Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEIpratropiumbromidehydrateCat.No.:HY-B1332CASNo.:66985-17-9Synonyms:Sch1000bromidehydrate分?式:C??H??BrNO?分?量:430.38作?靶點:mAChR作?通路:GPCR/GProtein;NeuronalSignaling儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗H2O:62.5mg/mL(145.22mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.3235mL11.6176mL23.2353mL5mM0.4647mL2.3235mL4.6471mL10mM0.2324mL1.1618mL2.3235mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；?旦配成溶液，請分裝保存，避免反復凍融造成的產(chǎn)品失效。儲備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。BIOLOGICALACTIVITY?物活性Ipratropiumbromide(Sch1000)hydrate毒蕈堿的受體(muscarinicreceptor)的拮抗劑，對M1、M2和M3受體的結(jié)合的IC50值分別為2.9nM、2nM和1.7nM。Ipratropiumbromidehydrate具有放松平滑肌的作?，可?于慢性阻塞性肺病(COPD)和哮喘等研究。1/3MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEIC50&TargetmuscarinicM1receptormuscarinicM2receptormuscarinicM3receptor2.9nM(IC50)2nM(IC50)1.7nM(IC50)體外研究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.體內(nèi)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?邊的抑制劑?師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