Metoprolol-fumarate-CGP-2175C-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEMetoprololfumarateCat.No.:HY-17503CCASNo.:80274-67-5Synonyms:CGP2175C;LopressorOROS分?式:C??H??N?O??分?量:650.8作?靶點:AdrenergicReceptor;Apoptosis作?通路:GPCR/GProtein;NeuronalSignaling;Apoptosis儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Metoprololfumarate(CGP2175C)?種具有?服活性的、選擇性的β1-腎上腺素受體(β1-adrenoceptor)拮抗劑。Metoprololfumarate具有抗炎、抗腫瘤和抗?管?成的特性。IC50&Targetβ1adrenoceptor體外研究Metoprolol(0-1000μg/mL;24-72h)showscytotoxiceffectonU937andMOLT-4cellsdoseandtimedependently[3].CellCytotoxicityAssay[3]CellLine:U937andMOLT-4cellsConcentration:1,10,50,100,500and1000μg/mLIncubationTime:24,48and72hResult:SignificantlydecreasedtheviabilityofU937andMOLT-4cellsat1000μg/mL(3740.14μM)concentrationafter48hoursincubationtime,significantlyreducedtheviabilityofU937cellsat≥500μg/ml(≥1870.07μM)concentrationsafter72hoursincubationtime,andsignificantlydecreasedtheviabilityofMOLT4cellsat≥100μg/ml(≥374.01μM)concentrationsafter72hoursincubation.體內(nèi)研究Metoprolol(2.5mg/kg/h;infusion;11weeks)reducesproinflammatorycytokinesandatherosclerosisin1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEApoE?/?Mice[1].Metoprolol(15mg/kg/q12h;i.g.;5days)showsanti-inflammationandanti-viruseffectsinmurinemodelwithcoxsackievirusB3-inducedviralmyocarditis[2].Metoprolol(2.5mg/kg;i.v.;3bolusinjections)significantlydecreasedactivatedcaspase-9proteinexpressionandinhibitsmyocardialapoptosisincoronarymicroembolization(CME)rats[4].AnimalModel:MaleApoE?/?mice[1]Dosage:2.5?mg/kg/hAdministration:Viaosmoticminipumps,11weeksResult:Significantlyreducedatheroscleroticplaqueareainthoracicaorta,reducedserumTNFαandthechemokineCXCL1aswellasdecreasingthemacrophagecontentintheplaques.AnimalModel:Balb/cmice,coxsackievirusB3(CVB3)inducedviralmyocarditis(VMC)model[2]Dosage:15mg/kg/q12hAdministration:Oralgavage,5consecutivedaysResult:ReducedpathologicalscoresofVMCinducedbyCVB3infection,protectedthemyocardiumagainstviraldamagebyreducingserumcTn-Ilevels.Decreasedthelevelsofmyocardialpro-inflammatorycytokinesandincreasetheexpressionofanti-inflammatorycytokine.Significantlydecreasedmyocardialvirustiters.戶使?本產(chǎn)品發(fā)表的科研?獻?JPharmacolSci.2020Sep;144(1):30-42.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].UllerydMA,etal.MetoprololreducesproinflammatorycytokinesandatherosclerosisinApoE-/-mice.BiomedResInt.2014;2014:548783.[2].WangD,etal.Carvedilolhasstrongeranti-inflammationandanti-viruseffectsthanmetoprololinmurinemodelwithcoxsackievirusB3-inducedviralmyocarditis.Gene.2014Sep1;547(2):195-201.[3].HajatbeigiB,etal.CytotoxicityofMetoprololonLeukemicCellsinVitro.IJBC2018;10(4):124-129.[4].SuQ,etal.Effectofmetoprololonmyocardialapoptosisandcaspase-9activationaftercoronarymicroembolizationinrats.ExpClinCardiol.2013Spring;18(2):161-5.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfully