| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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Purity: ≥98%
Vildagliptin (formerly also known as NVP LAF237; DSP-7238; LAF-237; trade name: Zomelis) is an potent and orally bioavailable anti-diabetic medication with an IC50 of 2.3 nM that functions as a DPP-4 (dipeptidyl peptidase 4) inhibitor. Vildagliptin prevents DPP-4 from inactivating GLP-1 and GIP, which enables GLP-1 and GIP to enhance insulin secretion in beta cells and inhibit glucagon release by alpha cells in the pancreatic islets of Langerhans. It has been demonstrated that vildagliptin lowers hyperglycemia in people with type 2 diabetes. In February 2008, the European Union approved vildagliptin as an anti-hyperglycemic medication.
| Targets |
DPP-IV (IC50 = 3.5 nM)
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|---|---|
| ln Vitro |
Vildagliptin inhibits cell apoptosis, which increases beta cell survival. Additionally, vildagliptin stimulates cell division[2].
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| ln Vivo |
Vildagliptin (35 mg/kg; once daily by oral gavage) raises the levels of plasma active GLP-1 in the islets of db/db mice[2].
Vildagliptin Vildagliptin (10 µmol/kg; oral) in obese male Zucker rats significantly reduces glucose excursions and increases insulin secretion[1]. in obese male Zucker rats significantly reduces glucose excursions and increases insulin secretion[1]. |
| Enzyme Assay |
Vildagliptin (LAF-237; NVP-LAF 237) has an IC50 of 2.3 nM, which inhibits DPP-4. Figure 2 represents vildagliptin, an N-substituted glycyl-2-cyanopyrrolidine. With an inhibitory concentration (IC50) of approximately 2–3 nmol/L, it is a strong, reversible, and competitive inhibitor of DPP-4 in both humans and rodents in vitro. Crucially, vildagliptin exhibits high specificity inhibition of DPP-4 in comparison to other analogous peptidases, wherein its IC50 surpasses 200 mol/L.
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| Animal Protocol |
Male db/db mice (BKS) and wildtype mice[2]
35 mg/kg Oral gavage; once daily; for 6 weeks |
| References |
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| Molecular Formula |
C17H25N3O2
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|---|---|
| Molecular Weight |
303.4
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| Exact Mass |
303.19
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| Elemental Analysis |
C, 67.30; H, 8.31; N, 13.85; O, 10.55
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| CAS # |
274901-16-5
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| Related CAS # |
(2R)-Vildagliptin;1036959-27-9;Vildagliptin-d3;1217546-82-1;Vildagliptin-13C5,15N;1044741-01-6;Vildagliptin dihydrate;2133364-01-7;Vildagliptin-d7;1133208-42-0
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| Appearance |
White to off-white solid powder
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| SMILES |
C1C[C@H](N(C1)C(=O)CNC23CC4CC(C2)CC(C4)(C3)O)C#N
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| InChi Key |
SYOKIDBDQMKNDQ-XWTIBIIYSA-N
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| InChi Code |
InChI=1S/C17H25N3O2/c18-9-14-2-1-3-20(14)15(21)10-19-16-5-12-4-13(6-16)8-17(22,7-12)11-16/h12-14,19,22H,1-8,10-11H2/t12?,13?,14-,16?,17?/m0/s1
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| Chemical Name |
(2S)-1-[2-[(3-hydroxy-1-adamantyl)amino]acetyl]pyrrolidine-2-carbonitrile
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| Synonyms |
Vildagliptin; DSP 7238; DSP7238; NVP-LAF 237; NVP LAF 237; DSP-7238; LAF237; LAF-237; LAF 237; NVP LAF-237; trade name: Zomelis
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (329.60 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
Solubility in Formulation 2: Saline: 30 mg/mL (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04410341 | Recruiting | Drug: Vildagliptin 50 MG Drug: Escitalopram 20 mg |
Major Depressive Disorder | Sadat City University | May 1, 2020 | Phase 1 Phase 2 |
| NCT05429554 | Recruiting | Drug: Vildagliptin | Type 2 Diabetes Mellitus | MTI University | June 2022 | |
| NCT04761861 | Recruiting | Drug: Vildagliptin 50 MG Drug: Placebo |
Schizophrenia Dyslipidemias |
Sadat City University | February 16, 2021 | Phase 2 |
| NCT03925701 | Recruiting | Drug: Vildagliptin Drug: vildagliptin\metformin |
dm | Sherief Abd-Elsalam | April 1, 2019 | Phase 3 |
| NCT06068686 | Recruiting | Drug: Vildagliptin 50 MG Drug: Glimepiride 3 Mg Oral Tablet |
Type 2 Diabetes | Damanhour University | October 1, 2022 | Not Applicable |
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