Vildagliptin dihydrate
Based on 5 publication(s) in Google Scholar
Vildagliptin dihydrate (LAF237 dihydrate) is a potent, stable, selective dipeptidyl peptidase IV (DPP-IV) inhibitor with an IC50 of 3.5 nM in human Caco-2 cells. Vildagliptin dihydrate possesses excellent oral bioavailability and potent antihyperglycemic activity.
For research use only. We do not sell to patients.
- CAS No.: 2133364-01-7
- Formula: C17H29N3O4
- Molecular Weight:339.43
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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HY-10284
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Linagliptin (Standard)DPP-4 Inhibitor
Publications Citing Use of MedChemExpress (MCE) Vildagliptin dihydrate
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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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Biological Activity
Description
IC50 & Target
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DPP-4 |
In Vitro
In Vivo
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.
Chemical Information
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CAS No. 2133364-01-7
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Molecular Weight 339.43
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Formula C17H29N3O4
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SMILES
O[C@@]1(C[C@H](C2)C3)C[C@H]3C[C@@]2(NCC(N4CCC[C@H]4C#N)=O)C1.O.O
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Synonyms
LAF237 dihydrate; NVP-LAF 237 dihydrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
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 dihydrate 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 dihydrate 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 dihydrate 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 dihydrate 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
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Protocol for Pharmacokinetic Study
Pharmacokinetic studies quantify how an organism handles a drug over time through absorption, distribution, metabolism, and excretion, and the core experimental readout is the concentration-time profile of parent drug and, when relevant, metabolites in biological matrices such as plasma, whole blood, urine, bile, or tissue. Pharmacokinetic analysis links dose, route, exposure, clearance, half-life, distribution, bioavailability, and systemic exposure to drug efficacy and toxicity hypotheses rather than measuring a signaling pathway directly. The literature links pharmacokinetics to drug-development phenotypes by showing that drug metabolism and pharmacokinetics influence compound progression, exposure-response interpretation, safety margins, dosing strategy, and failure risk during discovery and development. DMPK science contributes to compound optimization by integrating physicochemical properties, in vitro metabolism, transporter behavior, in vivo exposure, and pharmacodynamic contex
Purity & Documentation
References
[1]. Cheng Q, et al. Combination of the dipeptidyl peptidase IV inhibitor LAF237 [(S)-1-[(3-hydroxy-1-adamantyl)ammo]acetyl-2-cyanopyrrolidine] with the angiotensin II type 1 receptor antagonist valsartan [N-(1-oxopentyl)-N-[[2'-(1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl]methyl]-L-valine] enhances pancreatic islet morphology and function in a mouse model of type 2 diabetes. J Pharmacol Exp Ther. 2008 Dec;327(3):683-91. [Content Brief]
[2]. Shen M, et al. The synergistic effect of valsartan and LAF237 [(S)-1-[(3-hydroxy-1-adamantyl)ammo]acetyl-2-cyanopyrrolidine] on vascular oxidative stress and inflammation in type 2 diabetic mice. Exp Diabetes Res. 2012;2012:146194. [Content Brief]
[3]. Abdelhamid AM, et al. Vildagliptin/Pioglitazone Combination Improved The Overall Glycemic Control In Type I Diabetic Rats. Can J Physiol Pharmacol. 2018 Mar 6. doi: 10.1139/cjpp-2017-0680. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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