Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEPep2-AVKICat.No.:HY-P1059CASNo.:1315378-69-8分子式:C??H??N??O??分子量:1268.46Sequence:Tyr-Asn-Val-Tyr-Gly-Ile-Glu-Ala-Val-Lys-IleSequenceShortening:YNVYGIEAVKI作用靶點:iGluR作用通路:MembraneTransporter/IonChannel;NeuronalSignaling儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Pep2-AVKI是AMPA受體亞基(GluR2)亞基(位于C末端PDZ位點)與C激酶(PICK1)結(jié)合的選擇性肽抑制劑。Pep2-AVKI不影響(AMPA型谷氨酸受體)GluA2與GRIP或ABP的結(jié)合。Pep2-AVKI不增加AMPA電流幅度。Pep2-AVKI可用于神經(jīng)系統(tǒng)疾病的研究。體外研究Pep2-AVKI(1mM)selectivelybindstoPICKanddoesnotalter(MiniatureExcitatoryPostsynapticCurrent)mEPSCamplitudeorfrequency,butinhibitstheactivity-inducedincreasein(ExcitatoryPostsynapticCurrent)EPSCamplituderatioincerebellarstellatecells[1].Pep2-AVKI(1mM)blockstheincreaseinsynapticGluR2-containingreceptorsincerebellarstellatecells[1].Pep2-AVKIincreasesAMPA-evoked(radiolabelednorepinephrine)[3H]NAand(radiolabeledD-aspartate)[3H]D-ASPandincreases10μMNMDA/1μMGlycine(HY-Y0966)/50μM(S)AMPA-inducedtritiumrelease,butdoesnotalter10μMNMDA/1μMGlycine-induced[3H]D-ASPreleaseinhippocampalsynaptosomes[2][3].Pep2-AVKI(100μM)blocks(Long-TermDepression)LTDinpostsynapticneurons[4].REFERENCESLiuSJ,etal.SubunitinteractionwithPICKandGRIPcontrolsCa2+permeabilityofAMPARsatcerebellarsynapses.NatNeurosci.2005Jun;8(6):768-75.PittalugaA,etal.TraffickingofpresynapticAMPAreceptorsmediatingneurotransmitterrelease:neuronalselectivityandrelationshipswithsensitivitytocyclothiazide.Neuropharmacology.2006Mar;50(3):286-96.1/2 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemESummaM,etal.HippocampalAMPAautoreceptorspositivelycoupledtoNMDAautoreceptorstrafficinaconstitutivemannerandundergoadaptativechangesfollowingenrichedenvironmenttraining.Neuropharmacology.2011Dec;61(8):1282-90.ToyodaH,etal.Long-termdepressionrequirespostsynapticAMPAGluR2receptorinadultmousecingulatecortex.JCellPhysiol.2007May;211(2):336-43.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseon