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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.
Vildagliptin (35 mg/kg; once daily by oral gavage) increases plasma active GLP-1 levels in islets of db/db mice. Vildagliptin (10 µmol/kg; orally) significantly decreases glucose excursions and stimulate insulin secretion in obese male Zucker rats.
Pharmacology. 2023;108(2):166-175.
DPP4 Inhibitor Sitagliptin Reduces Inflammatory Responses and Mast Cell Activation in Allergic Rhinitis
Vildagliptin purchased from AbMole
| Cell Experiment | |
|---|---|
| Cell lines | |
| Preparation method | |
| Concentrations | |
| Incubation time | |
| Animal Experiment | |
|---|---|
| Animal models | Obese male Zucker rats |
| Formulation | 0.5% carboxymethylcellulose (CMC) and 0.2% Tween 80 |
| Dosages | 10 μmol/kg |
| Administration | Orally administrated at a single dose |
| Molecular Weight | 303.4 |
| Formula | C17H25N3O2 |
| CAS Number | 274901-16-5 |
| Solubility (25°C) | Water 45 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[1] Michał Wiciński, et al. Vasculoprotective Effects of Vildagliptin. Focus on Atherogenesis
| Related Dipeptidyl Peptidase Products |
|---|
| Sitagliptin phosphate monohydrate
Sitagliptin phosphate (MK-0431) is a potent inhibitor of dipeptidyl peptidase-4 (DPP-4) with IC50 of 19 nM. |
| Trelagliptin
Trelagliptin (SYR-472) is a novel once-weekly oral DPP-4 inhibitor for type 2 diabetes. |
| Alogliptin
Alogliptin is a potent, selective inhibitor of DPP-4 with IC50 of <10 nM, exhibits greater than 10,000-fold selectivity over DPP-8 and DPP-9. |
| Linagliptin
Linagliptin is a highly potent, selective DPP-4 inhibitor with IC50 of 1 nM. |
| Saxagliptin
Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active inhibitor of dipeptidyl peptidase 4 (DPP-4) (Ki = 0.6-1.3 nM). Saxagliptin can be used in type 2 diabetes studies. |
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