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.

Size Price Stock Quantity  
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.
Targets
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 NVizV3NqTnWwY4Tpc44h[XO|YYm= NXXlVplrUW6qaXLpeIlwdiCxZjDoeY1idiCGUGC0JIV5eHKnc4Pl[EBqdiCFYXPvMVIh[2WubIOsJGtqRTBwMEC0JO69VQ>? MXOxO|A{PDF2OB?=
insect cells MXnGeY5kfGmxbjDhd5NigQ>? NYPvSZhRUW6qaXLpeIlwdiCxZjDoeY1idiC{ZXPvcYJqdmGwdDDIbZMufGGpZ3XkJGRRWDRiZYjwdoV{e2WmIHnuJIlve2WldDDj[YxteyxiSVO1NF0xNjB3NjFOwG0> NIW5N40zODdzOESyNC=>

... 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]

Protocol

Animal Research:[1]
+ Expand
  • 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:
Saline
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
Formula

C17H25N3O2

CAS No. 274901-16-5
Storage powder
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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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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DPP-4 Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID