Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBromfenacCat.No.:HY-B1888CASNo.:91714-94-2分?式:C??H??BrNO?分?量:334.16作?靶點(diǎn):COX作?通路:Immunology/Inflammation儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Bromfenac?種強(qiáng)效且具有?服活性的COX抑制劑，對COX-1和COX-2的IC50分別為5.56和7.45nM。Bromfenac可?于眼部炎癥研究。IC50&TargetHumanCOX-1HumanCOX-25.56nM(IC50)7.45nM(IC50)體外研究Bromfenac(0-80μg/mL;24h)caninhibittransforminggrowthfactor-β2-inducedepithelial-mesenchymaltransitioninHLEC-B3inaconcentration-dependentmanner[2].Bromfenac(80μg/mL;48h)inhibitstransforminggrowthfactor-β2-inducedepithelial-mesenchymaltransitioninhumananteriorcapsules[2].CellViabilityAssay[2]CellLine:Transforminggrowthfactor-β2-treatedhumananteriorcapsulesConcentration:80μg/mLIncubationTime:48hoursResult:Suppressedtransforminggrowthfactor-β2-inducedepithelial-mesenchymaltransitioninprimarylensepithelialcells(LECs).CellMigrationAssay[2]CellLine:HLEC-B3cells1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEConcentration:0,20,40,60,and80μg/mLIncubationTime:24hoursResult:Suppressedtransforminggrowthfactor-β2-inducedcellmigrationinHLEC-B3cells,andexhibitedinhibitionoftheover-expressionofepithelial-mesenchymaltransitionmarkers.體內(nèi)研究Bromfenac(0.0032-3.16%;100or200μL;rubbedontothebacks)producessignificantanti-inflammatoryactivityatconcentrationsaslowas0.1%(4hpretreatmenttime)or0.32%(18hpretreatmenttime)inrats[3].Bromfenac(0.032-3.16%;100μL;rubbedontothepaws)producesdose-relatedanti-inflammatoryactivityinrats[3].Bromfenac(0.032-1.0%;50μL)is26timesmorepotentthanindomethacininblockingtheerythemawhenapplieddirectlyontotheskinareaexposedtoUVlightinguineapigs[3].Bromfenac(0.0032-0.1%;50μL;rubbedontotheuninjectedpawfor4hperdayand5daysperweek)producesadoseandtimedependentreductioninthepawvolumeofbothhindlimbsinrats[3].Bromfenac(0.32%;50μL;rubbedontotheabdomen)producessignificantblockadeofabdominalconstrictiontoAChchallengeinmice[3].Bromfenac(eyedropinstillation;1μL(0.09%)pereye;twice-daily;4w)partiallyreducescornealstaining,andbecomessomoreslowlybythe4-weektimepoint[4].AnimalModel:MaleSprague-Dawleyrats(150-250g)areinjectedcarrageenan[3]Dosage:0.0032,0.01,0.032,0.1,0.32,1.0,3.16%(100or200μL)Administration:Rubbedontothebacksbefore1-72hofinjectedcarrageenanResult:Producedsignificantanti-inflammatoryactivitywhenapplied1,2,and4hpriortocarrageenanchallengeat0.32%.Applied1or4hpriortocarrageenanchallengewasactive,butnotwhenapplied24h(orlonger)priortochallengeat0.2%.AnimalModel:MaleinjectedwithSalinorBTX-B[4]Dosage:1μL(0.09%)pereyeAdministration:Eyedropinstillation;1μL(0.09%)pereye;twice-daily;4weeksResult:Improvedthecornealfluoresceinstainingscorelaterat4weeksaftertreatment.REFERENCES[1].TetsuoKida,etal.Pharmacokineticsandefficacyoftopicallyappliednonsteroidalanti-inflammatorydrugsinretinochoroidaltissuesinrabbits.PLoSOne.2014May5;9(5):e96481.2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[2].XiaoboZhang,etal.Drug-elutingintraocularlenswithsustainedbromfenacreleaseforconqueringposteriorcapsularopacification.BioactMater.2021Jul23;9:343-357.[3].NolanJC,et,al.Thetopicalanti-inflammatoryandanalgesicpropertiesofbromfenacinrodents.AgentsActions.1988Aug;25(1-2):77-85.[4].KaevalinLekhanont,etal.Effectsoftopicalanti-inflammatoryagentsinabotulinumtoxinB-inducedmousemodelofkeratoconjunctivitissicca.JOculPharmacolTher.2007Feb;23(1):27-34.McePdfHeightCauti