Ipratropium-bromide-hydrate-Sch-1000-bromide-hydrate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEIpratropiumbromidehydrateCat.No.:HY-B1332CASNo.:66985-17-9Synonyms:Sch1000bromidehydrate分⼦式:C₂₀H₃₂BrNO₄分⼦量:430.38作⽤靶点:mAChR作⽤通路:GPCR/GProtein;NeuronalSignaling储存⽅式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性数据体外实验H2O:62.5mg/mL(145.22mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3235mL11.6176mL23.2353mL5mM0.4647mL2.3235mL4.6471mL10mM0.2324mL1.1618mL2.3235mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。BIOLOGICALACTIVITY⽣物活性Ipratropiumbromide(Sch1000)hydrate毒蕈碱的受体(muscarinicreceptor)的拮抗剂，对M1、M2和M3受体的结合的IC50值分别为2.9nM、2nM和1.7nM。Ipratropiumbromidehydrate具有放松平滑肌的作⽤，可⽤于慢性阻塞性肺病(COPD)和哮喘等研究。1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEIC50&TargetmuscarinicM1receptormuscarinicM2receptormuscarinicM3receptor2.9nM(IC50)2nM(IC50)1.7nM(IC50)体外研究Ipratropiumbromidehydrate(1nM,10nM,100nM;15min)exertsitstoxiceffectsviadisruptionofmitochondrialmembranepotential[1].Ipratropiumbromidehydrate(1nM-1μM;4h)increasesinfarctsizeinisolatedperfusedheartischaemia/reperfusionexperimentswithadose-responsivemanner(EC50=22.7nM)[1].Ipratropiumbromidehydrate(0.001nM-0.1mM;2h)inhibitsadultratcardiacmyocytegrowthafter4hhypoxiatreatment[1].CellViabilityAssay[1]CellLine:AdultRatCardiacMyocyteConcentration:0.001nM-0.1mMIncubationTime:2hindark;priorto4hhypoxiaResult:Resultedcellviabilityinadose-dependentmanner,withtheinhibitionrateof52.7%at0.1mMdose.体内研究Ipratropiumbromidehydrate(1.0μg/kg;i.v.;singledose)enhancesvagalnervestimulationinduingbronchoconstriction[2].Ipratropiumbromidehydrate(0.04mg/20mLand0.20mg/20mL;inhalationfor30min,rate=30mL/30min)canprotectthelungsagainstthecadmium-inducedacuteneutrophilicinflammationbyreducingtheparenchymainflammatoryinfiltrationofneutrophils[4].AnimalModel:Guinea-pigsoftheDunkinHartleystrain[2]Dosage:0.1-1μg/kgAdministration:Intravenousinjection;singledoseResult:Resultedlittleblockingeffectonpost-junctionalmuscarinicreceptorsat0.3μg/kg,andinhibitedACh-inducedbronchoconstrictionat0.5μg/kg.AnimalModel:MaleSprague-Dawleyrats(300-350g)[4]Dosage:0.04mg/20mLand0.20mg/20mLAdministration:Inhalation;atomizationrateof30mL/30min;30minResult:Hadnosignificanteffectsonanyparametersrecordedinhealthyratsbutexertedaprotectiveeffectagainsttheinflammatoryreactionelicitedbycadmium.REFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].FryerAD,etal.Maclagan,Ipratropiumbromidepotentiatesbronchoconstrictioninducedbyvagalnervestimulationintheguinea-pig.EurJPharmacol,1987.139(2):p.187-91.[2].Harvey,etal.Maddock,IpratropiumBromide-MediatedMyocardialInjuryinInVitroModelsofMyocardialIschaemia/Reperfusion.ToxicolSci,2014.[3].MariaPrat,etal.Discoveryofnovelquaternaryammoniumderivativesof(3R)-quinuclidinylamidesaspotentandlongactingmuscarinicantagonists.BioorgMedChemLett.2015Apr15;25(8):1736-1741.[4].WenhuiZhang,etal.Anti-inflammatoryeffectsofformoterolandipratropiumbromideagainstacutecadmium-inducedpulmonaryinflammationinrats.EurJPharmacol.2010Feb25;628(1-3):171-8.[5].VenkatasamyR,etal.NovelrelaxanteffectsofRPL554onguineapigtrachealsmoothmusclecontractility.BrJPharmacol.2016Aug;173(15):2335-51.McePdfHeightCaution:Produ