store at low temperature
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Vildagliptin [274901-16-5]
Référence T1502-500mg
Conditionnement : 500mg
Marque : TargetMol
Contactez votre distributeur local :
Téléphone : +1 850 650 7790
Vildagliptin
Catalog No. T1502 CAS 274901-16-5
Synonyms: NVP-LAF 237, LAF237
Vildagliptin (LAF237) is a cyanopyrrolidine-based, orally bioavailable inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. Vildagliptin's cyano moiety undergoes hydrolysis and this inactive metabolite is excreted mainly via the urine.
All TargetMol products are for research or drug registration purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose in violation of laws and regulations.
Vildagliptin, CAS 274901-16-5
| Description | Vildagliptin (LAF237) is a cyanopyrrolidine-based, orally bioavailable inhibitor of dipeptidyl peptidase 4 (DPP-4), with hypoglycemic activity. Vildagliptin's cyano moiety undergoes hydrolysis and this inactive metabolite is excreted mainly via the urine. |
| Targets&IC50 | DPP4:2.3 nM |
| In vitro | In obese male Zucker rats, oral administration of Vildagliptin (10 μmol/kg, p.o.) during a glucose tolerance test increases GLP-1 levels, additionally stimulates insulin secretion, and significantly reduces fluctuations in blood glucose levels. In cynomolgus monkeys treated with Vildagliptin (1 μmol/kg, p.o.), plasma DPP-IV activity is maximally inhibited (95%) approximately 2 hours post-treatment, with inhibition >50% occurring within 30 minutes and lasting over 10 hours. In adult male Sprague-Dawley rats induced with diabetes by Streptozotocin, Vildagliptin treatment of 10 mg/kg for 32 weeks prevents nerve fiber loss. At a dosage of 60 mg/kg, Vildagliptin enhances β-cell replication and decreases apoptosis, leading to an increase in pancreatic β-cell mass, which remains elevated for 12 days post withdrawal of Vildagliptin. |
| In vivo | As the most stable DPP-4 inhibitor, Vildagliptin binds to the DPP-4 S1 and S2 catalytic sites, mimicking the transition state of the P-1 site. |
| Synonyms | NVP-LAF 237, LAF237 |
| Molecular Weight | 303.4 |
| Formula | C17H25N3O2 |
| CAS No. | 274901-16-5 |
Storage
Solubility Information
Ethanol: 56 mg/mL (184.6 mM)
DMSO: 20 mg/mL (65.92 mM)
H2O: 55 mg/mL (181.3 mM)
References and Literature
1. Villhauer EB, et al. J Med Chem, 2003, 46(13), 2774-2789. 2. Duttaroy A, et al. Eur J Pharmacol, 2011, 650(2-3), 703-707. 3. Jin HY, et al. Arch Med Res, 2009, 40(7), 536-544. 4. JMiura K, et al. Horm Metab Res, 2010, 42(10), 731-735. 5. Dong L, Shen S, Chen W, et al. Discovery of Novel Inhibitors Targeting Human O-GlcNAcase: Docking-Based Virtual Screening, Biological Evaluation, Structural Modification, and Molecular Dynamics Simulation[J]. Journal of chemical information and modeling. 2019, 59(10): 4374-4382.