Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEPep2-SVKECat.No.:HY-P1055CASNo.:1315378-76-7分子式:C??H??N??O??分子量:1300.41Sequence:Tyr-Asn-Val-Tyr-Gly-Ile-Glu-Ser-Val-Lys-GluSequenceShortening:YNVYGIESVKE作用靶點:iGluR作用通路:MembraneTransporter/IonChannel;NeuronalSignaling儲存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性Pep2-SVKE是pep2-SVKI(HY-P1056)的非活性對照肽。Pep2-SVKE是一種抑制肽，對應(yīng)于GluR2AMPA受體亞基C末端的最后10個氨基酸。Pep2-SVKE不能阻斷AMPA介導(dǎo)的[3H]DA胞吐。Pep2-SVKE不能與GRIP或PICK43結(jié)合，也不會阻斷GST-GluR2和LTD對PICK1的保留。IC50&TargetAMPAReceptor體外研究Pep2-SVKE(100μM)doesnotblockmGluR-LTDindopaminergic(DA)neurons[1].Pep2-SVKE(1mM)doesnotbindtoPICKorGRIP46,nordoesitinhibittheincreaseinEPSCamplituderatio(R+40/-60mV)inducedbyactivepeptides[2].Pep2-SVKE(1mM)doesnotbindtoGRIPorPICK43,nordoesitaltermEPSCamplitudeandAMPA-andNMDA-induced[3H]AChreleaseatsomaticAMPARreceptors[2][4].Pep2-SVKE(1μM)doesnotalterthedramaticreductionin[3H]DAefflux[3].Pep2-SVKEdoesnotabolishAMPAreceptorsensitivitytocyclothiazide,whichcontrolsthereleaseof[3H]nucleosideanalogs(NA)[4].Pep2-SVKE(133μM)doesnotblocktheretentionofPICK1byGST-GluR2andLTD[5].REFERENCESMameliM,etal.RapidsynthesisandsynapticinsertionofGluR2formGluR-LTDintheventraltegmentalarea.Science.2007Jul27;317(5837):530-3.1/2 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemELiuSJ,etal.SubunitinteractionwithPICKandGRIPcontrolsCa2+permeabilityofAMPARsatcerebellarsynapses.NatNeurosci.2005Jun;8(6):768-75.GrilliM,etal.InvitroexposuretonicotineinducesendocytosisofpresynapticAMPAreceptorsmodulatingdopaminereleaseinratnucleusaccumbensnerveterminals.Neuropharmacology.2012Oct;63(5):916-26.PittalugaA,etal.TraffickingofpresynapticAMPAreceptorsmediatingneurotransmitterrelease:neuronalselectivityandrelationshipswithsensitivitytocyclothiazide.Neuropharmacology.2006Mar;50(3):286-96.DawMI,etal.PDZproteinsinteractingwithC-terminalGluR2/3areinvolvedinaPKC-dependentregulationofAMPAreceptorsathippocampalsynapses.Neuron.2000Dec;28(3):873-86.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearch