Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEDMU2105Cat.No.:HY-101284CASNo.:1821143-79-6分?式:C??H??NO分?量:259.3作?靶點(diǎn):CytochromeP450作?通路:MetabolicEnzyme/Protease儲(chǔ)存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:33.33mg/mL(128.54mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM3.8565mL19.2827mL38.5654mL5mM0.7713mL3.8565mL7.7131mL10mM0.3857mL1.9283mL3.8565mL請(qǐng)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(qǐng)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。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)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(qǐng)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(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:2.67mg/mL(10.30mM);Suspendedsolution;Needultrasonic1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥3.33mg/mL(12.84mM);ClearsolutionBIOLOGICALACTIVITY?物活性DMU2105有效的特異性細(xì)胞?素P4501B1(CYP1B1)的抑制劑，其對(duì)CYP1B1和CYP1A1的IC50值分別為10nM和742nM。IC50&TargetCYP1B1CYP1A110nM(IC50)742nM(IC50)體外研究DMU2105(Compound7k)shows74and120-foldselectivityforCYP1B1overCYP1A1andCYP1A2.InthepresenceofDMU2105however,theEC50goesdownto1μMindicatingthatthecellshavesufferedfromtoxicitywhichmayhavebeenmediatedbyCYP1B1inhibition.Un-transfectedcells(HEK293:pcDNA3.1),whentreatedwithcisplatinandDMU2105(10×IC50)donotshowanyperceptibledecreaseofcisplatinEC50(8.5μM±0.9)[1].REFERENCES[1].HorleyNJ,etal.DiscoveryandcharacterizationofnovelCYP1B1inhibitorsbasedonheterocyclicchalcones:OvercomingcisplatinresistanceinCYP1B1-overexpressinglines.EurJMedChem.2017Mar31;129:159-174.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.Tel:400-