ELX-02-disulfate-NB-124-disulfate-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEELX-02disulfateCat.No.:HY-114231BCASNo.:2244622-33-9Synonyms:NB-124disulfate分⼦式:C₁₉H₄₂N₄O₁₈S₂分⼦量:678.68作⽤靶点:Others作⽤通路:Others储存⽅式:-20°C,storedundernitrogen*Insolvent:-80°C,6months;-20°C,1month(storedunder

nitrogen)溶解性数据体外实验H2O:100mg/mL(147.34mM;Needultrasonic)DMSO:<1mg/mL(insolubleorslightlysoluble)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.4734mL7.3672mL14.7345mL5mM0.2947mL1.4734mL2.9469mL10mM0.1473mL0.7367mL1.4734mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(storedundernitrogen)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验请根据您的实验动物和给药⽅式选择适当的溶解⽅案。以下溶解⽅案都请先按照InVitro⽅式配制澄的储备液，再依次添加助溶剂：(为保证实验结果的可靠性，澄的储备液可以根据储存条件，适当保存；体内实验的⼯作液，建议您现⽤现配，当天使⽤；以下溶剂前显⽰的百分⽐指该溶剂在您配制终溶液中的体积占⽐；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的⽅式助溶)1.请依序添加每种溶剂：PBS1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemESolubility:100mg/mL(147.34mM);Clearsolution;NeedultrasonicBIOLOGICALACTIVITY⽣物活性ELX-02disulfate(NB-124disulfate)⼀种⾸创的的合成的真核核糖体特异性糖苷(ERSG)，可⽤于研究⽆义突变引起的遗传疾病[1]。体外研究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.体内研究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—您⾝边的抑制剂⼤师www.MedChemECaution:Producthasnotbeenfullyvalidatedfor