For research use only. Not for therapeutic Use.
TFB-TBOA (CF3-Bza-TBOA) is a potent glutamate transporter blocker that potently suppresses the activity of glial transporters. TFB-TBOA shows IC50 values of 22, 17, and 300 nM for glutamate transporters EAAT1, EAAT2, and EAAT3 respectively in an uptake assay using cells transiently expressing EAATs[1].
TFB-TBOA (CF3-Bza-TBOA) inhibits synaptically activated transporter currents (STCs) in astrocytes in the stratum radiatum in rat hippocampal slices in a dose-dependent manner with an IC50 of 13 nM, and reduces them to approximately 10% of the control at 100 nM[2].
TFB-TBOA inhibits the Na+i response evoked by 200 µM glutamate in a concentration-dependent manner with IC50 value of 43 nM, as measured on the amplitude of the Na+i response[1].
| Catalog Number | I010577 |
| CAS Number | 480439-73-4 |
| Synonyms | (2S,3S)-2-amino-3-[[3-[[4-(trifluoromethyl)benzoyl]amino]phenyl]methoxy]butanedioic acid |
| Molecular Formula | C19H17F3N2O6 |
| Purity | ≥95% |
| InChI | InChI=1S/C19H17F3N2O6/c20-19(21,22)12-6-4-11(5-7-12)16(25)24-13-3-1-2-10(8-13)9-30-15(18(28)29)14(23)17(26)27/h1-8,14-15H,9,23H2,(H,24,25)(H,26,27)(H,28,29)/t14-,15-/m0/s1 |
| InChIKey | LPWONNPEPDHEAI-GJZGRUSLSA-N |
| SMILES | C1=CC(=CC(=C1)NC(=O)C2=CC=C(C=C2)C(F)(F)F)COC(C(C(=O)O)N)C(=O)O |
| Reference | [1]. Shimamoto K, et al. Characterization of novel L-threo-beta-benzyloxyaspartate derivatives, potent blockers of the glutamate transporters. Mol Pharmacol. 2004;65(4):1008-1015. [2]. Tsukada S, et al. Effects of a novel glutamate transporter blocker, (2S, 3S)-3-[3-[4-(trifluoromethyl)benzoylamino]benzyloxy]aspartate (TFB-TBOA), on activities of hippocampal neurons. Neuropharmacology. 2005;48(4):479-491. [3]. Bozzo L, et al. Inhibitory effects of (2S, 3S)-3-[3-[4-(trifluoromethyl)benzoylamino]benzyloxy]aspartate (TFB-TBOA) on the astrocytic sodium responses to glutamate. Brain Res. 2010;1316:27-34. |
