DL-TBOA-ammonium-DataSheet-生命科学试剂-MedChemExpress

Hotline:400-820-3792Inhibitors•Agonists•ScreeningLibrariesDL-TBOAammoniumCat.No.:HY-107522BCASNo.:2093503-71-8分⼦式:C₁₁H₁₆N₂O₅分⼦量:256.26作⽤靶点:EAAT2作⽤通路:MembraneTransporter/IonChannel储存⽅式:PleasestoretheproductundertherecommendedconditionsintheCertificateofAnalysis.BIOLOGICALACTIVITY⽣物活性DL-TBOAammonium⼀种有效的不可运输的兴奋性氨酸转运蛋⽩抑制剂，对兴奋性氨酸转运蛋⽩1(EAAT1)，EAAT2和EAAT3的IC50值分别为70μM，6μM和6μM。DL-TBOAammonium抑制表达⼈EAAT1和EAAT2的COS-1细胞摄取[14C]⾕氨酸，Ki值分别为42μM和5.7μM。DL-TBOAammonium以竞争性⽅式阻断EAAT4和EAAT5，Ki值分别为4.4μM和3.2μM。IC50&TargetIC50:70μM(EAAT1),6μM(EAAT2)and6μM(EAAT3);Ki:42μM(humanEAAT1),5.7μM(humanEAAT2),4.4μM(EAAT4)and3.2μM(EAAT5)[1][2][3]体外研究DL-TBOAammonium(70-350μM;48hours)treatmentconcentration-dependentlyenhancesSN38-inducedlossofviability.DL-TBOAreversedOxaliplatin-inducedlossofviability[4].DL-TBOAammonium(350μM;24hours)decreasesp53inductionbySN38andoxaliplatin[4].CellViabilityAssay[4]CellLine:HCT116cells,LoVocellsConcentration:70μM,350μMIncubationTime:48hoursResult:EnhancedSN38-induced,andcounteractedOxaliplatin-induced,celldeath.CellViabilityAssay[4]CellLine:HCT116cells,LoVocells1/3Concentration:350μMIncubationTime:24hoursResult:p53inductionbySN38andoxaliplatinwasdecreased.体内研究DL-TBOAammonium(10nmol;i.c.v.)tomorphine-dependentratssignificantlyfacilitatestheexpressionofnaloxone-precipitatedsomaticsignsandconditionedplaceaversion[5].AnimalModel:MaleSprague-Dawleyrats(180-250g)[5]Dosage:1nmol,3nmol,10nmolAdministration:Intracerebroventricularlyinjection(i.c.v.)Result:DosedependentlyfacilitatedvarioussomaticsignsinducedbyNaloxone(0.1mg/kg)-precipitatedmorphinewithdrawal.REFERENCES[1].ShimamotoK,etal.DL-threo-beta-benzyloxyaspartate,apotentblockerofexcitatoryaminoacidtransporters.MolPharmacol.1998Feb;53(2):195-201.[2].JabaudonD,etal.Inhibitionofuptakeunmasksrapidextracellularturnoverofglutamateofnonvesicularorigin.ProcNatlAcadSciUSA.1999Jul20;96(15):8733-8.[3].ShigeriY,etal.Effectsofthreo-beta-hydroxyaspartatederivativesonexcitatoryaminoacidtransporters(EAAT4andEAAT5).JNeurochem.2001Oct;79(2):297-302.[4].Pedraz-CuestaE,etal.TheglutamatetransportinhibitorDL-Threo-β-Benzyloxyasparticacid(DL-TBOA)differentiallyaffectsSN38-andoxaliplatin-induceddeathofdrug-resistantcolorectalcancercells.BMCCancer.2015May16;15:411.[5].YumikoSekiya,etal.Facilitationofmorphinewithdrawalsymptomsandmorphine-inducedconditionedplacepreferencebyaglutamatetransporterinhibitorDL-threo-beta-benzyloxyaspartateinrats.EurJPharmacol.2004Feb6;485(1-3):201-10.McePdfHeight2/3MedChemExpr