EWP-815-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEEWP815Cat.No.:HY-148001CASNo.:20231-01-0分⼦式:C₁₂H₂₂N₄S₄分⼦量:350.59作⽤靶点:Phosphatase;Dopamineβ-hydroxylase作⽤通路:MetabolicEnzyme/Protease储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性EWP815⼀种⼆硫类似物，Ins(1,4)P2磷酸酶和Ins(1,4,5)P35-磷酸酶的有效抑制剂。EWP815也参与抑制体内多巴胺酶β-羟化酶活性。IC50&TargetIns(1,4)P2phosphatase;Ins(1,4,5)P35-phosphatase[1];dopamineβ-hydroxylase[2]体外研究EWP815inhibitsthyrotropin-releasinghormone(TRH;0.03mM)-stimulatedinositolphospholipidbreakdownwithoutaffectingbasalbreakdownratesinprelabelledGH3cellswithIC50sof83mM(solubleenzymes)and71mM(particulateenzymes),respectively[1].EWP815(30μM;1h)exertshigherinhibitiononIns(1,4)P2phosphataseratherthanIns(1,4,5)P35-phosphatasewiththemean[3H]Ins(1,4)P2/mean[3H]InsPrecoveryratioof2.6[1].EWP815(6,8μM;10min)inhibitsdephosphorylationof[3H]Ins(1,4,5)P35-phosphataseinparticulateandsolublefractionswithIC50sof6μMand8μM,respectively[1].EWP815(3-300μM;30min)suppressesthyrotropin-releasinghormone(TRH)-stimulated(100nM)inositolphospholipidproductionby30%(100μM)and1.8%(300μM),respectively,withoutaffectingIns(1,4,5)P3binding[1].体内研究EWP815(50mg/kg;i.p.;30minbeforekilled)inhibitstheenzymedopamineβ-hydroxylaseactivityinmice[2].AnimalModel:Femalemice(20g)[2]Dosage:50mg/kg1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEAdministration:Intraperitonealinjection;30minbeforekilledResult:Intraperitonealinjection;30minbeforekilledInhibitedβ-hydroxylaseof3H-α-methyldopamine.Reducedtheamountof3H-α-Me-NAby12%.REFERENCES[1].FowlerCJ,etal.Inhibitionofinositol1,4,5-trisphosphate5-phosphatasebymicromolarconcentrationsofdisulfiramanditsanalogues.BiochemJ.1993Feb1;289(Pt3)(Pt3):853-9.[2].CarlssonA,etal.Onthebeta-hydroxylationof(+-)-alpha-methyldopamineinvivo.EurJPharmacol.1968Dec;5(1):85-92.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.T