Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETJ-M2010-5Cat.No.:HY-139397CASNo.:1357471-57-8分?式:C??H??N?OS分?量:406.54作?靶點(diǎn):MyD88作?通路:Immunology/Inflammation儲存?式:4°C,protectfromlight,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light,storedundernitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(245.98mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.4598mL12.2989mL24.5978mL5mM0.4920mL2.4598mL4.9196mL10mM0.2460mL1.2299mL2.4598mL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(protectfromlight,storedundernitrogen)。-80°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲存時(shí)，請?jiān)?個(gè)?內(nèi)使?。BIOLOGICALACTIVITY?物活性TJ-M2010-5?種MyD88抑制劑，可與MyD88的TIR結(jié)構(gòu)域結(jié)合以?擾其同?聚化和TLR/MyD88信號通路[1][2]。TJ-M2010-5可?于?肌缺?/再灌注損傷（MIRI）的研究[2]。體外研究TJ-M2010-5(40μM)inhibitsMyD88homodimerizationintransfectedHEK293cellsinaconcentration-dependentmannerandsuppressesMyD88signalinginLPS(100ng/mL)-responsiveRAW264.7cellsinvitro[1].1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemETJ-M2010-5(5-30μM)preventsBcellproliferationandinducesBcellsapoptosisafterstimulationwithR848(500ng/mL)[3].CellViabilityAssay[3]CellLine:PurifiedBcellsConcentration:0μM,5μM,10μM,20μMand30μMIncubationTime:48hoursResult:InhibitedtheviabilityofBcellswithorwithoutthestimulationofCD40L.體內(nèi)研究TJ-M2010-5treatmentstatisticallysignificantlyreducesAOM/DSS-inducedcolitisandcompletelypreventedCACdevelopmentwithlessrelatedbodymassloss,resultsin0%mortalityoftreatedmice,decreasescellproliferation,andincreasedapoptosisincolontissueina10-weekCACmousemodel[1].TJ-M2010-5statisticallysignificantlydecreasesTNF-α,IL-6,G-CSF,MIP-1β,IL-11,IL-17A,IL-22,andIL-23serumconcentrationsinmiceatbothtwoandsevenweekspostinduction,aswellasTGF-β1serumlevelsatsevenweekspostinduction[1].AnimalModel:FemaleBalB/cmice(6–8weeksold)[1]Dosage:50mg/kgAdministration:Treatedi.p.dailybeginningtwodaysbeforethefirstdextransodiumsulfate(DSS)administrationthroughouta10-weekobservationperiod.Result:Significantlypreventedinflammation/CAC-relatedbodyweightlossandmortality(0%vs53%inthecontrolgroup).REFERENCES[1].LinXie,etal.TargetingofMyD88HomodimerizationbyNovelSyntheticInhibitorTJ-M2010-5inPreventingColitis-AssociatedColorectalCancer.JNatlCancerInst.2015Dec28;108(4):djv364.[2].YanMiao,etal.InhibitionofMyD88byanovelinhibitorreversestwo-thirdsoftheinfarctareainmyocardialischemiaandreperfusioninjury.AmJTranslRes.2020Sep15;12(9):5151-5169.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapp