SC-51089-free-base-DataSheet-生命科學(xué)試劑-MCE

Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemESC51089freebaseCat.No.:HY-108563ACASNo.:146033-03-6分?式:C??H??ClN?O?分?量:422.86作?靶點(diǎn):ProstaglandinReceptor作?通路:GPCR/GProtein儲(chǔ)存?式:4°C,sealedstorage,awayfrommoistureandlight*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoistureandlight)溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:100mg/mL(236.48mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.3648mL11.8242mL23.6485mL5mM0.4730mL2.3648mL4.7297mL10mM0.2365mL1.1824mL2.3648mL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(sealedstorage,awayfrommoistureandlight)。-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?。BIOLOGICALACTIVITY?物活性SC51089freebase?種選擇性的前列腺素受體EP1拮抗劑，對(duì)EP1，TP，EP3和FP受體的Ki值分別為1.3，11.2，17.5和61.1μM。SC51089freebase具有神經(jīng)保護(hù)活性。IC50&TargetEP1TPEP3FP1.3μM(Ki)11.2μM(Ki)17.5μM(Ki)61.1μM(Ki)體外研究SC51089freebase(5μM;24h)attenuatesprostaglandinE2(PGE2)-inducedthedeathofneuronalcells1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEexposedtot-BuOOH[2].體內(nèi)研究SC51089freebase(40μg/kg;infusedi.p.for28d)amelioratesmotorcoordinationandbalancedysfunctionandrescueslong-termmemorydeficitinR6/1mousemodelofHD[3].AnimalModel:R6/1mousemodelofHuntington'sdisease(HD),from13to18weeksofage[3]Dosage:40μg/kg/dayAdministration:Infusedi.p.atarateof0.11μL/hduring28daysbyosmoticmini-pumpsystemResult:Amelioratedmotorcoordinationandbalancedysfunction.Rescuedlong-termmemorydeficit.Improvedtheexpressionofspecificsynapticmarkers.Reducedthenumberofhuntingtinnuclearinclusionsinthestriatumandhippocampus.REFERENCES[1].AbramovitzM,et,al.Theutilizationofrecombinantprostanoidreceptorstodeterminetheaffinitiesandselectivitiesofprostaglandinsandrelatedanalogs.BiochimBiophysActa.2000Jan17;1483(2):285-93.[2].SaleemS,et,al.EffectsofEP1receptoroncerebralbloodflowinthemiddlecerebralarteryocclusionmodelofstrokeinmice.JNeurosciRes.2007Aug15;85(11):2433-40.[3].Anglada-HuguetM,et,al.ProstaglandinE2EP1receptorantagonistimprovesmotordeficitsandrescuesmemorydeclineinR6/1mousemodelofHuntington'sdisease.MolNeurobiol.2014Apr;49(2):784-95.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresea