P-gp-inhibitor-1-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemEP-gpinhibitor1Cat.No.:HY-101791CASNo.:2050747-49-2分⼦式:C₃₂H₃₁N₅O₂分⼦量:517.62作⽤靶点:P-glycoprotein作⽤通路:MembraneTransporter/IonChannel储存⽅式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性数据体外实验DMSO:16.67mg/mL(32.21mM;ultrasonicandwarmingandheatto70°C)MassSolvent1mg5mg10mgConcentration制备储备液1mM1.9319mL9.6596mL19.3192mL5mM0.3864mL1.9319mL3.8638mL10mM0.1932mL0.9660mL1.9319mL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(protectfromlight)。-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。BIOLOGICALACTIVITY⽣物活性P-gpinhibitor1⼀种新型的可逆转P-糖蛋⽩介导的多药耐药性抑制剂。IC50&TargetP-glycoprotein[1]体外研究P-gpinhibitor1(12k)possesseshighpotency(EC50=57.9±3.5nM),lowcytotoxicity,andlongdurationofactivityinreversingdoxorubicin(DOX)resistanceinK562/A02cells(1μM,80minutes)[1].1/2MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEP-gpinhibitor1alsobooststhepotencyofotherMDR-relatedcytotoxicagentswithdifferentstructures,increasesaccumulationofDOX,blocksPgp-mediatedRh123efflux,andsuppressesP-gpATPaseactivityinK562/A02MDRcells(0.1,1,5μM,1hour)[1].WesternBlotAnalysis[1]CellLine:K562/A02cellConcentration:0.1,0.5,or2.0μMIncubationTime:72hoursResult:MDRreversalby12kwasnotcausedbyadecreasedproteinexpressionbutinsteadmostlikelyduetodirectinhibitionofP-gpefflux[1].REFERENCES[1].QiuQ,etal.Design,Synthesis,andPharmacologicalCharacterizationofN-(4-(2(6,7-Dimethoxy-3,4-dihydroisoquinolin-2(1H)yl)ethyl)phenyl)quinazolin-4-amineDerivatives:NovelInhibitorsReversingP-Glycoprotein-MediatedMultidrugResistance.JMedChemMcePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-820-3