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Vildagliptin

Vildagliptin
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.
Catalog No. T1502Cas No. 274901-16-5
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Vildagliptin

Catalog No. T1502Cas No. 274901-16-5

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.
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Pack SizePriceAvailabilityQuantity
10 mg$39In Stock
25 mg$50In Stock
50 mg$61In Stock
100 mg$85In Stock
500 mg$117In Stock
1 mL x 10 mM (in DMSO)$30In Stock
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Product Introduction

Bioactivity
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.
AliasNVP-LAF 237, LAF237
Chemical Properties
Molecular Weight303.4
FormulaC17H25N3O2
Cas No.274901-16-5
Storage & Solubility Information
Storagestore 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
1mg5mg10mg50mg
1 mM3.2960 mL16.4799 mL32.9598 mL164.7989 mL
5 mM0.6592 mL3.2960 mL6.5920 mL32.9598 mL
10 mM0.3296 mL1.6480 mL3.2960 mL16.4799 mL
20 mM0.1648 mL0.8240 mL1.6480 mL8.2399 mL
50 mM0.0659 mL0.3296 mL0.6592 mL3.2960 mL
H2O/Ethanol
1mg5mg10mg50mg
100 mM0.0330 mL0.1648 mL0.3296 mL1.6480 mL

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