| Description | DL-TBOA is an inhibitor of excitatory amino acid transporter proteins, inhibiting excitatory amino acid transporter protein 1 (EAAT1), EAAT2, and EAAT3. |
| In vitro | 在 HCT116 和 LoVo 细胞系中，DL-TBOA（70μM, 350μM；48小时）能增强 SN38 诱导的细胞死亡，并对抗奥沙利铂诱导的细胞死亡[4]。 |
| In vivo | 在体重为 180-250 克的雄性 Sprague-Dawley 大鼠中，DL-TBOA（1 nM, 3 nM, 10 nM；脑室内注射）能够剂量依赖性地促进由纳洛酮（0.1 mg/kg）诱导的各种躯体症状[5]。 |
| Target activity | EAAT2:6 μM, EAAT3:6 μM, EAAT1 (human):42 μM (Ki), EAAT2 (human):5.7 μM, EAAT4:4.4 μM, EAAT1:70 μM, EAAT5:3.2 μM |
| Synonyms | DLTBOA, DL TBOA |
| molecular weight | 239.22 |
| Molecular formula | C11H13NO5 |
| CAS | 205309-81-5 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 2 mg/mL (8.36 mM), Sonication is recommended. DMSO: 100 mg/mL (418.00 mM), Sonication is recommended. |
| 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. |