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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.

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Vildagliptin Chemical Structure
Vildagliptin, CAS 274901-16-5
Pack Size Availability Price/USD Quantity
10 mg In stock $ 39.00
25 mg In stock $ 50.00
50 mg In stock $ 61.00
100 mg In stock $ 85.00
500 mg In stock $ 117.00
1 mL * 10 mM (in DMSO) In stock $ 30.00
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Purity: 100%
Purity: 99.03%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
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 DPP-4:2.3 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

store at low temperature

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 56 mg/mL (184.6 mM)

DMSO: 56 mg/mL (184.6 mM)

H2O: 55 mg/mL (181.3 mM)

TargetMolReferences 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.

TargetMolCitations

1. 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. Journal of chemical information and modeling. 2019, 59(10): 4374-4382.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Highly Selective Inhibitor Library FDA-Approved & Pharmacopeia Drug Library Bioactive Compounds Library Max Autophagy Compound Library Metabolism Compound Library Anti-COVID-19 Compound Library Protease Inhibitor Library

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Keywords

Vildagliptin 274901-16-5 Apoptosis Proteases/Proteasome Ubiquitination Proteasome Ferroptosis DPP-4 Dipeptidyl Peptidase Inhibitor peptidase Caco-2 cells LAF-237 NVP-LAF 237 NVP-LAF237 dipeptidyl LAF 237 DPP-IV NVP-LAF-237 antihyperglycemic DPP LAF237 inhibit inhibitor

 

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