Tat-NR2B9c-Tat-NR2Bct-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•ScreeningLibraries•Proteinswww.MedChemETat-NR2B9cCat.No.:HY-P0117CASNo.:500992-11-0Synonyms:Tat-NR2Bct;NA-1分⼦式:C₁₀₅H₁₈₈N₄₂O₃₀分⼦量:2518.88SequenceShortening:YGRKKRRQRRRKLSSIESDV作⽤靶点:iGluR;NOSynthase作⽤通路:MembraneTransporter/IonChannel;NeuronalSignaling;Immunology/Inflammation储存⽅式:Powder-80°C2years-20°C1yearInsolvent-80°C6months-20°C1month溶解性数据体外实验H2O:≥50mg/mL(19.85mM)*"≥"meanssoluble,butsaturationunknown.MassSolvent1mg5mg10mgConcentration制备储备液1mM0.3970mL1.9850mL3.9700mL5mM0.0794mL0.3970mL0.7940mL10mM0.0397mL0.1985mL0.3970mL请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。储备液的保存⽅式和期限：-80°C,6months;-20°C,1month。-80°C储存时，请在6个⽉内使⽤，-20°C储存时，请在1个⽉内使⽤。体内实验Tat-NR2B9cispreparedinsaline[4].1/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemEBIOLOGICALACTIVITY⽣物活性Tat-NR2B9c(Tat-NR2Bct;NA-1)⼀种PSD-95的抑制剂，抑制PSD-95d2(PSD-95PDZdomain2)和PSD-95d1的EC50分别为6.7nM和670nM。Tat-NR2B9c扰乱了PSD-95/NMDAR的相互作⽤，抑制PSD-95和NR2A和NR2B结合的IC50值分别为0.5μM和8μM。Tat-NR2B9c还能抑制神经元⼀氧化氮合酶(nNOS)/PSD-95相互作⽤，具有神经保护作⽤。IC50&TargetEC50:6.7nM(PSD-95d2),670nM(PSD-95d1)[1]NOsynthase[1]体外研究Tat-NR2B9cisaPSD-95inhibitor,withanEC50of6.7nMforPSD-95d2,representinga>100-foldhigheraffinityforthisdomainthanforPSD-95d1(EC50,0.67μM).Tat-NR2B9cinhibitsNMDAR2A,NMDAR2B,andNMDAR2CbindingtoPSD-95,withIC50sof0.5μM,-8μM,and0.75μM,respectively.Tat-NR2B9calsoblockstheinteractionbetweenPSD-95andnNOSwithanIC50of-0.2μM[1].Tat-NR2B9creducesassociationofPSD-95withGluN2Bby-50%intheYAC128striatum,decreasesNMDA-inducedp38activationinYAC128striataltissue,butshowsnoeffectontheNMDA-inducedJNKactivation[2].体内研究Tat-NR2B9c(10ꢀnmol/g,i.v.)reducesinfarctionvolumeofmaleC57BL/6mice,buthasnoeffectat3ꢀnM/g[3].PROTOCOLCellAssay[2]Postnatalmono-culturedWTandYAC128striatalneurons(DIV9,duetotheviabilityofthesemono-culturedMSNs)arepretreatedfor1hwith200nMTat-NR2B9c,and/orSB-239063(p38inhibitor),and/orSP-600125(JNKinhibitor),thenincubatedwithorwithout500μMNMDAfor10min.AfterNMDAtreatment,striatalneuronsarewashedoncewithwarmplatingmedium(PM)andthenincubatedinconditionedPM(withoutTatpeptidesorp38,JNKinhibitors)for24h.ThencellsarewashedwithPBSonceandfixedwith4%paraformaldehyde(PFA)for30min[2].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.AnimalMice[3]Administration[3]Ineachstudymicearerandomlyallocatedtothreetreatmentgroups(0.0,3.0,10.0nMole/gTat-NR2B9c)ortoshamtreatment.Theindividualperformingtheexperimentalprocedures,administeringtreatmentsandperformingtheanalysesisblindedtothetreatmentassignments.Tat-NR2B9cispreparedattheindicateddosesandadministeredintravenouslyviathetailveinusingapumpinavolumeof1ꢀµL/gover5ꢀminbeginningatreperfusion[3].MCEhasnotindependentlyconfirmedtheaccuracyofthesemethods.Theyareforreferenceonly.户使⽤本产品发表的科研⽂献•JCerebBloodFlowMetab.2019Aug;39(8):1588-1601.•SciRep.2018May18;8(1):7848.•PLoSOne.2020Mar3;15(3):e0229499.2/3MasterofBioactiveMolecules—您⾝边的抑制剂⼤师www.MedChemE•JNeuropatholExpNeurol.2020Jul1;79(7):800-808.•BehavBrainRes.7January2022,113537.Seemorecustomervalidationsonwww.MedChemEREFERENCES[1].CuiH,etal.PDZproteininteractionsunderlyingNMDAreceptor-mediatedexcitotoxicityandneuroprotectionbyPSD-95inhibitors.JNeurosci.2007Sep12;27(37):9901-15.[2].FanJ,etal.P38MAPKisinvolvedinenhancedNMDAreceptor-dependentexcitotoxicityinYACtransgenicmousemodelofHuntingtondisease.NeurobiolDis.2012Mar;45(3):999-1009.[3].TevesLM,etal.EfficacyofthePSD95inhibitorTat-NR2B9cinmicerequiresdosetranslationbetweenspecies.JCerebBloodFlowMetab.2016Mar;36(3):555-61.[4].JingFan,etal.N-methyl-D-aspartateReceptorSubunit-AndNeuronal-TypeDependenceofExcitotoxicSignalingThroughPost-SynapticDensity9.JNeurochem.2010Nov;115(4):1045-56