Procaterol-DataSheet-生命科学试剂-MCE

Hotline:400-820-3792Inhibitors • ScreeningLibraries • Proteinswww.MedChemEProcaterolCat.No.:HY-114732CASNo.:72332-33-3分子式:C₁₆H₂₂N₂O₃分子量:290.36作用靶点:AdrenergicReceptor作用通路:GPCR/GProtein;NeuronalSignaling储存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Procaterol是一种可口服的选择性β2adrenergicreceptor激动剂。Procaterol可通过环磷酸腺苷依赖性机制直接抑制嗜酸性粒细胞迁移和BEAS-2B细胞释放嗜酸性粒细胞趋化活性因子。Procaterol对大鼠的支气管扩张作用和代谢作用存在较大的剂量差，可用于运动员哮喘研究[1]。IC50&Targetβ2adrenoceptor体外研究Procaterol(10-1000ng/mL,12,24,48h,BEAS-2B)directlyinhibitseosinophilmigrationandthereleaseofeosinophilchemotacticfactorfromBEAS-2BcellsthroughacyclicAMP-dependentmechanism[3].Procaterol(10-1000ng/mL,12,24,48h,BEAS-2B)Dose-dependentinhibitionofRANTESreleaseinresponsetoIL-1bandTNF-ainBEAS-2Bcellmonolayers,andenhancementofGM-CSFmRNAexpressioninresponsetoIL-1b[3].Procaterol(0.1μM,72h,Humantrachealsurfaceepithelialcells)reducerhinovirustitersandRNA,cytokineconcentrations,susceptibilitytorhinovirusinfection,andtheexpressionofintercellularadhesionmolecule-1(ICAM-1),thereceptorfortype14rhinovirus,andthenumberofacidicendosomesinthecellsfromwhichrhinovirusRNAentersintothecytoplasm[4].Procaterol(10nM,onetime,Lungepithelialcells)increasedciliarybendamplitude(CBA)andciliarybeatingfrequency(CBF)inadosedependentmannerviacAMP[5].CellMigrationAssay[3]CellLine:eosinophilConcentration:10,100,1000ng/mL1/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEIncubationTime:24hResult:Attenuatedtheeosinophilmigratoryresponseinadose-dependent.体内研究Procaterol(0.03-1mg/kg,inhalation3timesaday,14days)hasnosignificantchangesinweightorbodyweightgaininratgastrocnemiusmuscle[1].Procaterol(1mg/kg,inhalation3timesaday,14days)significantlyincreasesweightofthelevatoranimusclewithanaboliceffects[1].Procaterol(1mg/kg,inhalation3timesaday,14days)increasesventralprostateweightisassociatedwithdrugstimulationofb2adrenergicreceptorsintissues[1].Procaterol(0.03-1mg/kg,inhalation3timesaday,14days)differentdosebetweenbronchodilatorandanaboliceffects>30-fold,[1].Procaterol(0.1,1,10mg/kg,orally,beforeovalbumin(HY-W250978)(OVA)inhalation)inhalerdoesnotenhanceairwayhyperresponsiveness,airwaywallinflammation,orairwaywallthickening,anddecreaseseosinophilnumber[2].AnimalModel:Six-week-oldratswerecastratedonDay–5,exceptforanormalgroupof6rats[1]Dosage:0.03,0.1,0.3,1mg/mLAdministration:in-halation3timesaday(09:00,12:00,16:00)for14daysfromDay0toDay13.Result:Nosignificantchangedinweightorbodyweightgaininratgastrocnemiusmuscle.Significantlyincreasedtheweightofthelevatoranimuscle.Increasdinventralprostateweight.AnimalModel:Miceimmunizedwithovalbumin(HY-W250978)(OVA,inhalationof20mg/mLOVAfor10minuteseveryotherday,total7times)+alum[2]Dosage:0.1,1,10mg/kgAdministration:orally,beforeovalbumin(HY-W250978)(OVA)inhalationResult:Inhalationdidnotenhanceairwayhyperresponsiveness,airwaywallinflammation,orairwaywallthickeningafterOVAinhalation.ReducedthenumberofeosinophilsinBALFmice.REFERENCESIkezonoK,etal.Bronchodilatingeffectandanaboliceffectofinhaledprocaterol.IntJSportsMed.2008Nov;29(11):888-94.TashimoH,etal.Effectofprocaterol,abeta(2)selectiveadrenergicreceptoragonist,onairwayinflammationandhyperresponsiveness.AllergolInt.2007Sep;56(3):241-7.KoyamaS,etal.ProcaterolinhibitsIL-1beta-andTNF-alpha-mediatedepithelialcelleosinophilchemotacticactivity.EurRespirJ.19992/3 MasterofBioactiveMolecules—您身边的抑制剂大师www.MedChemEOct;14(4):767-75.YamayaM,etal.Procaterolinhibitsrhinovirusinfectioninprimaryculturesofhumantrachealepithelialcells.EurJPharmacol.2011Jan10;650(1):431-44.Komatani-TamiyaN,etal.Procaterol-stimulatedincreasesinciliarybendamplitudeandciliarybeatfrequencyinmousebronchioles.CellPhysiolBiochem.2012;29(3-4):511-22.M