| Name | Vildagliptin |
| 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. |
| 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. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Ethanol : 56 mg/mL (184.57 mM), Sonication is recommended.
DMSO : 250 mg/mL (823.99 mM), Sonication is recommended.
H2O : 55 mg/mL (181.28 mM), Sonication is recommended.
|
| Keywords | Vildagliptin | peptidase | NVP-LAF-237 | NVP-LAF237 | LAF-237 | LAF 237 | Inhibitor | inhibit | Ferroptosis | DPP-IV | DPP-4 | DPP4 | DPP | Dipeptidyl Peptidase | dipeptidyl | cells | Caco-2 | Apoptosis | antihyperglycemic |
| Inhibitors Related | Stavudine | Aceglutamide | Hemin | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sildenafil citrate |
| Related Compound Libraries | Highly Selective Inhibitor Library | Ferroptosis Compound Library | Bioactive Compound Library | EMA Approved Drug Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Inhibitor Library | Anti-Cancer Approved Drug Library | Immunology/Inflammation Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Cancer Drug Library |
United States
