Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEAnti-inflammatoryagent47Cat.No.:HY-155568CASNo.:2925288-12-4分子式:C??H??N?O?分子量:394.42作用靶點:ReactiveOxygenSpecies;Apoptosis作用通路:Immunology/Inflammation;MetabolicEnzyme/Protease;NF-κB;Apoptosis儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Flo8是一種強效的抗炎和抗氧化化合物。Flo8能抑制細胞內(nèi)活性氧(ROS)和一氧化氮(NO)的釋放，并通過抑制炎癥和凋亡信號通路來抑制神經(jīng)元凋亡apoptotic，可用于帕金森病(PD)的研究。體外研究CompoundFlo8(5μM,10μM,18h)haslessinhibitoryeffectonBV2cellviability[1].CompoundFlo8(5μM,18h)exhibitssignificantinhibitoryactivityagainstROSandNOproductioninBV2cells[1].CompoundFlo8(5μM,10μM,18h)reducestheapoptosislevelofSH-SY5YcellsbydecreasingtheexpressionofinflammatoryfactorsinBV2cells[1].CompoundFlo8(5μM,10μM,18h)inhibitsLPS-inducedM1polarizationandpromotesM2polarizationinmicroglia[1].CompoundFlo8(5μM,10μM,18h)inhibitsLPS-inducedphosphorylationofERK,p38andJNKinBV2cells[1].CellCytotoxicityAssay[1]CellLine:BV2cellsConcentration:5μM,10μMIncubationTime:18hResult:Exhibitedlowcytotoxicityat5μMconcentrationandshowedminimaltoxicityat10μMforBV2cells.1/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemERealTimeqPCR[1]CellLine:BV2cellsConcentration:5μM,10μMIncubationTime:18hResult:SuppressedLPS-inducedexpressionofM1markersandincreasedthemRNAlevelofCD206,Arg-1,andIL-10inBV2cells.DecreasedthemRNAexpressionlevelsofapoptosis-relatedgenesBAX,Caspase3andCleavedCaspase3butincreasedtheexpressionlevelsofBcl-2inSH-SY5Ycells.WesternBlotAnalysis[1]CellLine:BV2cellsConcentration:5μM,10μMIncubationTime:18hResult:InhibitedphosphorylationofERK,p38andJNKinBV2cells.InhibitedLPS-inducedexpressionofp-IκB-α,p-NF-κBinBV2cells.Decreasedtheproteinexpressionlevelsofapoptosis-relatedgenesBAX,Caspase3andCleavedCaspase3butincreasedtheexpressionlevelsofBcl-2inSH-SY5Ycells.Immunofluorescence[1]CellLine:BV2cellsConcentration:5μM,10μMIncubationTime:18hResult:InhibitedthetranslocationofNF-κBfromthecytoplasmtothenucleusinBV2cells.體內(nèi)研究CompoundFlo8(15and35mg/kgfori.p.,2weeksaday)canslowdownneuroinflammationandinhibitsneuronalapoptosisinthebrainofMPTP-inducedC57BL/6Jmice[1].AnimalModel:MPTPC57BL/6Jmicemodel[1]Dosage:15mg/kg,35mg/kgAdministration:Intraperitonealinjection(i.p.)Result:IncreasedthemRNAexpressionofCD86,TNF-α,IL-6andIL-1βbutdecreasedCD206,Arg-1andIL-10inbraintissue.InhibitedtheexpressionofMPTP-inducedphosphorylationofp38,ERK,JNKandNF-κ2/3 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemEB.ReduceddopaminelevelsinmouseserumintheMPTPgroup.IncreasedtheproteinexpressionofCaspase3andBAXbutdecreasedtheexpressionofBcl2afterMPTPinductioninbraintissue.REFERENCESShenZB,etal.Design,synthesis,andSARstudyofnovelflavone1,2,4-oxadiazolederivativeswithanti-inflammatoryactivitiesforthetreatmentofParkinson'sdisease.EurJMedChem.2023Jul5;255:115417.McePdfHeightCaution:Producthasnotbeenfullyva