2133364-01-7
2133364-01-7 structure
- Name: Vildagliptin dihydrate
- Chemical Name: Vildagliptin dihydrate
- CAS Number: 2133364-01-7
- Molecular Formula: C17H29N3O4
- Molecular Weight: 339.43
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Dipeptidyl Peptidase
- Create Date: 2018-03-06 18:08:19
- Modify Date: 2024-01-15 07:14:45
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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).
| Name | Vildagliptin dihydrate |
|---|
| 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). |
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| Related Catalog | |
| 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]. |
| Animal Admin | 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]. |
| References |
| Molecular Formula | C17H29N3O4 |
|---|---|
| Molecular Weight | 339.43 |
| Storage condition | 2-8℃ |