Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEELX-02disulfateCat.No.:HY-114231BCASNo.:2244622-33-9Synonyms:NB-124disulfate分?式:C??H??N?O??S?分?量:678.68作?靶點(diǎn):Others作?通路:Others儲(chǔ)存?式:-20°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性數(shù)據(jù)體外實(shí)驗(yàn)H2O:100mg/mL(147.34mM;Needultrasonic)DMSO:<1mg/mL(insolubleorslightlysoluble)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM1.4734mL7.3672mL14.7345mL5mM0.2947mL1.4734mL2.9469mL10mM0.1473mL0.7367mL1.4734mL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(chǔ)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(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month(storedundernitrogen)。-80°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的?式助溶)1.請依序添加每種溶劑：PBS1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:100mg/mL(147.34mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性ELX-02disulfate(NB-124disulfate)?種?創(chuàng)的的合成的真核核糖體特異性糖苷(ERSG)，可?于研究?義突變引起的遺傳疾病[1]。體外研究ELX-02(100-400μg/mL)isnottoxic,andpermitsread-throughofnonsensemutationsinhumancells[1].CellCytotoxicityAssay[1]CellLine:Wildtypehumanproximaltubulecells(HK-2)Concentration:0,100and400μg/mLIncubationTime:0,24,48and72hoursResult:Cytotoxicityassayinwildtypehumanproximaltubulecells(HK-2)showingnotoxiceffectof400μg/mLat0,24,48and72h.體內(nèi)研究ELX-02(10and30mg/kg;repeatsubcutaneousadministration;twiceweekly,totalof8doses)showsaccumulationintissuesthatisdosedependentwithoutgenderdifference[1].InplasmaELX-02israpidlyabsorbedwithaTmaxof0.25hafterbothsingle(asinglesubcutaneousinjectionat10mg/kgatdosevolumeof5mL/kg)andrepeatedadministration(twiceweeklywith10mg/kg/dosefor21days;totalof7administrations).ELX-02israpidlyeliminatedfromplasmainabiphasicmannerwiththeterminalhalf-life(T1/2)of0.5h[1].InaCtnsY226Xnonsensemutantmouse,subcutaneousELX-02accumulatesinkidneytissuewithoutovertrenaltoxicityandthatELX-02(10mg/kgX2/weekfor3weeks)reducesrenalcystineaccumulationinvivo[1].AnimalModel:Twenty-nineCtnsY226X/Y226Xmice5-7monthold[1]Dosage:10and30mg/kgAdministration:Subcutaneousinjection,atdosevolumeof5mL/kg,twiceweeklyforaperiodof28days(totalof8doses)Result:Highestlevelsweremeasuredinthekidney,followedbyspleenandliver,withlowerlevelsinothertissues(lung,heart,cochleaandbrain).REFERENCES[1].LeubitzA,etal.Safety,Tolerability,andPharmacokineticsofSingleAscendingDosesofELX-02,aPotentialTreatmentforGeneticDisordersCausedbyNonsenseMutations,inHealthyVolunteers.ClinPharmacolDrugDev.2019Jan16.McePdfHeight2/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemECaution:Producthasnotbeenfullyvalidatedfor