ビルダグリプチン
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度 : 99.93%
- CAS 番号: 274901-16-5
- 分子式: C17H25N3O2
- 分子量:303.40
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 Vildagliptin
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Cell Proliferation/Viability Assay
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Bio/Physico-chemical Assay
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RT-PCR
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IF
生物活性
製品説明
IC50 & Target
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DPP-4 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | IC50 |
62 nM
Compound: Vildagliptin
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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
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[PMID: 23623674] |
| HEK293 | IC50 |
52 μM
Compound: 3
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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
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[PMID: 22525314] |
| Sf9 | IC50 |
0.14 μM
Compound: Vildagliptin
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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
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[PMID: 30642693] |
| Sf9 | IC50 |
2.3 μM
Compound: Vildagliptin
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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
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[PMID: 30642693] |
| U-87MG ATCC | IC50 |
79.76 μM
Compound: Vildagliptin
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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
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[PMID: 32527554] |
体外実験
体内実験
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.
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Animal Model:Male db/db mice (BKS) and wildtype mice[2]
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Dosage:35 mg/kg
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Administration:Oral gavage; once daily; for 6 weeks
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Result:Increased plasma active GLP-1 levels (22.63±1.19 vs. 11.69±0.44).
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Animal Model:Obese male Zucker rats[1]
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Dosage:10 µmol/kg (Pharmacokinetic Analysis)
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Administration:Orally
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Result:Significantly decreased glucose excursions and stimulate insulin secretion.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 274901-16-5
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性状 Solid
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分子量 303.40
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分子式 C17H25N3O2
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Color White to off-white
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SMILES
O[C@@]1(C2)C[C@H]3C[C@H](C[C@]2(NCC(N4[C@H](C#N)CCC4)=O)C3)C1
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別名
Vildagliptin; LAF237; NVP-LAF 237
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
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
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Most Recent
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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).
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Cell Rep
Dipeptidylpeptidase 4 promotes survival and stemness of acute myeloid leukemia stem cells. [Abstract]2023 Feb 28;42(2):112105. PMID: 36807138
Vildagliptin purchased from MedChemExpress. Usage Cited in: Cell Rep. 2023 Feb 28;42(2):112105. [Abstract]
DPP4 inhibitors (linagliptin 200 nM, vildagliptin 300 nM) suppress the growth of THP1 cells (n = 3 wells).
Vildagliptin purchased from MedChemExpress. Usage Cited in: Cell Rep. 2023 Feb 28;42(2):112105. [Abstract]
Comparative efficacies of two different DPP4 inhibitors at indicated concentrations in suppression of mouse MLL-AF9 cell CFU numbers (2,000 cells/well, n = 3 wells) and DPP4 enzyme activity of 1 × 106 cells (n = 3 repeats). L, linagliptin; V, vildagliptin.
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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.
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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
溶剤 & 溶解度
体外:
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.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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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.
純度とドキュメンテーション
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データシート (276 KB)
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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)
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取扱説明書 (2659 KB)
参考文献
[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.
Vildagliptin 関連分類
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