P-gp-inhibitor-1-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEP-gpinhibitor1Cat.No.:HY-101791CASNo.:2050747-49-2分?式:C??H??N?O?分?量:517.62作?靶點:P-glycoprotein作?通路:MembraneTransporter/IonChannel儲存?式:4°C,protectfromlight*Insolvent:-80°C,6months;-20°C,1month(protectfrom

light)溶解性數(shù)據(jù)體外實驗DMSO:16.67mg/mL(32.21mM;ultrasonicandwarmingandheatto70°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM1.9319mL9.6596mL19.3192mL5mM0.3864mL1.9319mL3.8638mL10mM0.1932mL0.9660mL1.9319mL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)。-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P-gpinhibitor1?種新型的可逆轉(zhuǎn)P-糖蛋?介導(dǎo)的多藥耐藥性抑制劑。IC50&TargetP-glycoprotein[1]體外研究P-gpinhibitor1(12k)possesseshighpotency(EC50=57.9±3.5nM),lowcytotoxicity,andlongdurationofactivityinreversingdoxorubicin(DOX)resistanceinK562/A02cells(1μM,80minutes)[1].1/2MasterofBioactiveMolecules—您?邊的抑制劑?師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