Vildagliptin

SKU: orb1308423

Description

Vildagliptin

Research Area

Cell Biology, Neuroscience

Key Properties

• CAS Number: 274901-16-5
• MW: 303.40
• Purity: >98%
• Formula: C₁₇H₂₅N₃O₂
• SMILES: OC12CC3CC(C1)CC(C3)(C2)NCC(=O)N1CCCC1C#N
• Target: Protease
• Solubility: Soluble in DMSO (up to 45 mg/ml), in DMF (up to 20 mg/ml), or in Ethanol (up to 20 mg/ml).

Bioactivity

• Target IC50:
  DPP4:2.3 nM
• In Vivo:
  As the most stable DPP-4 inhibitor, Vildagliptin binds to the DPP-4 S1 and S2 catalytic sites, mimicking the transition state of the P-1 site.
• In Vitro:
  In obese male Zucker rats, oral administration of Vildagliptin (10 μmol/kg, p.o.) during a glucose tolerance test increases GLP-1 levels, additionally stimulates insulin secretion, and significantly reduces fluctuations in blood glucose levels. In cynomolgus monkeys treated with Vildagliptin (1 μmol/kg, p.o.), plasma DPP-IV activity is maximally inhibited (95%) approximately 2 hours post-treatment, with inhibition >50% occurring within 30 minutes and lasting over 10 hours. In adult male Sprague-Dawley rats induced with diabetes by Streptozotocin, Vildagliptin treatment of 10 mg/kg for 32 weeks prevents nerve fiber loss. At a dosage of 60 mg/kg, Vildagliptin enhances β-cell replication and decreases apoptosis, leading to an increase in pancreatic β-cell mass, which remains elevated for 12 days post withdrawal of Vildagliptin.
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Storage & Handling

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

Alternative Names

LAF237

Compound Identifiers

PubChem CID

5251896