Etodolac-AY-24236-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEtodolacCat. No.: HY-76251CAS No.: 41340-25-4Synonyms: AY-24236分式: CHNO分量: 287.35作靶点: COX作通路: Immunology/Inflammation储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 100 mg/mL (348.01 mM)H2O

2、 : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (8.70 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (8.70 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (8.70 mM); Clea

3、r solutionBIOLOGICAL ACTIVITY物活性 Etodolac (AY-24236)甾体抗炎化合物，对 COX 的 IC50为53.5 nM。IC50 & Target COX-2 COX-141 nM (IC50, in CHO cells) -50000 nM (IC50, in CHO cells)体外研究 Post-marketing studies demonstrated that etodolac inhibition of cyclooxygenase is somewhat COX-2selective similar to celecoxib and o

4、ther COX-2 inhibitors. Unlike rofecoxib, both etodolac and celecoxib canfully inhibit COX-1 and are designated as having preferential selectivity toward COX-2. The (inactiveagainst COX) r-enantiomer of etodolac inhibits beta-catenin levels in hepatoma cells.REFERENCES1. Riendeau D, et al. Biochemica

5、l and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor. Br JPharmacol. 1997 May;121(1):105-17.2. Ito S, Tajima K, Nogawa M et al. Etodolac, a cyclooxygenase-2 inhibitor, attenuates paclitaxel-induced peripheral neuropathy in a mousemodel of mechanical allo

6、dynia. J Pharmacol Exp Ther. 2012 Jul;342(1):53-60.3. Yanaoka K, Oka M, Yoshimura N et al. Preventive effects of etodolac, a selective cyclooxygenase-2 inhibitor, on cancer development inextensive metaplastic gastritis, a Helicobacter pylori-negative precancerous lesion. Int J Cancer. 2010 Mar 15;12

7、6(6):1467-73.4. Matsuyama M, Yoshimura R, Hase T et al. Administration of the selective cyclooxygenase (COX)-2 inhibitor etodolac prolongs cardiacallograft survival in a mouse model. Mol Med Report. 2010 Sep-Oct;3(5):771-4.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use o