Product 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].
Applications: Neuroscience-Neuromodulation
Formula: C11H13NO5
References: [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.
CAS Number: 205309-81-5
Molecular Weight: 239.23
Compound Purity: 99.60
Research Area: Neurological Disease
Solubility: DMSO : 200 mg/mL (ultrasonic)/H2O : 5 mg/mL (ultrasonic;warming;heat to 60°C)
Target: EAAT