Hotline:400-820-3792Inhibitors?ScreeningLibraries?Proteinswww.MedChemETFB-TBOACat.No.:HY-107521CASNo.:480439-73-4Synonyms:CF3-Bza-TBOA分?式:C??H??F?N?O?分?量:426.34作?靶點(diǎn):EAAT2作?通路:MembraneTransporter/IonChannel儲(chǔ)存?式:Powder-20°C3yearsInsolvent-80°C6months-20°C1month溶解性數(shù)據(jù)體外實(shí)驗(yàn)DMSO:50mg/mL(117.28mM;Needultrasonic)MassSolvent1mg5mg10mgConcentration制備儲(chǔ)備液1mM2.3455mL11.7277mL23.4555mL5mM0.4691mL2.3455mL4.6911mL10mM0.2346mL1.1728mL2.3455mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；?旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。儲(chǔ)備液的保存?式和期限：-80°C,6months;-20°C,1month。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?，-20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?個(gè)?內(nèi)使?。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥?式選擇適當(dāng)?shù)娜芙?案。以下溶解?案都請(qǐng)先按照InVitro?式配制澄的儲(chǔ)備液，再依次添加助溶劑：(為保證實(shí)驗(yàn)結(jié)果的可靠性，澄的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的?作液，建議您現(xiàn)?現(xiàn)配，當(dāng)天使?；以下溶劑前顯?的百分?指該溶劑在您配制終溶液中的體積占?；如在配制過(guò)程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過(guò)加熱和/或超聲的?式助溶)1.請(qǐng)依序添加每種溶劑：10%DMSO>>40%PEG300>>5%Tween-80>>45%salineSolubility:≥1.25mg/mL(2.93mM);Clearsolution1/2MasterofBioactiveMolecules—您?邊的抑制劑?師www.MedChemE2.請(qǐng)依序添加每種溶劑：10%DMSO>>90%(20%SBE-β-CDinsaline)Solubility:≥1.25mg/mL(2.93mM);Clearsolution3.請(qǐng)依序添加每種溶劑：10%DMSO>>90%cornoilSolubility:≥1.25mg/mL(2.93mM);ClearsolutionBIOLOGICALACTIVITY?物活性TFB-TBOA(CF3-Bza-TBOA)?種有效的?氨酸轉(zhuǎn)運(yùn)體(glutamatetransporter)阻滯劑，可有效抑制神經(jīng)膠質(zhì)轉(zhuǎn)運(yùn)體的活性。TFB-TBOA對(duì)?氨酸轉(zhuǎn)運(yùn)蛋?EAAT1、EAAT2和EAAT3的IC50值分別為22、17和300nM。體外研究TFB-TBOA(CF3-Bza-TBOA)inhibitssynapticallyactivatedtransportercurrents(STCs)inastrocytesinthestratumradiatuminrathippocampalslicesinadose-dependentmannerwithanIC50of13nM,andreducesthemtoapproximately10%ofthecontrolat100nM[2].TFB-TBOAinhibitstheNa+iresponseevokedby200μMglutamateinaconcentration-dependentmannerwithIC50valueof43nM,asmeasuredontheamplitudeoftheNa+iresponse[1].REFERENCES[1].ShimamotoK,etal.CharacterizationofnovelL-threo-beta-benzyloxyaspartatederivatives,potentblockersoftheglutamatetransporters.MolPharmacol.2004;65(4):1008-1015.[2].TsukadaS,etal.Effectsofanovelglutamatetransporterblocker,(2S,3S)-3-[3-[4-(trifluoromethyl)benzoylamino]benzyloxy]aspartate(TFB-TBOA),onactivitiesofhippocampalneurons.Neuropharmacology.2005;48(4):479-491.[3].BozzoL,etal.Inhibitoryeffectsof(2S,3S)-3-[3-[4-(trifluoromethyl)benzoylamino]benzyloxy]aspartate(TFB-TBOA)ontheastrocyticsodiumresponsestoglutamate.BrainRes.2010;1316:27-34.McePdfHeightCaution:Producthasnotbeenfullyvalidatedformedicalapplications.Forres