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Pack Size | Price | Availability | Quantity |
---|---|---|---|
10 mg | $39 | In Stock | |
25 mg | $50 | In Stock | |
50 mg | $61 | In Stock | |
100 mg | $85 | In Stock | |
500 mg | $117 | In Stock | |
1 mL x 10 mM (in DMSO) | $30 | In Stock |
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. |
Alias | NVP-LAF 237, LAF237 |
Molecular Weight | 303.4 |
Formula | C17H25N3O2 |
Cas No. | 274901-16-5 |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||||||||||||||||||||||
Solubility Information | Ethanol: 56 mg/mL (184.6 mM) DMSO: 20 mg/mL (65.92 mM) H2O: 55 mg/mL (181.3 mM) | ||||||||||||||||||||||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||||||||||||||||||||||
DMSO/H2O/Ethanol
H2O/Ethanol
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