Vildagliptin (LAF-237)

Catalog No.S3033

For research use only.

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

Vildagliptin (LAF-237) Chemical Structure

CAS No. 274901-16-5

Selleck's Vildagliptin (LAF-237) has been cited by 7 Publications

Purity & Quality Control

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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 MVfGeY5kfGmxbjDhd5NigQ>? NIf5eFhKdmirYnn0bY9vKG:oIHj1cYFvKESSUESg[ZhxemW|c3XkJIlvKEOjY3:tNkBk\WyuczygT4k:OC5yMESg{txO Mn7KNVcxOzRzNEi=
insect cells NWHqS5E3TnWwY4Tpc44h[XO|YYm= MnLaTY5pcWKrdHnvckBw\iCqdX3hckBz\WOxbXLpcoFvfCCKaYOteIFo\2WmIFTQVFQh\XiycnXzd4VlKGmwIHnud4VkfCClZXzsd{whUUN3ME2wMlA2PiEQvF2= MkK3NlA4OTh2MkC=
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 (from reference)

Animal Research:[1]
  • Animal Models: Obese male Zucker rats
  • Dosages: 10 μmol/kg
  • Administration: Orally administrated at a single dose

Solubility (25°C)

In vitro

In vivo

Add solvents to the product individually and in order
(Data is from Selleck tests instead of citations):
Saline
For best results, use promptly after mixing.

30 mg/mL

Chemical Information

Molecular Weight 303.4
Formula

C17H25N3O2

CAS No. 274901-16-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1CC(N(C1)C(=O)CNC23CC4CC(C2)CC(C4)(C3)O)C#N

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

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.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 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.

Molarity Calculator

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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 --
NCT05337969 Completed Drug: Metformin and Vildagliptin 850/50 mg To Determine Bioequivalence Under Fed Conditions AET Laboratories Private Limited|Alfred E. Tiefenbacher (GmbH & Co. KG) December 2015 Not Applicable
NCT05329857 Completed Drug: Metformin and Vildagliptin 1000/50 mg To Determine Bioequivalence Under Fed Conditions AET Laboratories Private Limited|Alfred E. Tiefenbacher (GmbH & Co. KG) December 2015 Not Applicable
NCT05329844 Completed Drug: Vildagliptin 50 MG Diabetes Mellitus AET Laboratories Private Limited|Alfred E. Tiefenbacher (GmbH & Co. KG) February 2014 Not Applicable

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

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.

Handling Instructions

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