ELQ-300-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEELQ-300Cat.No.:HY-13836CASNo.:1354745-52-0分?式:C??H??ClF?NO?分?量:475.84作?靶點:Parasite作?通路:Anti-infection儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗DMSO:15.62mg/mL(32.83mM;Needultrasonic)H2O:<0.1mg/mL(insoluble)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.1015mL10.5077mL21.0155mL5mM0.4203mL2.1015mL4.2031mL10mM0.2102mL1.0508mL2.1015mL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。-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(dāng)?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(dāng)保存；體內(nèi)實驗的?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:2.25mg/mL(4.73mM);Suspendedsolution;NeedultrasonicBIOLOGICALACTIVITY?物活性ELQ-300?種有效的、有?服?物活性的抗瘧疾劑，結(jié)合并抑制細(xì)胞?素bc1復(fù)合物(cytbc1)的還原(Qi)位點。ELQ-300抑制惡性瘧原?Dd2，Tm90-C2B和D1的IC50值分別為6.6，4.6和160nM。ELQ-300可?于抗瘧疾的研究。IC50&TargetIC50:6.6nM(P.falciparumDd2),4.6nM(P.falciparumTm90-C2B),160nM(P.falciparumD1)[1]體外研究ELQ-300(0-70nM,21d)inhibitsP.falciparumDd2,Tm90-C2B,andD1growthwithIC50valuesof6.6,4.6and160nM,respectively[1].體內(nèi)研究ELQ-300(1and10mg/kg;p.o.oncedailyfor1or4days)inhibitsP.yoeliigrowthinanacuteinfectionmodel[2].ELQ-300(10and20mg/kg;p.o.oncedailyfor1or4days)preventsrecurrenceofinfectioninmice[2].AnimalModel:6-weekfemaleCF-1micewithP.yoelii-WTinfection[2]Dosage:1and10mg/kgAdministration:Oralgavage;1mg/kgoncedailyfor4-day;10mg/kgoncedailyfor1-dayResult:InhibitedP.yoeliiwithED50valuesof0.04and0.03mg/kgfor4-daydosingand1-daydosing,respectively.AnimalModel:6-weekfemaleCF-1micewithP.yoelii-WTinfection[2]Dosage:10and20mg/kgAdministration:Oralgavage;10mg/kgoncedailyfor4-day;20mg/kgoncedailyfor1-dayResult:Effectivelypreventedrecrudescenceinthe4-daydosingstudieswithinfectionmice.REFERENCES[1].SticklesAM,etal.AtovaquoneandELQ-300CombinationTherapyasaNovelDual-SiteCytochromebc1InhibitionStrategyforMalaria.AntimicrobAgentsChemother.2016Jul22;60(8):4853-9.[2].SticklesAM,etal.Subtlechangesinendochin-likequinolonestructurealterthesiteofinhibitionwithinthecytochromebc1complexofPlasmodiumfalciparum.AntimicrobAgentsChemother.2015Apr;59(4):1977-82.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplicat