Home Proteases DPP inhibitor Vildagliptin

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Vildagliptin DPP inhibitor

Cat.No.S3033

Vildagliptin inhibits DPP−4 with IC50 of 2.3 nM.
Vildagliptin DPP inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 303.4

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Quality Control

Batch: Purity: 99.84%
99.84

Cell Culture, Treatment & Working Concentration

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
insect cells Function assay Inhibition of human recombinant His-tagged DPP4 expressed in insect cells, IC50=0.056 μM
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 60 mg/mL (197.75 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 60 mg/mL

Ethanol : 60 mg/mL

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In vivo
Batch:

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.
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Chemical Information, Storage & Stability

Molecular Weight 303.4 Formula

C17H25N3O2

 Storage (From the date of receipt)
CAS No. 274901-16-5 Download SDF Storage of Stock Solutions

Synonyms LAF-237, NVP-LAF 237 Smiles C1CC(N(C1)C(=O)CNC23CC4CC(C2)CC(C4)(C3)O)C#N

Mechanism of Action

Targets/IC50/Ki
DPP-4
(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.

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. This compound 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 this compound (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. This chemical (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. This compound administrated at doses of 10 mg/kg for 32 weeks protects nerve fiber loss in streptozotocin (STZ)-induced diabetic adult male Sprague Dawley rats.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/20625970/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

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