration |
| References | J Med Chem. 2003 Jun 19;46(13):2774-89; Eur J Pharmacol. 2011 Jan 15;650(2-3):703-7. |
