Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEBisoprololfumarateCat.No.:HY-120829CASNo.:105878-43-1分?式:C??H??NO?分?量:441.52作?靶點:AdrenergicReceptor作?通路:GPCR/GProtein;NeuronalSignaling儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Bisoprololfumarate?種有效的、選擇性的、具有?服活性的β1腎上腺素受體(β1-adrenergicreceptor)阻滯劑，對β2受體的活性很?。Bisoprololfumarate可?于??壓，冠狀動脈疾病和穩(wěn)定的?室功能障礙的研究。IC50&TargetBeta-1adrenergicreceptor體外研究Bisoprololfumarate(2μM,1h)protectsmyocardialcells(H9c2)fromischemia/reperfusion(I/R)injury[2].Bisoprololfumarate(2μM,1h)reducestheH/R-inducedROSproductionandapoptosisinH9c2cells[2].Bisoprololfumarate(2μM,1h)increasesAKTandGSK3βphosphorylationinH9c2cells[2].Bisoprololfumarate(100μM,24h)reversesEpinephrine-inhibitedemigrationincholesterol-loadedDCs(dendriticcell)throughincreasinginβ-arrestin2,CCR7andPI3Kphosphorylation[3].CellViabilityAssay[2]CellLine:H9c2cellsConcentration:0.2,2,20μMIncubationTime:1hResult:ElevatedthesurvivalratesofcardiomyocytessubjectedtoH/R(hypoxia/reoxygenation)to73.20%,90.38%,81.25%respectively.CellMigrationAssay[3]1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECellLine:DCsConcentration:100μMIncubationTime:6,12,24hResult:Increasedtheamountofmigratingcellsby46.00%(6h),64.25%(12h)and55.74%(24h).體內(nèi)研究Bisoprololfumarate(oraladministration,5mg/kg,for1week)increasesleftventricularejectionfraction(LVEF)anddecreasestheheartratevalue[2].Bisoprololfumarate(oralgavage,8mg/kg,dailyforfourweeks)showsprotectiveeffectsagainstCadmium-inducedmyocardialtoxicityinrats[4].Bisoprololfumarate(oralgavage,1mg/kg,dailyfor6weeks)reversessmallconductancecalcium-activatedpotassiumchannel(SK)remodelinginavolume-overloadratmodel[5].AnimalModel:Ischemia/reperfusion(I/R)injuryrats[2]Dosage:0.5,5,10mg/kgAdministration:Oraladministration,for1week,priorto0.5hischemia/4hreperfusion.Result:Reducedinfarctsizefrom44%inI/Rgroupto31%intreatedgroup.AnimalModel:Cadmium-inducedrats[4]Dosage:2,8mg/kgAdministration:Oralgavage,dailyforfourweeks.Result:Decreasedmeanarterialpressure(MAP)at8mg/kg.Decreasedserumbiomarkers(ALT,AST)andNF-kBp65expressionandTNF-αlevels(cardiactissuesamples)at8mg/kg.戶使?本產(chǎn)品發(fā)表的科研?獻?MolNeurobiol.2019Jan;56(1):367-377.?ACSOmega.August8,2022.?JPharmaceutBiomed.2020,113870.Seemorecustomervalidationsonwww.MedChemEREFERENCES2/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE[1].JillianGBaker,etal.Theselectivityofbeta-adrenoceptorantagonistsatthehumanbeta1,beta2andbeta3adrenoceptors.BrJPharmacol.2005Feb;144(3):317-22.[2].JingWang,etal.Bisoprolol,aβ1antagonist,protectsmyocardialcellsfromischemia-reperfusioninjuryviaPI3K/AKT/GSK3βpathway.FundamClinPharmacol.2020Dec;34(6):708-720.[3].HongYang,etal.Bisoprololreversesepinephrine-mediatedinhibitionofcellemigrationthroughincreasesintheexpressionofβ-arrestin2andCCR7andPI3Kphosphorylation,indendriticcellsloadedwithcholesterol.ThrombRes.2013Mar;131(3):230-7.[4].JinhuaLiu,etal.ProtectiveEffectsofBisoprololAgainstCadmium-inducedMyocardialToxicityThroughInhibitionofOxidativeStressandNF-κΒSignallinginRats.JVetRes.2021Oct20;65(4):505-511.[5].YajuanNi,etal.Bisoprololreversedsmallconductancecalcium-activatedpotassiumchannel(SK)remodelinginavolume-overloadratmodel.MolCellBiochem.2013Dec;384(1-2):95-103.McePdfHeightCaution:Pro