Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEER-000444793Cat.No.:HY-100852CASNo.:792957-74-5分?式:C??H??N?O?分?量:354.4作?靶點:MitochondrialMetabolism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:50mg/mL(141.08mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.8217mL14.1084mL28.2167mL5mM0.5643mL2.8217mL5.6433mL10mM0.2822mL1.4108mL2.8217mL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(fù)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ER-000444793有效的線粒體通透性轉(zhuǎn)換孔(mPTP)開放抑制劑。ER-000444793抑制mPTP，IC50為2.8μM。IC50&TargetIC50:2.8?μM(mPTP)[1]1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE體外研究ER-000444793isasmallmolecule,non-toxicmPTPinhibitorwithamechanismofactionindependentofCypDinhibition.ER-000444793potentlyanddose-dependentlyinhibitsCa2+-inducedmPT.ER-000444793bindsCypD,aCsA/CypDhomogenoustime-resolvedfluorescence(HTRF)assayisusedtostudycompoundbinding.BothCsAandSfAdose-dependentlydecreaseHTRFsignal,suggestingdisplacementoflabelledCsAfromrhCypDprotein(CsAIC50=23?nMandSfAIC50=?5?nM).Incontrast,ER-000444793hasnoeffectuptoaconcentrationof50?μM,indicatinglackofdisplacementoflabelled-CsAfromrhCypDprotein.Together,thesedatasuggestthemechanismofER-000444793indelayingmPTisindependentofCypDfunctionalinhibition[1].PROTOCOLCellAssay[1]NFAT-RE-luc2Jurkatcellsarecollected,centrifugedat300?gfor5?minutesandre-suspendedinserum-freeRPMI-1640media,plussupplementswithoutantibiotic.Cellsuspension(15,000cells/20?μL)isaddedtoeachwellofasolidblack384wellplateandincubatedinthepresenceofcompoundfor20?hoursat37?°C.AlamarBlueisusedandisaddedtoeachwellat2xconcentrationinmediaandreactionallowedtoproceedfor4?hoursat37?°C.Fluorescence(ex.540?nm/em.590?nm)isrecordedusingPherastarFS[1].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.戶使?本產(chǎn)品發(fā)表的科研?獻(xiàn)?Biochemistry.2022Apr19;61(8):639-655.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].BristonT,etal.IdentificationofER-000444793,aCyclophilinD-independentinhibitorofmitochondrialpermeabilitytransition,usingahigh-throughputscreenincryopreservedmitochondria.SciRep.2016Nov25;6:37798.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.F