Zofenopril-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEZofenoprilCat.No.:HY-108321CASNo.:81872-10-8分?式:C??H??NO?S?分?量:429.55作?靶點(diǎn):Angiotensin-convertingEnzyme(ACE)作?通路:MetabolicEnzyme/Protease儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:5mg/mL(11.64mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.3280mL11.6401mL23.2802mL5mM0.4656mL2.3280mL4.6560mL10mM0.2328mL1.1640mL2.3280mL請(qǐng)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(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。BIOLOGICALACTIVITY?物活性Zofenopril?個(gè)angiotensin-convertingenzyme(ACE)抑制劑，其IC50值為81μM。IC50&TargetIC50:81μM(ACE)[1]體外研究KineticanalysesdemonstratethatenalaprilinhibitstheuptakeofGlySarinacompetitivemanner(Ki1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEapproximately6mM).FosinoprilandZofenoprilhavethegreatestinhibitorypotency(IC50valuesof55and81μM,respectively)whiletheotherACEinhibitorsexhibitlow-affinityinteractionswiththerenalpeptidetransporter[1].體內(nèi)研究Zofenopril,asulphydryliccompound,atdoseshigherthan70mg/ducessignificantprotection(i.e.at70mg/kg,P=0.044,F=2.17,d.f.=18;athigherconcentrationP50valuesagainstclonusofsomeAEDswiththeexceptionsofdiazepam,felbamate,phenobarbitalandphenytoincomparewithconcurrentgroups,suggestinganincreaseinanticonvulsantactivity[2].PROTOCOLCellAssay[1]StudiesareperformedinrabbitrenalbrushbordermembranevesiclesinwhichtheuptakeofradiolabeledGlySarisexaminedintheabsenceandpresenceofcaptopril,enalapril,enalaprilat,fosinopril,lisinopril,quinapril,quinaprilat,ramiprilandZofenopril[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMaleandfemalemiceweighing8to12g(22to26daysold)or20to28g(48to56daysold)areused.MiceAdministration[2]areexposedtoauditorystimulation,45,60or120minfollowingintraperitoneal(i.p.)administrationofACEinhibitors(includingZofenopril)(10to100mg/kg)orvehicleand45minfollowingi.p.injectionoftheAEDsstudied.AllACEinhibitorsaresuspendedina1%solutionofTween80beforeadministration[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.REFERENCES[1].LinCJ,etal.Competitiveinhibitionofglycylsarcosinetransportbyenalaprilinrabbitrenalbrushbordermembranevesicles:interactionofACEinhibitorswithhigh-affinityH+/peptidesymporter.PharmRes.1999May;16(5):609-15.[2].SarroGD,etal.Fosinoprilandzofenopril,twoangiotensin-convertingenzyme(ACE)inhibitors,potentiatetheanticonvulsantactivityofantiepilepticdrugsagainstaudiogenicseizuresinDBA/2mice.PharmacolRes.2012Mar;65(3):285-96.McePdfHeightCaution:Producthasnotbeenfullyvalidatedform