DL-TBOA
Tocris Bioscience | Catalog # 1223
Key Product Details
Description
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 (Ki 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, Ki values are 2.2, 2.9, and 9.3 μM, respectively. In a FLIPR Membrane Potential (FMP) assay, Km 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.
Product Specifications for DL-TBOA
Molecular Weight
Formula
Storage
Purity
Chemical Name
CAS Number
PubChem ID
InChI Key
SMILES
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Solubility
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| water | 1.2 | 5 with gentle warming | |
| DMSO | 23.92 | 100 |
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.
| 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. See our Citations tab to view 209 publications citing the usage of this 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
Product Documents for DL-TBOA
Certificate of Analysis
To download a Certificate of Analysis, please enter a lot or batch number in the search box below.
Product Specific Notices for DL-TBOA
For research use only
Citations for DL-TBOA
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Species: MouseAssay Type: In VitroCell Line/Tissue: Mixed neuron-gliaVerified Customer | Posted 07/12/2020Incubate for 24hTBOA (100 μM)
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Species: MouseAssay Type: Ex VivoVerified Customer | Posted 04/09/2019Used at 100uMUsed for slice electrophysiology experiments to inhibit glutamate transport.
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