Vildagliptin

SKU: orb1225450

Description

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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 274901-16-5
• MW: 303.4
• Purity: >98% (HPLC)
• Formula: C₁₇H₂₅N₃O₂
• SMILES: N#C[C@H]1N(C(CN[C@@]23C[C@@]4(O)C[C@](C3)([H])C[C@@](C4)([H])C2)=O)CCC1
• Target: DPP
• Solubility: Ethanol: 60 mg/mL (197.75 mM); Water: 60 mg/mL (197.75 mM); DMSO: 60 mg/mL (197.75 mM)

Bioactivity

• 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. 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.
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• In Vitro:
  Vildagliptin promotes beta cell survival by inhibiting cell apoptosis. Vildagliptin also promotes cell proliferation.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

LAF-237

Quick Database Links

Gene Symbol

DPP