Vildagliptin (Synonyms: LAF237; NVP-LAF 237)

Name: Vildagliptin
Brand: MedChemExpress
SKU: HY-14291
Rating: 5.0 (6 reviews)

Cat. No.: HY-14291 Purity: 99.61%: FAQs
Data Sheet SDS COA Handling Instructions

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Vildagliptin (LAF237) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC₅₀ of 3.5 nM in human Caco-2 cells. Vildagliptin possesses excellent oral bioavailability and potent antihyperglycemic activity.

For research use only. We do not sell to patients.

Vildagliptin Chemical Structure

CAS No. : 274901-16-5

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water ready for reconstitution	USD 61	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in Water	USD 61	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 35	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 55	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 77	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
500 mg	USD 154	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 6 publication(s) in Google Scholar

Other Forms of Vildagliptin:

4 Publications Citing Use of MCE Vildagliptin

RT-PCR

: Vildagliptin purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022, 23(22), 14101; qPCR Assay. Vildagliptin (5 µM; 0, 6, 12, 24, 48, 72 h) stimulates the expression of IL-6 in HaCaT cells.

: Vildagliptin purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2018 Apr 28;420:26-37. [Abstract]; Representative images showing visible metastatic nodules in the lungs of mice treated with Vildagliptin and fed an high-fat diet (HFD).

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DPP-1 DPP-2 DPP-4 DPP-8 DPP-9

Biological Activity
Purity & Documentation
References
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Description

IC₅₀ & Target

DPP-4

Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	IC₅₀	62 nM Compound: Vildagliptin	Inhibition of DPP4 in human Caco2 cells using H-Ala-Pro-7-amido-4-trifluoromethylcoumarin as substrate after 1 hr by fluorescence assay Inhibition of DPP4 in human Caco2 cells using H-Ala-Pro-7-amido-4-trifluoromethylcoumarin as substrate after 1 hr by fluorescence assay	[PMID: 23623674]
HEK293	IC₅₀	52 μM Compound: 3	Inhibition of mouse recombinant FAP expressed in HEK293 cells assessed as pNA release from Ala-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique Inhibition of mouse recombinant FAP expressed in HEK293 cells assessed as pNA release from Ala-Pro-p-nitroanilide pre-incubated with enzyme for 15 mins prior to substrate addition by fluorescence technique	[PMID: 22525314]
Sf9	IC₅₀	0.14 μM Compound: Vildagliptin	Inhibition of recombinant full-length human N-terminal GST-tagged DPP9 expressed in Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay Inhibition of recombinant full-length human N-terminal GST-tagged DPP9 expressed in Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay	[PMID: 30642693]
Sf9	IC₅₀	2.3 μM Compound: Vildagliptin	Inhibition of recombinant full-length human N-terminal GST-tagged DPP8 expressed in Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay Inhibition of recombinant full-length human N-terminal GST-tagged DPP8 expressed in Sf9 insect cells using Gly-Pro-AMC as substrate measured at 60 secs interval for 20 mins by fluorescence assay	[PMID: 30642693]
U-87MG ATCC	IC₅₀	79.76 μM Compound: Vildagliptin	Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay Inhibition of FAP in human U87MG cells using Suc-Gly-Pro-AMC as substrate by fluorescence based assay	[PMID: 32527554]

In Vitro

Vildagliptin promotes beta cell survival by inhibiting cell apoptosis. Vildagliptin also promotes cell proliferation^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Vildagliptin (35 mg/kg; once daily by oral gavage) increases plasma active GLP-1 levels in islets of db/db mice^[2].
Vildagliptin (10 μmol/kg; orally) significantly decreases glucose excursions and stimulate insulin secretion in obese male Zucker rats^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male db/db mice (BKS) and wildtype mice^[2]
Dosage:	35 mg/kg
Administration:	Oral gavage; once daily; for 6 weeks
Result:	Increased plasma active GLP-1 levels (22.63±1.19 vs. 11.69±0.44).

Animal Model:	Obese male Zucker rats^[1]
Dosage:	10 µmol/kg (Pharmacokinetic Analysis)
Administration:	Orally
Result:	Significantly decreased glucose excursions and stimulate insulin secretion.

Clinical Trial

Molecular Weight

303.40

Formula

C₁₇H₂₅N₃O₂

CAS No.

274901-16-5

Appearance

Solid

Color

White to off-white

SMILES

O[C@@]1(C2)C[C@H]3C[C@H](C[C@]2(NCC(N4[C@H](C#N)CCC4)=O)C3)C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

H₂O : 50 mg/mL (164.80 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.2960 mL	16.4799 mL	32.9598 mL
5 mM	0.6592 mL	3.2960 mL	6.5920 mL
10 mM	0.3296 mL	1.6480 mL	3.2960 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: PBS
Solubility: 100 mg/mL (329.60 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).

Purity & Documentation

Purity: 99.61%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (251 KB) LCMS (89 KB)

Handling Instructions (2659 KB)

References

[1]. Villhauer EB, et al. 1-[[(3-hydroxy-1-adamantyl)amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties. J Med Chem. 2003 Jun 19;46(13):2774-89. [Content Brief]

[2]. Wu YJ, et al. Dipeptidyl peptidase-4 inhibitor, vildagliptin, inhibits pancreatic beta cell apoptosis in associationwith its effects suppressing endoplasmic reticulum stress in db/db mice. Metabolism. 2015 Feb;64(2):226-35. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

H₂O	1 mM	3.2960 mL	16.4799 mL	32.9598 mL	82.3995 mL
	5 mM	0.6592 mL	3.2960 mL	6.5920 mL	16.4799 mL
	10 mM	0.3296 mL	1.6480 mL	3.2960 mL	8.2399 mL
	15 mM	0.2197 mL	1.0987 mL	2.1973 mL	5.4933 mL
	20 mM	0.1648 mL	0.8240 mL	1.6480 mL	4.1200 mL
	25 mM	0.1318 mL	0.6592 mL	1.3184 mL	3.2960 mL
	30 mM	0.1099 mL	0.5493 mL	1.0987 mL	2.7466 mL
	40 mM	0.0824 mL	0.4120 mL	0.8240 mL	2.0600 mL
	50 mM	0.0659 mL	0.3296 mL	0.6592 mL	1.6480 mL
	60 mM	0.0549 mL	0.2747 mL	0.5493 mL	1.3733 mL
	80 mM	0.0412 mL	0.2060 mL	0.4120 mL	1.0300 mL
	100 mM	0.0330 mL	0.1648 mL	0.3296 mL	0.8240 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Vildagliptin Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Vildagliptin274901-16-5LAF237 NVP-LAF 237LAF 237LAF-237Dipeptidyl PeptidaseFerroptosisApoptosisDPPdipeptidylpeptidaseDPP-IVCaco-2cellsantihyperglycemicInhibitorinhibitorinhibit

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Vildagliptin (Synonyms: LAF237; NVP-LAF 237)

Customer Review

Other Forms of Vildagliptin:

Vildagliptin Related Antibodies

4 Publications Citing Use of MCE Vildagliptin

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•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Dipeptidyl Peptidase Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Vildagliptin Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Vildagliptin Related Classifications

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