For research use only.
CAS No. 274901-16-5
Vildagliptin (LAF-237) inhibits DPP−4 with IC50 of 2.3 nM.
Selleck's Vildagliptin (LAF-237) has been cited by 6 publications
Purity & Quality Control
Choose Selective DPP-4 Inhibitors
|Description||Vildagliptin (LAF-237) inhibits DPP−4 with IC50 of 2.3 nM.|
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. 
|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.  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. |
|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(Data is from Selleck tests instead of citations):
For best results, use promptly after mixing.
* 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.
In vivo Formulation Calculator (Clear solution)
|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
|Dosage||mg/kg||Average weight of animals||g||Dosing volume per animal||ul||Number of animals|
|Step 2: Enter the in vivo formulation ()|
|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take μL DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
1.Please make sure the liquid is clear before adding the next solvent.
2.Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04081857||Completed||Drug: HGP1810|Drug: HCP1704||Health Subjective||Hanmi Pharmaceutical Company Limited||June 3 2019||Phase 1|
|NCT04087525||Completed||Drug: HIP1701|Drug: HGP1809||Health Subjective||Hanmi Pharmaceutical Company Limited||October 23 2018||Phase 1|
|NCT03577184||Withdrawn||Drug: Metformin/Vildagliptin||Diabetes Mellitus Type 2||Clinision||July 2018||--|
|NCT02145611||Completed||Drug: Glibenclamide|Drug: Vildagliptin||Type 2 Diabetes Mellitus|Hypertension|Endothelial Dysfunction||Dr. José Fernando Vilela-Martin MD PhD|Novartis|Hospital de Base||July 2013||Phase 4|
|NCT01862263||Terminated||Drug: Vildagliptin|Drug: Insulin|Drug: Placebo||Type 2 Diabetes Mellitus||Novartis Pharmaceuticals|Novartis||May 2013||Phase 4|
|NCT01686932||Completed||Drug: Vildagliptin|Drug: Sitagliptin||Diabetes Mellitus Type 2||Novartis Pharmaceuticals|Novartis||November 2012||Phase 4|
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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