TFB-TBOA

Product Description

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.

Solubility

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

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

• Fu Chemoenzymatic synthesis and pharmacological characterization of functionalized aspartate analogues as novel excitatory amino acid transporter inhibitors. J.Med.Chem. 2018 PMID: 30011368
• Bozzo and Chatton Inhibitory effects of (2S, 3S)-3-[3-[4-(trifluoromethyl)benzoylamino]benzyloxy]aspartate (TFB-TBOA) on the astrocytic sodium responses to glutamate. Brain Res. 2010 PMID: 20026319
• Shimamoto and Shigeri Elucidation of glutamate transporter functions using selective inhibitors. CNS Agents Med.Chem.
• Magi Physical and functional interaction of NCX1 and EAAC1 transporters leading to glutamate-enhanced ATP production in brain mitochondria. PLoS One 2012 PMID: 22479505
• Tsukada 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 PMID: 15755476