Vildagliptin (LAF-237)

Catalog No.S3033

Vildagliptin (LAF-237) Chemical Structure

Molecular Weight(MW): 303.4

Vildagliptin (LAF-237) inhibits DPP−4 with IC50 of 2.3 nM.

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In DMSO USD 200 In stock
USD 150 In stock
USD 270 In stock
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Biological Activity

Description Vildagliptin (LAF-237) inhibits DPP−4 with IC50 of 2.3 nM.
DPP-4 [1]
(Cell-free assay)
2.3 nM
In vitro

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. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Caco-2 cells M3PwbGZ2dmO2aX;uJIF{e2G7 NHzwbnRKdmirYnn0bY9vKG:oIHj1cYFvKESSUESg[ZhxemW|c3XkJIlvKEOjY3:tNkBk\WyuczygT4k:OC5yMESg{txO MnTpNVcxOzRzNEi=
insect cells M3jXPWZ2dmO2aX;uJIF{e2G7 MV3Jcohq[mm2aX;uJI9nKGi3bXHuJJJm[2:vYnnuZY51KEircz30ZYdo\WRiRGDQOEBmgHC{ZYPz[YQhcW5iaX7z[YN1KGOnbHzzMEBKSzVyPUCuNFU3KM7:TR?= Mmq4NlA4OTh2MkC=

... Click to View More Cell Line Experimental Data

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. [1] 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. [2] 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. [3]


Animal Research:[1]
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  • Animal Models: Obese male Zucker rats
  • Formulation: 0.5% carboxymethylcellulose (CMC) and 0.2% Tween 80
  • Dosages: 10 μmol/kg
  • Administration: Orally administrated at a single dose
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 60 mg/mL (197.75 mM)
Water 60 mg/mL (197.75 mM)
Ethanol 60 mg/mL (197.75 mM)
In vivo Add solvents to the product individually and in order:
For best results, use promptly after mixing.
30 mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 303.4


CAS No. 274901-16-5
Storage powder
in solvent
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02849899 Not yet recruiting Disorder Related to Renal Transplantation|Diabetes Centre Hospitalier Universitaire de Besancon|University Hospital, Tours|University Hospital, Lille|Recherche Clinique Paris Descartes Necker Cochin Sainte Anne|Amiens University Hospital|University Hospital, Brest|Rennes University Hospital|Tenon Hospital, Paris|Centre Hospitalier Universitaire de Nice|University Hospital, Strasbourg, France January 2017 Phase 3
NCT02803892 Recruiting Diabetes Mellitus, Type 1 Piemonti Lorenzo|Fondazione Italiana Diabete Onlus|Ospedale San Raffaele May 2016 Phase 2
NCT02999841 Recruiting Diabetes Mellitus, Type 2|Obesity Peking University March 2016 Phase 4
NCT02475070 Recruiting Type 2 Diabetes Lund University January 2016 Phase 4
NCT02832999 Recruiting Type 2 Diabetes Mellitus Yaounde Central Hospital|University of Yaounde 1|University of Buea January 2016 Phase 4
NCT02343926 Completed Type 2 Diabetes Mellitus Sanofi December 2014 Phase 3

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DPP-4 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID