Perphenazine-dihydrochloride-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEPerphenazinedihydrochlorideCat.No.:HY-A0077ACASNo.:2015-28-3分⼦式:C₂₁H₂₈Cl₃N₃OS分⼦量:476.89作⽤靶点:DopamineReceptor;HistamineReceptor;5-HTReceptor;AdrenergicReceptor;Apoptosis;Autophagy作⽤通路:GPCR/GProtein;NeuronalSignaling;Immunology/Inflammation;Apoptosis;Autophagy储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性Perphenazinedihydrochloride⼀种具有⼝服活性的多巴胺受体(dopaminereceptor)和组胺-1受体(histamine-1receptor)拮抗剂,Ki值分别为0.56nM(D2)、0.43nM(D3)、0.6nM(5-HT2A)。Perphenazinedihydrochloride还可与Alpha-1A肾上腺素受体(Alpha-1Aadrenergicreceptor)结合。Perphenazinedihydrochloride抑制癌细胞增殖，并诱导细胞凋亡(apoptosis)。Perphenazinedihydrochloride可⽤于精神疾病、癌症、炎症的研究。IC50&TargetD2ReceptorD3ReceptorD4Receptor5-HT2AReceptor0.56nM(Ki)0.43nM(Ki)28.5nM(Ki)5.6nM(Ki)5-HT6Receptor5-HT7Receptor5-HT2CReceptor5-HT1AReceptor17nM(Ki)23nM(Ki)132nM(Ki)421nM(Ki)体外研究Perphenazine(40μM,48h)dihydrochlorideinhibitscellviability,andinducescellapoptosismediatedbyCTSD(CathepsinD)inL02cells[2].Perphenazine(30μM,24h)dihydrochlorideinducesintenselysosomevacuolation,impairedlysosomalmembrane,andinduceslysosomalmembranepermeabilization(LMP),ultimatelytriggeringlysosomalcelldeathinL02cells[2].Perphenazine(10-40μM,24h)dihydrochlorideinhibitsautophagicfluxinL02cells[2].Perphenazine(1µM,24h)dihydrochloridedecreasesglioblastomaU-87MGcellmigrationandinvasion[4].CellViabilityAssay[2]1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemECellLine:L02cellsConcentration:10-100μMIncubationTime:12,24,48hResult:Inhibitedcellviabilityinaconcentrationandtime-dependentmanner.WesternBlotAnalysis[2]CellLine:L02cellsConcentration:10,20,30,and40μMIncubationTime:24hResult:IncreasedLC3I/IIandP62/SQSTM1levelsCellMigrationAssay[4]CellLine:U-87MGcellsConcentration:0,3,6,9,12,and24hIncubationTime:0,3,6,9,12,and24hResult:Increasedthewoundclosureinhumanglioblastomacellculturesfrom24.6to62.7%.体内研究Perphenazine(oralgavage,180mg/kg,everyotherdayfor21days)dihydrochlorideinducesliverinjuryandlysosomalmembranedamageinICRmice[2].Perphenazine(oraladministration,10mg/kg,everyotherdayfor6days)dihydrochlorideattenuatesmorphologicalphenotypeinmousemodelsofTh2-typeallergicdermatitis[3].AnimalModel:ICRmice[2]Dosage:10,30,60,120,180mg/kgAdministration:Oralgavage,everyotherdayfor21days.Result:Increasedhistologicalinjuryandaminotransferasescomparedwithcontrol.AnimalModel:Oxazolone-treatedanimalmodelofdermatitis[3]Dosage:10mg/kgAdministration:Oraladministration,everyotherdayfor6daysResult:DecreasedThelevelsofmiceearswelling.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE户使⽤本产品发表的科研⽂献•ToxicolLett.29July2022.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].RichtandNM,etal.Dopamineandserotoninreceptorbindingandantipsychoticefficacy.Neuropsychopharmacology.2007Aug;32(8):1715-26.[2].LeiTao,etal.Lysosomalmembranepermeabilizationmediatedapoptosisinvolveinperphenazine-inducedhepatotoxicityinvitroandinvivo.ToxicolLett.2022Jul29;367:76-87.[3].Min-JeongHeo,etal.PerphenazineAttenuatesthePro-InflammatoryResponsesinMouseModelsofTh2-TypeAllergicDermatitis.IntJMolSci.2020May3;21(9):3241.[4].MichałOtręba,etal.PerphenazineandprochlorperazinedecreaseglioblastomaU-87MGcellmigrationandinvasion:AnalysisoftheABCB1andABCG2transporters,E-cadherin,α-tubulinandintegrins(α3,α5,andβ1)levels.OncolLett.2022Jun;23(6):182.[5].MichałOtręba,etal.nvitroanticanceractivityoffluphenazine,perphenazineandprochlorperazine.Areview.JApplToxicol.2021Jan;41(1):82-94.McePdfHeight