Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEPep2mCat.No.:HY-P1058CASNo.:243843-42-7分子式:C??H??N??O??S分子量:1173.43Sequence:Lys-Arg-Met-Lys-Val-Ala-Lys-Asn-Ala-GlnSequenceShortening:KRMKVAKNAQ作用靶點(diǎn):iGluR作用通路:MembraneTransporter/IonChannel;NeuronalSignaling儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Pep2m是一種肽類受體抑制劑。Pep2m抑制AMPA型谷氨酸受體(GluA2)亞基C末端與N-乙基馬來酰亞胺敏感融合蛋白(NSF)的相互作用。Pep2m可阻止突觸的長時(shí)程抑制(LTD)。Pep2m可以降低神經(jīng)元的突觸后電流、培養(yǎng)海馬神經(jīng)元的AMPA介導(dǎo)電流以及AMPA受體表面表達(dá)。IC50&TargetAMPAReceptor體外研究Pep2mreducesEPSCamplitudeandblocksLTDinCA1pyramidalcellsofhippocampalslicesbyreducingthenumberoffunctionalAMPARs[1].Pep2mreducesthecurrentresponsetolocallyappliedAMPAinculturedhippocampalneurons[2].Pep2mreducesthefrequencyofrecordedAMPA-miniatureexcitatorypostsynapticcurrents(mEPSCs)inthepresenceoftetrodotoxin(TTX)[2].Pep2mreducesthesurfaceexpressionofAMPAreceptorscontainingAMPA-typeglutamatereceptors(GluR2),butdoesnotreducethesurfaceexpressionofNMDAreceptorsandtheingrowthaggregationofAMPAreceptors[2].Pep2mdoesnotaffectbasalsynaptictransmissionandlow-frequencystimulation(LFS)-inducedLTDinyoungGluA2KOmice,anddoesnotaffectbasalsynaptictransmissionbutrestoresLFS-inducedLTDinmatureGluA2KOmice[3].Pep2mreducesAMPA-inducedradiolabelednorepinephrine([3H]NA)butnotAMPA-inducedradiolabeledacetylcholine([3H]Ach)release[5].1/2 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemE體內(nèi)研究Pep2m(1μLof450nM,ICV,once)impairslearningrateandlong-termmemoryexpressioninmaleC57B6Jmice[4].AnimalModel:AdultmaleC57B6Jmice(8weeks)[4]Dosage:1μLof450nMAdministration:ICV,onceResult:Impairedlearningrateandlong-termmemoryexpression.REFERENCESLüthiA,etal.HippocampalLTDexpressioninvolvesapoolofAMPARsregulatedbytheNSF-GluR2interaction.Neuron.1999Oct;24(2):389-99.NoelJ,etal.SurfaceexpressionofAMPAreceptorsinhippocampalneuronsisregulatedbyanNSF-dependentmechanism.Neuron.1999Jun;23(2):365-76.CaoF,etal.HippocampalLong-TermDepressioninthePresenceofCalcium-PermeableAMPAReceptors.FrontSynapticNeurosci.2018Nov13;10:41.ConboyL,etal.StressatlearningfacilitatesmemoryformationbyregulatingAMPAreceptortraffickingthroughaglucocorticoidaction.Neuropsychopharmacology.2010Feb;35(3):674-85.PittalugaA,etal.TraffickingofpresynapticAMPAreceptorsmediatingneurotransmitterrelease:neuronalselectivityandrelationshipswithsensitivitytocyclothiazide.Neuropharmacology.2006Mar;50(3):286-96.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalappli