Name: Vildagliptin
Brand: Selleck Chemicals
SKU: S3033
Availability: InStock
Rating: 5 (13 reviews)

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Quality Control

Batch: Purity: 99.84%

99.84

Related Targets	HDAC Caspase Proteasome Secretase MMP HCV Protease Cysteine Protease Tyrosinase HIV Protease Serine Protease
Other DPP Inhibitors	Talabostat (Val-boroPro, PT-100) Mesylate Puromycin aminonucleoside MK-3102 (Omarigliptin) Brensocatib Lobeliae Chinensis Extract Teneligliptin Hydrobromide Hydrate Anagliptin Trelagliptin Teneligliptin hydrobromide Trelagliptin succinate

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Activity Description
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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	Saline Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	30.000mg/ml (98.88mM)	Taking the 1 mL working solution as an example, add 30 mg of this product to 1 ml of physiological saline (0.9% NaCL solution), mix evenly to make it clear, The mixed solution should be used immediately for optimal results.

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: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

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.

Chemical Information, Storage & Stability

Molecular Weight	303.4	Formula	C₁₇H₂₅N₃O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	274901-16-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	LAF-237, NVP-LAF 237			SMILES	C1CC(N(C1)C(=O)CNC23CC4CC(C2)CC(C4)(C3)O)C#N

Read more about storage stability stock solution CAS number SMILES

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	[1] https://pubmed.ncbi.nlm.nih.gov/12801240/ [2] https://pubmed.ncbi.nlm.nih.gov/21070766/ [3] https://pubmed.ncbi.nlm.nih.gov/20082866/ [4] https://pubmed.ncbi.nlm.nih.gov/20625970/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2019-04-29)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03925701	RECRUITING	dm	Sherief Abd-Elsalam	2019-04-01	PHASE3
NCT06951334	NOT_YET_RECRUITING	Parkinson's Disease	First Affiliated Hospital, Sun Yat-Sen University	2025-06-01
NCT05366868	ACTIVE_NOT_RECRUITING	Diabetes Mellitus, Type 2	National Center for Global Health and Medicine, Japan	2022-05-26	PHASE4
NCT06851962	COMPLETED	Diabetes Mellitus Type 2	Fundación para la Investigación del Hospital Clínico de Valencia	2025-05-26	PHASE4
NCT04761861	WITHDRAWN	Schizophrenia; Dyslipidemias	Sadat City University	2021-02-16	PHASE2
NCT06142656	RECRUITING	Poly Cystic Ovary Syndrome	October 6 University	2023-11-25	PHASE2; PHASE3

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Vildagliptin DPP inhibitor

Chemical Structure

Molecular Weight: 303.4