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Vildagliptin(NVP LAF 237 DSP7238 LAF237)
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Vildagliptin(NVP LAF 237 DSP7238 LAF237)图片
CAS NO:274901-16-5
规格:≥98%
包装与价格：
包装价格(元)
100mg电议
250mg电议
500mg电议
1g电议
2g电议
5g电议

产品介绍
Vildagliptin (formerly also known as NVP LAF237; DSP-7238; LAF-237; trade name: Zomelis) is an potent and orally bioavailable anti-diabetic drug that acts as an inhibitor of DPP-4 (dipeptidyl peptidase 4) with an IC50 of 2.3 nM. Vildagliptin inhibits the inactivation of GLP-1 and GIP by DPP-4, allowing GLP-1 and GIP to potentiate the secretion of insulin in the beta cells and suppress glucagon release by the alpha cells of the islets of Langerhans in the pancreas. Vildagliptin has been shown to reduce hyperglycemia in type 2 diabetes mellitus. Vildagliptin was approved in Feb 2008 by in EU as an anti-hyperglycemic agent.
理化性质和储存条件
Molecular Weight (MW)303.4
FormulaC17H25N3O2
CAS No.274901-16-5
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 60 mg/mL (197.8 mM)
Water: N/A
Ethanol: 60 mg/mL (197.8 mM)
Solubility (In vivo)Saline: 30 mg/mL
SynonymsVildagliptin; DSP 7238; DSP7238; NVP-LAF 237; NVP LAF 237; DSP-7238; LAF237; LAF-237; LAF 237; NVP LAF-237; trade name: Zomelis

Chemical Name:   (S)-1-(2-(((1s,3R,5R,7S)-3-hydroxyadamantan-1-yl)amino)acetyl)pyrrolidine-2-carbonitrile

InChi Key:   SYOKIDBDQMKNDQ-AUOOEQCUSA-N

InChi Code:   InChI=1S/C17H25N3O2/c18-9-14-2-1-3-20(14)15(21)10-19-16-5-12-4-13(6-16)8-17(22,7-12)11-16/h12-14,19,22H,1-8,10-11H2/t12-,13+,14-,16-,17-/m0/s1

SMILES Code:   N#C[C@H]1N(C(CN[C@@]23C[C@@]4(O)C[C@](C3)([H])C[C@@](C4)([H])C2)=O)CCC1

实验参考方法
In Vitro

In vitro activity: Vildagliptin is the most stable DPP-IV inhibitor, binding in the S1- and S2-catalytic sites of DPP-IV, possessing a P-1 site transition-state mimetic.

Kinase Assay: Vildagliptin (LAF-237; NVP-LAF 237) inhibits DPP-4 with IC50 of 2.3 nM. Vildagliptin is an N-substituted glycyl-2-cyanopyrrolidine (figure 2). It is a potent competitive and reversible inhibitor of human and rodent DPP-4 in vitro, with a median inhibitory concentration (IC50) ~2-3 nmol/L. Importantly, vildagliptin inhibits DPP-4 with high specificity relative to other similar peptidases where its IC50 exceeds 200 mol/L.

In VivoVildagliptin(orally dosed with 10 μmol/kg) is a potent, orally active inhibitor of plasma DPP-IV activity that provides increased levels of GLP-1 in an oral glucose tolerance test (OGTT) with Obese male Zucker rats. Vildagliptin orally dosed with 10 μmol/kg both significantly decreases glucose excursions and stimulates insulin secretion in Obese male Zucker rats. Maximum inhibition of plasma DPP-IV activity (95%) is observed approximately 2 hours postdose of Vildagliptin (1 μmol/kg, po) while>50% inhibition of DPP-IV is observed within 30 min postdose and persisted for>10 hours in normal Cynomolgus monkeys. Vildagliptin(60 mg/kg) increases pancreatic beta cell mass through enhanced beta cell replication and reduced apoptosis, and the increased beta cell mass is sustained for 12 days after vildagliptin washout. Vildagliptin administrated at doses of 10 mg/kg for 32 weeks protects nerve fiber loss in streptozotocin (STZ)-induced diabetic adult male Sprague Dawley rats.
Animal modelObese male Zucker rats
Formulation & DosageDissolved in 0.5% carboxymethylcellulose (CMC) and 0.2% Tween 80; 10 μmol/kg; p.o. administration
ReferencesJ Med Chem. 2003 Jun 19;46(13):2774-89; Eur J Pharmacol. 2011 Jan 15;650(2-3):703-7.