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    Vildagliptin (LAF-237)
    Vildagliptin (LAF-237)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0743
    CAS #: 274901-16-5; Purity ≥98%

    Description: Vildagliptin (also known as LAF-237; trade name: Zomelis) is an potent and orally bioavailable anti-diabetic drug that acts as an inhibitor of DPP-4 (dipeptidyl peptidase 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 as an anti-hyperglycemic agent.

    References: J Med Chem. 2003 Jun 19;46(13):2774-89; Eur J Pharmacol. 2011 Jan 15;650(2-3):703-7. 

    Related CAS: 2133364-01-7 (Vildagliptin dihydrate)

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    Molecular Weight (MW)303.4
    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: N/A
    Ethanol: 60 mg/mL (197.8 mM)
    Solubility (In vivo)Saline: 30 mg/mL
    SynonymsLAF237; LAF-237; LAF 237; DSP 7238; DSP-7238; DSP7238; NVP-LAF 237; NVP LAF 237; NVP LAF-237; trade name: Zomelis 

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


    InChi Code: InChI=1S/C17H25N3O2/c18-9-14-2-1-3-20(14)15(21)10-19-16-5-12-4-13(6-16)8-17(22,7-12)11-16/h12-14,19,22H,1-8,10-11H2/t12-,13+,14-,16-,17-/m0/s1

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

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    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: Vildagliptin (LAF-237; NVP-LAF 237) inhibits DPP-4 with IC50 of 2.3 nM. Vildagliptin is an N-substituted glycyl-2-cyanopyrrolidine (figure 2). It is a potent competitive and reversible inhibitor of human and rodent DPP-4 in vitro, with a median inhibitory concentration (IC50) ~2-3 nmol/L. Importantly, vildagliptin inhibits DPP-4 with high specificity relative to other similar peptidases where its IC50 exceeds 200 mol/L.

    In VivoVildagliptin(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 modelObese male Zucker rats
    Formulation & DosageDissolved in 0.5% carboxymethylcellulose (CMC) and 0.2% Tween 80; 10 μmol/kg; p.o. administration
    ReferencesJ Med Chem. 2003 Jun 19;46(13):2774-89; Eur J Pharmacol. 2011 Jan 15;650(2-3):703-7. 

    These protocols are for reference only. InvivoChem does not independently validate these methods.

     Vildagliptin (LAF-237) 
    Histological and morphometric analysis of pancreatic islets from neonatal rats ...
    Eur J Pharmacol. 2011 Jan 15;650(2-3):703-7.


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