Vildagliptin
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.
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 274901-16-5
- Formula: C17H25N3O2
- Molecular Weight:303.40
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Apoptosis Compound Library
HY-L003
-
Immunology/Inflammation Compound Library
HY-L007
-
Metabolism/Protease Compound Library
HY-L012
-
FDA-Approved Drug Library
HY-L022
-
Anti-Cancer Compound Library
HY-L025
-
Drug Repurposing Compound Library
HY-L035
-
Covalent Screening Library
HY-L036
-
Anti-diabetic Compound Library
HY-L040
-
Ferroptosis Compound Library
HY-L051
-
NMPA-Approved Drug Library
HY-L053
-
FDA Approved & Pharmacopeial Drug Library
HY-L066
-
Lipid Metabolism Compound Library
HY-L091
-
EMA-Approved Drug Library
HY-L116
-
FDA-Approved Anticancer Drug Library
HY-L122
-
Human Metabolite Library
HY-L123
-
Non-steroidal Anti-Inflammatory Compound Library
HY-L130
-
Heterocyclic Compound Library
HY-L138
-
Off-patent Drug Library
HY-L141
-
Metabolic Enzyme Compound Library
HY-L146
-
Protease Inhibitor Library
HY-L147
-
Highly Selective Inhibitors Library
HY-L158
-
Cell Death Library
HY-L162
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Covalent Screening Library Plus
HY-L036P
-
Drug Repurposing Compound Library Plus
HY-L035P
-
FDA-Approved Drug Library Plus
HY-L022P
-
FDA-Approved Drug Library Mini
HY-L022M
-
Bioactive Compound Library
HY-L001
-
Amino Acid Metabolism Compound Library
HY-L189
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
-
Mass Spectrometry Human Metabolite Library
HY-L215
-
Classic FDA-Approved Drug Library
HY-L261
Publications Citing Use of MedChemExpress (MCE) Vildagliptin
More
Customer Validation & Images
-
RT-PCR
-
IF
Biological Activity
|
DPP-4 |
|
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] |
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 274901-16-5
-
Appearance Solid
-
Molecular Weight 303.40
-
Formula 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
-
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
Publications (5)
-
Journal Impact Factor
-
Most Recent
-
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
Solvent & Solubility
H2O : 50 mg/mL (164.80 mM; Need ultrasonic)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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
Please enter the basic information of animal 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.
Purity & Documentation
-
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)
- Portuguese - PT (393 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
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.
| 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.
Powered by Bioz