Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEDMU2139Cat.No.:HY-101285CASNo.:1821143-80-9分?式:C??H??NO?分?量:289.33作?靶點:CytochromeP450作?通路:MetabolicEnzyme/Protease儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:77.5mg/mL(267.86mM;Needultrasonic)Ethanol:5mg/mL(17.28mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲備液1mM3.4563mL17.2813mL34.5626mL5mM0.6913mL3.4563mL6.9125mL10mM0.3456mL1.7281mL3.4563mL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。-80°C儲存時，請在6個?內(nèi)使?，-20°C儲存時，請在1個?內(nèi)使?。體內(nèi)實驗請根據(jù)您的實驗動物和給藥?式選擇適當?shù)娜芙?案。以下溶解?案都請先按照InVitro?式配制澄的儲備液，再依次添加助溶劑：(為保證實驗結(jié)果的可靠性，澄的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的?作液，建議您現(xiàn)?現(xiàn)配，當天使?；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：10%DMSO>>40%PEG300>>5%Tween-80>>45%saline1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemESolubility:≥2.58mg/mL(8.92mM);Clearsolution2.請依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥2.58mg/mL(8.92mM);ClearsolutionBIOLOGICALACTIVITY?物活性DMU2139有效的特異性細胞?素P4501B1(CYP1B1)的抑制劑，其對CYP1B1和CYP1A1的IC50值分別為9nM，795nM。IC50&TargetCYP1B1CYP1A19nM(IC50)795nM(IC50)體外研究DMU2139(6j)shows88and133-foldselectivityforCYP1B1overCYP1A1andCYP1A2.InthepresenceofDMU2139,theEC50isreversedbackto8.3μMfrom61μM(seeninCYP1B1-expressingcellswithoutanyinhibitor).TheEC50value,inthepresenceofDMU2139,resemblestheEC50ofcisplatin,8.7μM,incellstransfectedwiththeemptyplasmidwhichhasnoCYP1B1geneandthereforecannotexpressCYP1B1protein[1].REFERENCES[1].HorleyNJ,etal.DiscoveryandcharacterizationofnovelCYP1B1inhibitorsbasedonheterocyclicchalcones:OvercomingcisplatinresistanceinCYP1B1-overexpressinglines.EurJMedChem.2017Mar31;129:159-174.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-8