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Vildagliptin

Vildagliptin

Item no.	S3033-10
Manufacturer	Selleckchem
CASRN	274901-16-5
Amount	10 mg
Quantity options	10 mg 1 g 10 g 10 mM/1 ml 25 mg 5 g
Category	Metabolism Diabetes Cholesterol & Lipid Metabolism Regulation of Appetite Inhibitors & Compound Libraries Small Molecules
Type	Inhibitors
Specific against	other
Smiles	C1CC(N(C1)C(=O)CNC23CC4CC(C2)CC(C4)(C3)O)C#N
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	LAF-237,NVP-LAF 237
Similar products	Vildagliptin
Available
Storage Conditions	2 years -80 in solvent
Molecular Weight	303, 4
Administration	Orally administrated at a single dose
Animal Models	Obese male Zucker rats
Clinical Trials	Vildagliptin is in Phase IVclinical trial in patients with Type 2 Diabetes.
Dosages	10 umol/kg
Formulation	0.5% carboxymethylcellulose (CMC) and 0.2% Tween 80
IC50	2.3 nM [1], 2.3 nM [1], 2.3 nM [1], 2.3 nM [1], 2.3 nM [1], 2.3 nM [1]
In vitro	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. [1]
In vivo	Vildagliptin(orally dosed with 10 umol/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 umol/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 umol/kg, po) while >50% inhibition of DPP-IV is observed within 30 min postdose and persisted for >10 hours in normal Cynomolgus monkeys. [1] 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. [2] 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. [3]
Kinase Assay	DPP-IV Inhibition Measurement, An extract from human colonic carcinoma cells (Caco-2) is used as the source of DPP-IV in the assay. The cells are differentiated to induce DPP-IV expression as described. Cell extract is prepared from cells solubilized in lysis buffer (10 mM Tris-HCl, 0.15 M NaCl, 0.04 T.I.U. (trypsin inhibitor unit) aprotinin, 0.5% nonidet-P40, pH 8.0) then centrifuged at 3.5x4g for 30 min at 4 C to remove cell debris. The assay is conducted by adding 20 ug of solubilized Caco-2 protein, diluted to a final volume of 125 uL in assay buffer (25 mM Tris-HCl pH 7.4, 140 mM NaCl, 10 mM KCl, 1% bovine serum albumin) to 96-well flat-bottom microtiter plates. The reaction is initiated by adding 25 uL of 1 mM substrate. The reaction is run at room temperature for 10 min, and then 19 uL of 25% glacial acetic acid is added to stop the reaction. Fluorescence is measured using a CytoFluor II fluorometer (excitation 380 nm/ emission 460 nm). Vildagliptin and solvent controls are added as 30 uL additions, and the assay buffer volume is reduced to 95 uL.
Solubility (25C)	DMSO 60 mg/mL, Water 60 mg/mL, Ethanol 60 mg/mL
Information	Vildagliptin inhibits DPP−4 with IC50 of 2.3 nM.
Chemical Name	2-Pyrrolidinecarbonitrile, 1-[2-[(3-hydroxytricyclo[3.3.1.13, 7]dec-1-yl)amino]acetyl]-, (2S)-

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S3033-10-datasheet.pdf

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