Biological Activity
Potent and selective glial glutamate transporter EAAT1 and EAAT2 inhibitor (IC50 values are 17, 22 and 300 nM for EAAT2, EAAT1 and EAAT3 respectively). Has no effect on EAAT4 and EAAT5, or a wide range of neuronal receptors and transporters. Attenuates glutamate-stimulated intracellular Na+ elevation in astrocytes in vitro (IC50 = 43 nM). Induces severe convulsions in vivo.
Licensing Information
Sold for research purposes under license from Suntory Ltd.
Technical Data
| M. Wt | 426.35 |
| Formula | C19H17F3N2O6 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 480439-73-4 |
| PubChem ID | 52941382 |
| InChI Key | LPWONNPEPDHEAI-GJZGRUSLSA-N |
| Smiles | OC([C@@H](N)[C@H](OCC1=CC=CC(NC(C2=CC=C(C(F)(F)F)C=C2)=O)=C1)C(O)=O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.63 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 426.35. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.35 mL | 11.73 mL | 23.45 mL |
| 5 mM | 0.47 mL | 2.35 mL | 4.69 mL |
| 10 mM | 0.23 mL | 1.17 mL | 2.35 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.47 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Tsukada et al (2005) Effects of a novel glutamate transporter blocker, (2S, 3S)-3-{3-[4-(trifluoromethyl)benzoylamino]benzyloxy}aspartate (TFB-TBOA), on activities of hippocampal neurons. Neuropharmacology 48 479 PMID: 15755476
Shimamoto and Shigeri (2006) Elucidation of glutamate transporter functions using selective inhibitors. CNS Agents Med.Chem. 6 59 PMID:
Magi et al (2012) Physical and functional interaction of NCX1 and EAAC1 transporters leading to glutamate-enhanced ATP production in brain mitochondria. PLoS One 7 e34015 PMID: 22479505
Bozzo and Chatton (2010) Inhibitory effects of (2S, 3S)-3-[3-[4-(trifluoromethyl)benzoylamino]benzyloxy]aspartate (TFB-TBOA) on the astrocytic sodium responses to glutamate. Brain Res. 1316 PMID: 20026319
Keywords: TFB-TBOA, supplier, High, affinity, EAAT1, EAAT2, blockers, EAAT, Excitatory, Amino, Acid, Transporters, GLAST, GLT-1, Glutamate, Monoamine, Neurotransmitter, Glutamate, Transporters, Glutamate, Transporters, Tocris Bioscience
