Nelonemdaz-potassium-Salfaprodil-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemENelonemdazpotassiumCat.No.:HY-106408ACASNo.:916214-57-8Synonyms:Salfaprodil;Neu2000potassium分⼦式:C₁₅H₇F₇KNO₃分⼦量:421.31作⽤靶点:iGluR作⽤通路:MembraneTransporter/IonChannel;NeuronalSignaling储存⽅式:4°C,sealedstorage,awayfrommoisture*Insolvent:-80°C,6months;-20°C,1month(sealed

storage,awayfrommoisture)溶解性数据体外实验DMSO:200mg/mL(474.71mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制备储备液1mM2.3735mL11.8677mL23.7355mL5mM0.4747mL2.3735mL4.7471mL10mM0.2374mL1.1868mL2.3735mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month(sealedstorage,awayfrommoisture)。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。BIOLOGICALACTIVITY⽣物活性Nelonemdaz(Salfaprodil)potassium⼀种NR2B选择性和⾮竞争性的N-甲-D-天冬氨酸(NMDA)受体拮抗剂，也⼀种⾃由除剂。Nelonemdazpotassium对NMDA和⾃由诱导的细胞死亡具有出⾊的神经保护作⽤。IC50&TargetNMDA[1]1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE体外研究Nelonemdazpotassium(10-300μM)showsapparentneuroprotectionagainst300μMN-methyl-d-aspartate(NMDA)atdosesaslowas30μM[1].Nelonemdazpotassium(10-500μM)inhibitstheelectrophysiologicresponseofculturedcorticalneuronsto300μMNMDAinaconcentration-dependentmanner[1].Nelonemdazpotassium(0.1-1μM)producesamarkedreductionofFe2+-inducedneurotoxicity,evenatdosesof0.1to0.3μM[1].Nelonemdazpotassium(0.1-1μM)blocksthedegenerationofneuronsandgliaincorticalcellcultures[1].Nelonemdazpotassium(0-350μM)effectivelyscavengessuperoxideradicals(IC50=63.07±1.44μM),nitricoxide(IC50=155.8±4.88μM),andhydroxylradicals(IC50=58.45±1.74μM)[3].Nelonemdazpotassium(0.78-12.5μM)decreasestheamountofantimycinA-inducedROS/RNSformationinadose-dependentmanner,withanIC50of2.21±0.11μM[3].Nelonemdazpotassium(0.19-12.5μM)inhibitsmalondialdehyde(MDA)formationwithanIC50of2.72±0.26μM[3].Nelonemdazpotassium(0-125μM)effectivelyreducesiron-ascorbate-inducedlipidperoxidation(IC50=24.56±0.07μM)[3].体内研究Nelonemdazpotassium(0.5-20mg/kg;i.v.)reducescerebralinfarctevolving24hafter60-minsocclusionofthemiddlecerebralarteryocclusion(MCAO)substantiallyanddosedependently[1].Nelonemdazpotassium(5mg/kg;i.v.)protectswhitemattersuchasaxonsandmyelinaswellasgraymatterfromischemicbraininjury[1].AnimalModel:MaleSprague-Dawleyrats(260to300g)(clipocclusionmodel)[1]Dosage:0.5-20mg/kgAdministration:I.v.administration5minsafterreperfusionResult:Producedalargeneuroprotectiveeffect,withamaximalreductionininfarctvolumeof66%atdosesof2.5to5mg/kg.Notobservedneuronaldamageinthemostvulnerablecorticalareaafteradministrationof5mg/kg.AnimalModel:MaleSprague-Dawleyrats(260to300g)(intraluminalthreadocclusionmodel)[1]Dosage:5mg/kgAdministration:I.v.administration30minsafterreperfusionResult:DidnotchangephysiologicvariablessuchasarterialpH,PCO2,PO2,andhematocrit.Reducedinfarctvolumeevolvinginthecortexandthestriatumsubstantially.Reducedwhitematterdamageinthestriatumandexternalcapsulemarkedly.REFERENCES2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE[1].NishantPV,et,al.AntioxidantPropertiesofNeu2000onMitochondrialFreeRadicalsandOxidativeDamage.ToxicolInVitro.2013Mar;27(2):788-97.[2].GwagBJ,etal.MarkedpreventionofischemicbraininjurybyNeu2000,anNMDAantagonistandantioxidantderivedfromaspirinandsulfasalazine.JCerebBloodFlowMetab.2007Jun;27(6):1142-51.[3].SungIC,et,al.Neu2000,anNR2B-selective,ModerateNMDAReceptorAntagonistandPotentSpinTrappingMoleculeforStroke.DrugNewsPerspect.2010Nov;23(9):549-56.McePdfHeightCaution