1. Metabolic Enzyme/Protease
  2. Dipeptidyl Peptidase

Vildagliptin dihydrate (Synonyms: LAF237 dihydrate; NVP-LAF 237 dihydrate)

Cat. No.: HY-14291A
Handling Instructions

Vildagliptin (LAF237 dihydrate;NVP-LAF 237 dihydrate) is a dipeptidyl peptidase 4 (DPP4) inhibitor that delays the degradation of glucagon-like peptide-1 (GLP-1).

For research use only. We do not sell to patients.

Vildagliptin dihydrate Chemical Structure

Vildagliptin dihydrate Chemical Structure

CAS No. : 2133364-01-7

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Customer Review

Other Forms of Vildagliptin dihydrate:

    Vildagliptin dihydrate purchased from MCE. Usage Cited in: Cancer Lett. 2018 Apr 28;420:26-37.

    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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    Description

    Vildagliptin (LAF237 dihydrate;NVP-LAF 237 dihydrate) is a dipeptidyl peptidase 4 (DPP4) inhibitor that delays the degradation of glucagon-like peptide-1 (GLP-1).

    IC50 & Target

    Target: Dipeptidyl Peptidase 4 (DPP4)[1]

    In Vivo

    Treatment of obese diabetic mice with 1 mg/kg/day Vildagliptin or with 10 mg/kg/day valsartan for 8 weeks increases pancreatic islet β-cell density and stimulates islet β-cell proliferation while preventing apoptosis and islet fibrosis and decreasing superoxide production and nitrotyrosine formation. The combination of both compounds significantly magnifies the beneficial effect of either monotherapy[1]. Valsartan or Vildagliptin pretreatment significantly increases plasma GLP-1 expression, reduces apoptosis of endothelial cells isolated from diabetic mice aorta. The expression of NADPH oxidase subunits also significantly decreases resulting in decreased superoxide production and ICAM-1 (fold change: valsartan : 7.5±0.7, P<0.05; LAF237: 10.2±1.7, P<0.05), VCAM-1 (fold change: valsartan : 5.2±1.2, P<0.05; LAF237: 4.8±0.6, P<0.05), and MCP-1 (fold change: valsartan: 3.2±0.6, LAF237: 4.7±0.8; P<0.05) expression. Moreover, the combination treatment with valsartan and Vildagliptin results in a more significant increase of GLP-1 expression. The decrease of the vascular oxidative stress and inflammation reaction is also higher than monotherapy with valsartan or Vildagliptin[2]. Daily oral administration of Vildagliptin (5 mg/kg) alone or in combination with Pioglitazone (20 mg/kg) for 7 weeks significantly reduces blood glucose levels and HbA1c. It increases serum insulin levels and decreases serum glucagon. It also shows a strong anti-oxidant activity[3].

    Clinical Trial
    References
    Animal Administration
    [1][3]

    Rats[3]

    Rats are randomly divided into four groups. (I) Normal control: Untreated control animals (n=12). (II) Diabetic control: Untreated diabetic group (n=18). (III) Vildagliptin: Diabetic rats treated with Vildagliptin (5 mg/kg) (n=12). (IV) Vildagliptin/Pio: Diabetic rats treated with Vildagliptin (5 mg/kg) and Pio (20 mg/kg) (n=12). Treatments are given once daily per-oral for 7 weeks starting from day 1 of confirmation of diabetes. Blood samples are collected from tail vein weekly for 7 weeks. Animals are sacrificed for further analysis[3].

    Mice[1]

    For chronic treatment, 4-week-old obese db/db male mice are randomly assigned to Vildagliptin dosage groups. Each group consists of 6 to 10 mice. The mice receive different concentrations of Vildagliptin dissolved in their drinking water for 8 weeks to determine optimal dose for reducing hyperglycemia and glucose intolerance. From initial pilot studies, the dose of Vildagliptin (1 mg/kg/day) is selected for further analysis. Two additional groups of 4-week-old db/db mice receive either valsartan alone (10 mg/kg/day) or combined with Vildagliptin (1 mg/kg/day)[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    339.43

    Formula

    C₁₇H₂₉N₃O₄

    CAS No.

    2133364-01-7

    SMILES

    O[[email protected]@]1(C[[email protected]](C2)C3)C[[email protected]]3C[[email protected]@]2(NCC(N4CCC[[email protected]]4C#N)=O)C1.O.O

    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.

    Shipping

    Room temperature in continental US; may vary elsewhere

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    Product Name:
    Vildagliptin dihydrate
    Cat. No.:
    HY-14291A
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    Vildagliptin dihydrate

    Cat. No.: HY-14291A