Diclofenac-potassium-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEDiclofenacpotassiumCat.No.:HY-15038CASNo.:15307-81-0分?式:C??H??Cl?KNO?分?量:334.24作?靶點(diǎn):COX;Apoptosis作?通路:Immunology/Inflammation;Apoptosis儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1monthBIOLOGICALACTIVITY?物活性Diclofenacpotassium?種有效的，?選擇性抗炎劑，為COX的抑制劑，在CHO細(xì)胞中，對?COX-1和COX-2的IC50值分別為4和1.3nM[1]。Diclofenacpotassium對綿?COX-1和COX-2的IC50值分別為5.1μM，0.84μM[2]。Diclofenacpotassium通過活化caspase級聯(lián)反應(yīng)來誘導(dǎo)神經(jīng)?細(xì)胞凋亡(apoptosis)[3]。IC50&TargetHumanCOX-2HumanCOX-1OvineCOX-2OvineCOX-11.3nM(IC50,inCHO4nM(IC50,inCHO0.84nM(IC50)5.1nM(IC50)cells)cells)體外研究DiclofenaceffectivelyblocksCOX-1mediatedprostanoidproductionfromU937cellmicrosomes,withanIC50of7±3nM[1].Diclofenac(1-60μM;1day)inducesneuralstemcells(NSCs)deathinaconcentration-dependentmanner[3].Diclofenac(10-60μM;6hours)increasestheexpressionofcleaved(activated)caspase-3[3].CellViabilityAssay[3]CellLine:Neuralstemcells(NSCs)Concentration:1,3,10,30,60μM1/3MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemEIncubationTime:1dayResult:Inductionofcelldeathwasconcentration-dependentandtheeffectwasnotsaturatedataconcentrationofupto60μM.WesternBlotAnalysis[3]CellLine:Neuralstemcells(NSCs)Concentration:10,30or60μMIncubationTime:6hoursResult:Theactivationofcaspase-3wasincreasedinaconcentration-dependentmanner.體內(nèi)研究Diclofenac(3mg/kg,b.i.d.,for5days)significantlyincreasesfaecal51Crexcretioninrats,andsucheffectisalsoobservedinsquirrelmonkeysafteradministratedof1mg/kgtwicedailyfor4days[1].Diclofenac(10mg/kg;administeredviaoralroutejustpriortoinductionofinflammation)showsinvivoanti-inflammatoryactivityinWistarrats[1].AnimalModel:MaleSprague-Dawleyrats(150±200g)[1]Dosage:3mg/kgAdministration:Oraladministration,b.i.d.,for5daysResult:Resultedinasignificantincreaseinfaecal51Crexcretion.AnimalModel:Wistarrats(150-175g)bearingFormalin-inducedratfootpawedemamodel[2]Dosage:10mg/kgAdministration:AdministeredviaoralroutejustpriortoinductionofinflammationResult:Showedinvivoanti-inflammatoryactivity(%edemainhibition=29.2,1h;22.2,3h;20,6h).?JHazardMater.2015May30;289:18-27.?Chemosphere.2019Jun;225:378-387.?JPhysChemSolids.2017October;109:117-123.?PhysChemChemPhys.2016Jan21;18(3):1526-36.?ToxicolMechMethods.2019Jul25:1-24.2/3MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemESeemorecustomervalidationsonwww.MedChemEREFERENCES[1].ChihoKudo,etal.DiclofenacInhibitsProliferationandDifferentiationofNeuralStemCells.BiochemPharmacol.2003Jul15;66(2):289-95.[2].RiendeauD,etal.BiochemicalandpharmacologicalprofileofatetrasubstitutedfuranoneasahighlyselectiveCOX-2inhibitor.BrJPharmacol.1997May;121(1):105-17.[3].LabibMB,etal.Design,synthesisofnovelisoindolinehybridsasCOX-2inhibitors:Anti-inflammatory,analgesicactivitiesanddockingstudy.BioorgChem.2018Oct;80:70-80.McePdfHeightCaution:Producthasnotbeenfully