Enoximone-DataSheet-生命科學試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?Agonists?ScreeningLibrarieswww.MedChemEEnoximoneCat.No.:HY-B1639CASNo.:77671-31-9分?式:C??H??N?O?S分?量:248.3作?靶點:Phosphodiesterase(PDE)作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:8.33mg/mL(33.55mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM4.0274mL20.1369mL40.2739mL5mM0.8055mL4.0274mL8.0548mL10mM0.4027mL2.0137mL4.0274mL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，并請注意儲備液的保存?式和期限。BIOLOGICALACTIVITY?物活性Enoximone?種正性肌??管舒張劑，也?種選擇性的，具有?服活性的磷酸?酯酶III(PDE3)抑制劑，IC50為5.9μM。Enoximone通過抑制cGMP抑制的PDE來誘導?管舒張并增加細胞內(nèi)cAMP?平。Enoximone還表現(xiàn)出PDE4抑制作?，對?肌PDE4A的IC50為21.1μM。Enoximone可?于充?性??衰竭的研究，并具有??管擴張，抗哮喘和抗炎作?。IC50&TargetPDE3/PDEⅢPDE4A5.9μM(IC50)21.1μM(IC50,myocardialPDE4A)1/2MasterofSmallMolecules—您?邊的抑制劑?師www.MedChemE體外研究Invitro,10μMEnoximone-treatedbronchoalveolarlavage(BAL)eosinophilsinducedbyIL-33treatmentshowssignificantlylowerCD11bexpressionwhencomparedwithdiluent-treatedBALeosinophils[1].體內(nèi)研究TopicalEnoximone(25μg;intratrachealroute)abrogateshousedustmite(HDM)-inducedallergicairwayinflammation[1].TheEnoximone-treated(25μg;for5days)HDM-exposedmiceshowssignificantreductionsininflammatorycellnumbersincludingeosinophils,macrophages,neutrophils,ILC2s,andTcells,indicatingthatEnoximonetreatmentreducesairwayinflammation[1].REFERENCES[1].JanBeute,etal.APathophysiologicalRoleofPDE3inAllergicAirwayInflammation.JCIInsight.2018Jan25;3(2):e94888.[2].RCDage,etal.PharmacologyandPharmacokineticsofEnoximone.Cardiology.1990;77Suppl3:2-13;discussion27-33.[3].MBVroom,etal.EffectofPhosphodiesteraseInhibitorsonHumanArteriesinVitro.BrJAnaesth.1996Jan;76(1):122-9.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400