Home Proteases DPP inhibitor Vildagliptin For research use only.

Vildagliptin

Synonyms: LAF-237, NVP-LAF 237

Vildagliptin inhibits DPP−4 with IC50 of 2.3 nM.

Vildagliptin Chemical Structure

Vildagliptin Chemical Structure

CAS: 274901-16-5

Selleck's Vildagliptin has been cited by 10 publications

Purity & Quality Control

Batch: Purity: 99.84%
99.84

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Caco-2 cells Function assay Inhibition of human DPP4 expressed in Caco-2 cells, Ki=0.004 μM 17034148
insect cells Function assay Inhibition of human recombinant His-tagged DPP4 expressed in insect cells, IC50=0.056 μM 20718420
Click to View More Cell Line Experimental Data

Biological Activity

Description Vildagliptin inhibits DPP−4 with IC50 of 2.3 nM.
Targets
DPP-4 [1]
(Cell-free assay)
2.3 nM
In vitro
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]
In Vivo
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 Animal Models Obese male Zucker rats
Dosages 10 μmol/kg
Administration Orally administrated at a single dose
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04081857 Completed Health Subjective Hanmi Pharmaceutical Company Limited June 3 2019 Phase 1
NCT04087525 Completed Health Subjective Hanmi Pharmaceutical Company Limited October 23 2018 Phase 1
NCT03577184 Withdrawn Diabetes Mellitus Type 2 Clinision July 2018 --
NCT05337969 Completed To Determine Bioequivalence Under Fed Conditions AET Laboratories Private Limited|Alfred E. Tiefenbacher (GmbH & Co. KG) December 2015 Not Applicable
NCT05329857 Completed To Determine Bioequivalence Under Fed Conditions AET Laboratories Private Limited|Alfred E. Tiefenbacher (GmbH & Co. KG) December 2015 Not Applicable
NCT05329844 Completed Diabetes Mellitus AET Laboratories Private Limited|Alfred E. Tiefenbacher (GmbH & Co. KG) February 2014 Not Applicable

Chemical lnformation & Solubility

Molecular Weight 303.4 Formula

C17H25N3O2
CAS No. 274901-16-5 SDF Download Vildagliptin SDF
Smiles C1CC(N(C1)C(=O)CNC23CC4CC(C2)CC(C4)(C3)O)C#N
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 60 mg/mL ( (197.75 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 60 mg/mL

Ethanol : 60 mg/mL


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In vivo
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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.
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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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