DL-TBOA

DL-TBOA

• CAS Number: 205309-81-5
• UNSPSC Description: DL-TBOA is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA inhibits the uptake of [14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively[1][2][3].
• Target Antigen: EAAT
• Type: Reference compound
• Related Pathways: Membrane Transporter/Ion Channel
• Applications: Neuroscience-Neuromodulation
• Field of Research: Neurological Disease
• Assay Protocol: https://www.medchemexpress.com/dl-tboa.html
• Purity: 99.60
• Solubility: DMSO : 200 mg/mL (ultrasonic)|H2O : 5 mg/mL (ultrasonic;warming;heat to 60°C)
• Smiles: OC([C@@H](N)[C@@H](C(O)=O)OCC1=CC=CC=C1)=O
• Molecular Weight: 239.23
• References & Citations: [1]Shimamoto K, et al. DL-threo-beta-benzyloxyaspartate, a potent blocker of excitatory amino acid transporters. Mol Pharmacol. 1998 Feb;53(2):195-201.|[2]Jabaudon D, et al. Inhibition of uptake unmasks rapid extracellular turnover of glutamate of nonvesicular origin. Proc Natl Acad Sci U S A. 1999 Jul 20;96(15):8733-8.|[3]Shigeri Y, et al. Effects of threo-beta-hydroxyaspartate derivatives on excitatory amino acid transporters (EAAT4 and EAAT5). J Neurochem. 2001 Oct;79(2):297-302.|[4]Pedraz-Cuesta E, et al. The glutamate transport inhibitor DL-Threo-β-Benzyloxyaspartic acid (DL-TBOA) differentially affects SN38- and oxaliplatin-induced death of drug-resistant colorectal cancer cells. BMC Cancer. 2015 May 16;15:411.|[5]Yumiko Sekiya, et al. Facilitation of morphine withdrawal symptoms and morphine-induced conditioned place preference by a glutamate transporter inhibitor DL-threo-beta-benzyloxyaspartate in rats. Eur J Pharmacol. 2004 Feb 6;485(1-3):201-10.
• Shipping Conditions: Room Temperature
• Storage Conditions: -20°C, 3 years; 4°C, 2 years (Powder)
• Clinical Information: No Development Reported