Hotline:400-820-3792Inhibitors ? ScreeningLibraries ? Proteinswww.MedChemEpep2-SVKICat.No.:HY-P1056CASNo.:328944-75-8分子式:C??H??N??O??分子量:1284.46Sequence:Tyr-Asn-Val-Tyr-Gly-Ile-Glu-Ser-Val-Lys-IleSequenceShortening:YNVYGIESVKI作用靶點(diǎn):iGluR作用通路:MembraneTransporter/IonChannel;NeuronalSignaling儲(chǔ)存方式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY生物活性pep2-SVKI是一種選擇性肽抑制劑。pep2-SVKI可抑制AMPA型谷氨酸受體(GluA2)(C端PDZ位點(diǎn))與谷氨酸受體相互作用蛋白(GRIP)、AMPA受體結(jié)合蛋白(ABP)和C激酶相互作用蛋白(PICK1)的結(jié)合。pep2-SVKI增加AMPA受體介導(dǎo)的電流幅度并阻斷長(zhǎng)時(shí)程抑制(LTD)。pep2-SVKI可用于神經(jīng)系統(tǒng)疾病的研究。體外研究pep2-SVKI(1mM)reduces(MiniatureExcitatoryPostsynapticCurrent)mEPSCamplitudeatboth?60mVand+40mVinthesynapticmembraneofstellatecells[1].pep2-SVKI(100μM)causesanincreaseinAMPAR-mediated(ExcitatoryPostsynapticCurrent)EPSCsinhippocampalCA1Neurons[2].pep2-SVKI(100μM)preventstheexpressionofLTDina(ProteinKinaseC)PKC-DependentMannerinhippocampalCA1Neurons[2].pep2-SVKIincreasestritiumreleaseinducedbyexposureto100μMAMPAinhippocampalsynaptosomesprelabeledwith(radiolabelednorepinephrine)[3H]NAandpotentiatestheAMPA-evokedreleaseof[3H]NAinrathippocampalsynaptosomes[3].pep2-SVKIcausesincreaseinthenumberofAMPARsexposedonthemembraneinrathippocampalsynaptosomes[3].pep2-SVKIabolishesthesensitivitytoCyclothiazide(HY-101165)oftheAMPAreceptorscontrolling[3H]NArelease[3].REFERENCES1/2 MasterofBioactiveMolecules—您身邊的抑制劑大師www.MedChemELiuSJ,etal.SubunitinteractionwithPICKandGRIPcontrolsCa2+permeabilityofAMPARsatcerebellarsynapses.NatNeurosci.2005Jun;8(6):768-75.DawMI,etal.PDZproteinsinteractingwithC-terminalGluR2/3areinvolvedinaPKC-dependentregulationofAMPAreceptorsathippocampalsynapses.Neuron.2000Dec;28(3):873-86.PittalugaA,etal.TraffickingofpresynapticAMPAreceptorsmediatingneurotransmitterrelease:neuronalselectivityandrelationshipswithsensitivitytocyclothiazide.Neuropharmacology.2006Mar;50(3):286-96.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forresearchuseonly.T