RN-1-dihydrochloride-DataSheet-生命科學(xué)試劑-MedChemExpress

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemERN-1dihydrochlorideCat.No.:HY-110130CASNo.:1781835-13-9分?式:C??H??Cl?N?O?分?量:452.42作?靶點:HistoneDemethylase作?通路:Epigenetics儲存?式:Powder-20°C3years4°C2yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實驗H2O:20mg/mL(44.21mM;ultrasonicandwarmingandheatto60°C)MassSolvent1mg5mg10mgConcentration制備儲備液1mM2.2103mL11.0517mL22.1034mL5mM0.4421mL2.2103mL4.4207mL10mM0.2210mL1.1052mL2.2103mL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?。BIOLOGICALACTIVITY?物活性RN-1dihydrochloride?種有效的、可透過?腦屏障、不可逆的、選擇性的賴氨酸特異性脫甲酶1(LSD1)抑制劑，IC50為70nM。RN-1dihydrochloride對LSD1的選擇性?于MAO-A和MAO-B，IC50值分別為0.51μM和2.785μM。IC50&TargetIC50:70nM(LSD1),0.51μM(MAO-A)and2.785μM(MAO-B)[1]1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE體外研究RN-1dihydrochlorideshowscytotoxicforovariancancercells(SKOV3,OVCAR3,A2780andcisplatin-resistantA2780cis),withIC50valuesof≈100-200μM[3].體內(nèi)研究RN-1(3-10mg/kg;i.p.;daily;for2or4consecutiveweeks)dihydrochlorideeffectivelyinducesfetalhemoglobin(HbF)levelsinredbloodcellsandreducesdiseasepathologyinSCDmice[2].InC57BL/6malemice,afterintraperitonealadministrationofRN-1dihydrochloride(10mg/kg),concentrationsaredetectableupto24hpostdoseinbothplasmaandbraintissues.Thebrain/plasmaexposureratiois88.9.RN-1dihydrochloridesignificantlyimpairslong-termmemory,butnotshort-termmemory[1].AnimalModel:Sicklecelldisease(SCD)mice[2]Dosage:3mg/kgor10mg/kgAdministration:i.p.;daily;for2or4consecutiveweeksResult:EffectivelyinducedHbFlevelsinredbloodcellsandreduceddiseasepathologyinSCDmice.REFERENCES[1].RameshNeelamegam,etal.Brain-penetrantLSD1inhibitorscanblockmemoryconsolidation.ACSChemNeurosci.2012Feb15;3(2):120-128.[2].ShuaiyingCui,etal.TheLSD1inhibitorRN-1inducesfetalhemoglobinsynthesisandreducesdiseasepathologyinsicklecellmice.Blood.2015Jul16;126(3):386-96.[3].SergiyKonovalov,etal.Analysisofthelevelsoflysine-specificdemethylase1(LSD1)mRNAinhumanovariantumorsandtheeffectsofchemicalLSD1inhibitorsinovariancancercelllines.JOvarianRes.2013Oct29;6(1):75.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forres