Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemEPep4cCat.No.:HY-P1057CASNo.:243843-43-8分?式:C??H??N??O??S分?量:1146.41Sequence:Lys-Arg-Met-Lys-Val-Ala-Lys-Ser-Ala-GlnSequenceShortening:KRMKVAKSAQ作?靶點:iGluR作?通路:MembraneTransporter/IonChannel;NeuronalSignaling儲存?式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY?物活性Pep4cPep2m(HY-P1058)的?活性對照肽。Pep4c缺乏功能活性，?法破壞蛋?與C激酶1(PICK1)-AMPA受體(GluA2)或N-?馬來酰亞胺敏感因?(NSF)-GluA2的相互作?。在實驗中，Pep4c被?作性對照，以驗證Pep2m對AMPA受體運輸和突觸可塑性的響的特異性。IC50&TargetAMPAReceptorNMDAReceptor體外研究Pep4cdoesnotreducethecurrentresponsetotopicallyappliedAMPA,nordoesitaffectthefrequencyandamplitudeofAMPA-mEPSCsinculturedhippocampalneurons[1].Pep4cdoesnotalterthesurfaceexpressionofAMPAreceptorsinculturedhippocampalneuronsbutimprovesthecolocalizationofGluR2andsynaptophysininculturedhippocampalneurons[1].Pep4cdoesnotaffectlong-termdepression(LTD)andbasalparallelfiberexcitatorypostsynapticcurrent(PF-EPSC)inhippocampalslices,butcaninducelong-termpotentiation(LTP)by1Hzparallelfiber(PF)stimulation[2][3].Pep4cdoesnotbindtoNSFanddoesnotalterautisticEPSCsevokedinPep2m-loadedneurons[4].Pep4cdoesnotalterthereleaseofradiolabeledD-aspartate([3H]D-ASP)inrathippocampalsynaptosomes,eitherintheabsence(notshown)orinthepresenceof50μM(S)AMPA[5].Pep4cdoesnotaffecttritiumreleaseinducedby10μMNMDA/1μMGlycine(HY-Y0966),butcausedchangesin[3H]D-ASPreleaseinducedby10μMNMDA/1μMGlycineand10μMNMDA/1μMGlycine/50μM(S)AMPA[5].Pep4cdoesnotattenuatesynaptictransmission[6].1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemEREFERENCES[1].NoelJ,etal.SurfaceexpressionofAMPAreceptorsinhippocampalneuronsisregulatedbyanNSF-dependentmechanism.Neuron.1999Jun;23(2):365-76.[2].LüthiA,etal.HippocampalLTDexpressioninvolvesapoolofAMPARsregulatedbytheNSF-GluR2interaction.Neuron.1999Oct;24(2):389-99.[3].GallimoreAR,etal.SwitchingOnDepressionandPotentiationintheCerebellum.CellRep.2018Jan16;22(3):722-733.[4].CingolaniLA,etal.Activity-dependentregulationofsynapticAMPAreceptorcompositionandabundancebybeta3integrins.Neuron.2008Jun12;58(5):749-62.[5].SummaM,etal.HippocampalAMPAautoreceptorspositivelycoupledtoNMDAautoreceptorstrafficinaconstitutivemannerandundergoadaptativechangesfollowingenrichedenvironmenttraining.Neuropharmacology.2011Dec;61(8):1282-90.[6].CorreiaSS,etal.Motorprotein-dependenttransportofAMPAreceptorsintospinesduringlong-termpotentiation.NatNeurosci.2008Apr;11(4):457-66.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicala