Art. -Nr.: HY-14291

Vildagliptin

(Synonyms: LAF237; NVP-LAF 237)

5 Cited Publications

Kundenbewertung

Based on 5 publication(s) in Google Scholar

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.

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Reinheit: 99.93%
CAS. Nr.: 274901-16-5
Formel: C₁₇H₂₅N₃O₂
Molecular Weight:303.40

Speicherung:

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

Vildagliptin Chemical Structure

CAS. Nr.: 274901-16-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (5)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

DPP-4

Alle Dipeptidyl Peptidase Isoform-spezifische Produkte anzeigen :

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 274901-16-5
Appearance Solid
Molecular Weight 303.40
Formel C₁₇H₂₅N₃O₂
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
Synonyms

LAF237; NVP-LAF 237
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Publications (5)

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Journal Impact Factor

Cancer Lett

Inhibition of dipeptidyl peptidase IV prevents high fat diet-induced liver cancer angiogenesis by downregulating chemokine ligand 2. [Abstract]

2018 Apr 28:420:26-37. PMID: 29409972

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).
Cell Rep

Dipeptidylpeptidase 4 promotes survival and stemness of acute myeloid leukemia stem cells. [Abstract]

2023 Feb 28;42(2):112105. PMID: 36807138
Int J Mol Sci

Dipeptidyl Peptidase-4 Inhibitor-Related Bullous Pemphigoid: Clinical, Laboratory, and Histological Features, and Possible Pathogenesis. [Abstract]

2022 Nov 15;23(22):14101. PMID: 36430582

Vildagliptin purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Nov 15;23(22):14101. [Abstract]

qPCR Assay. Vildagliptin (5 µM; 0, 6, 12, 24, 48, 72 h) stimulates the expression of IL-6 in HaCaT cells.
J Biol Chem

Human DPP9 represses NLRP1 inflammasome and protects against autoinflammatory diseases via both peptidase activity and FIIND domain binding. [Abstract]

2018 Dec 7;293(49):18864-18878. PMID: 30291141
3 Biotech

Neuroprotective effects of DPP-4 inhibitors sitagliptin and vildagliptin in Parkinson's disease via autophagy modulation. [Abstract]

2026 Apr;16(4):146. PMID: 41853215

Lösungsmittel & Löslichkeit

In Vitro:

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

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

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

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

Working solution concentration: 0.22 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) .

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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.

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.

Keywords

Vildagliptin

5 Cited Publications

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Vildagliptin

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Publications Citing Use of MedChemExpress (MCE) Vildagliptin

Alle Dipeptidyl Peptidase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Vildagliptin Related Classifications

HY-14291 Related Classifications