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Description: Potent and selective EAAT1 and EAAT2 blocker
Chemical Name: (3S)-3-[[3-[[4-(Trifluoromethyl)benzoyl]amino]phenyl]methoxy]-L-aspartic acid
Purity: ≥98% (HPLC)
Citations (12)
Literature (1)

Biological Activity for TFB-TBOA

TFB-TBOA is a potent and selective glial glutamate transporter EAAT1 and EAAT2 inhibitor (IC50 values are 17, 22 and 300 nM for EAAT2, EAAT1 and EAAT3, respectively). Exhibits selectivity for EAAT1 and EAAT2 over EAAT4 and EAAT5, and a wide range of neuronal receptors and transporters. In HEK293 cells expressing human EAAT1, 2, and 3, TFB-TBOA exhibited selectivity for hEAAT1 and hEAAT2 over hEAAT3 (respective IC50 values are 3.6, 10, and 120 nM), while in tsA201 cells expressing rat EAAT4, [3H]-d-Asp uptake was inhibited with an IC50 of 40 nM. Attenuates glutamate-stimulated intracellular Na+ elevation in astrocytes in vitro (IC50 = 43 nM). Induces severe convulsions in vivo.

Compound Libraries for TFB-TBOA

TFB-TBOA is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for TFB-TBOA

M. Wt 426.35
Formula C19H17F3N2O6
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 480439-73-4
PubChem ID 52941382
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for TFB-TBOA

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 21.32 50

Preparing Stock Solutions for TFB-TBOA

The following data is based on the product molecular weight 426.35. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
0.5 mM 4.69 mL 23.45 mL 46.91 mL
2.5 mM 0.94 mL 4.69 mL 9.38 mL
5 mM 0.47 mL 2.35 mL 4.69 mL
25 mM 0.09 mL 0.47 mL 0.94 mL

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Product Datasheets for TFB-TBOA

Certificate of Analysis / Product Datasheet
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References for TFB-TBOA

References are publications that support the biological activity of the product.

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

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

Fu et al (2018) Chemoenzymatic synthesis and pharmacological characterization of functionalized aspartate analogues as novel excitatory amino acid transporter inhibitors. J.Med.Chem. 61 7741 PMID: 30011368

If you know of a relevant reference for TFB-TBOA, please let us know.

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Keywords: TFB-TBOA, TFB-TBOA supplier, High, affinity, EAAT1, EAAT2, blockers, EAAT, Excitatory, Amino, Acid, Transporters, GLAST, GLT-1, Glutamate, Monoamine, Neurotransmitter, 2532, Tocris Bioscience

12 Citations for TFB-TBOA

Citations are publications that use Tocris products. Selected citations for TFB-TBOA include:

Obba et al (2015) The PRKAA1/AMPKα1 pathway triggers autophagy during CSF1-induced human monocyte differentiation and is a potential target in CMML. Mol Pain 11 1114 PMID: 26029847

Yan et al (2015) PacT. induces acute pain via directly activating toll like receptor 4. Physiol Rep 11 10 PMID: 25868824

Fleischer et al (2015) High-frequency voltage oscillations in cultured astrocytes. PLoS One 3 PMID: 25969464

Afzalov et al (2013) Low micromolar Ba(2+) potentiates glutamate transporter current in hippocampal astrocytes. Front Cell Neurosci 7 135 PMID: 24009556

Do you know of a great paper that uses TFB-TBOA from Tocris? Please let us know.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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Huntington's Disease Poster

Huntington's disease (HD) is a severe monogenic neurodegenerative disorder, which is characterized by the prevalent loss of GABAergic medium spiny neurons (MSN) in the striatum. This poster summarizes the effects of mutant huntingtin aggregation implicated in the pathology of HD, as well as highlighting the use of iPSCs for HD modeling.