DL-TBOA

Product Description

DL-TBOA is a competitive, non-transportable blocker of excitatory amino acid transporters (IC₅₀ values are 6 μM, 6 μM and 70 μM, for EAAT2, EAAT3 and EAAT1, respectively). DL-TBOA also inhibits EAAT4 and EAAT5 (K_i values are 4.4 μM and 3.2 μM respectively). DL-TBOA displays high selectivity for EAATs over ionotropic and metabotropic glutamate receptors. In [³H]-d-Asp uptake assays in HEK293 cells expressing human EAAT2, EAAT1 and EAAT3, K_i values are 2.2, 2.9, and 9.3 μM, respectively. In a FLIPR Membrane Potential (FMP) assay, K_m values are 0.59, 1.8 and 2.8 μM for human EAAT2, EAAT3 and EAAT1, respectively. DL-TBOA augments SN 38 (Cat. No. 2684) induced colorectal cancer cell death in drug-resistant cell lines. DL-TBOA enhances synaptic activity in the frog labyrinth.

Solubility

Preparing Stock Solutions for DL-TBOA

The following data is based on the product molecular weight 239.23

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
1 mM	4.18 mL	20.90 mL	41.80 mL
5 mM	0.84 mL	4.18 mL	8.36 mL
10 mM	0.42 mL	2.09 mL	4.18 mL
50 mM	0.08 mL	0.42 mL	0.84 mL

Calculators

Background References

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

• Rossi Pre- and postsynaptic effects of glutamate in the frog labyrinth. Neuroscience 2018 PMID: 29913242
• Jensen and Bräuner-Osborne Pharmacological characterization of human excitatory amino acid transporters EAAT1, EAAT2 and EAAT3 in a fluorescence-based membrane potential assay. Biochem.Pharmacol. 2004 PMID: 15135308
• Pedraz-Cuesta The glutamate transport inhibitor DL-Threo--Benzyloxyaspartic acid (DL-TBOA) differentially affects SN38- and oxaliplatin-induced death of drug-resistant colorectal cancer cells. BMC Cancer 2015 PMID: 25981639
• Shimamoto Syntheses of optically pure β-hydroxyaspartate derivatives as glutamate transporter blockers. Bioorg.Med.Chem.Lett. 2000 PMID: 11078189
• Shimamoto DL-threo-β-benzyloxyaspartate, a potent blocker of excitatory amino acid transporters. Mol.Pharmacol. 1998 PMID: 9463476
• Shigeri Effects of threo-β-hydroxyaspartate derivatives on excitatory amino acid transporters (EAAT4 and EAAT5). J.Neurochem. 2001 PMID: 11677257
• Jabaudon Inhibition of uptake unmasks rapid extracellular turnover of glutamate of nonvesicular origin. Proc.Natl.Acad.Sci.U.S.A. 1999 PMID: 10411944