DL-TBOA ammonium

CAS: 2093503-71-8 F: C11H16N2O5 W: 256.26

DL-TBOA ammonium is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6

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Bioactivity	DL-TBOA ammonium 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 ammonium 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 ammonium blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively[1][2][3].
Target	IC50: 70 μM (EAAT1), 6 μM (EAAT2), 6 μM (EAAT3); Ki: 42 μM (human EAAT1), 5.7 μM (human EAAT2), 4.4 μM (EAAT4), 3.2 μM (EAAT5)
Invitro	DL-TBOA ammonium (70-350 μM; 48 hours) treatment concentration-dependently enhances SN38-induced loss of viability. DL-TBOA reversed Oxaliplatin-induced loss of viability[4].DL-TBOA ammonium (350 μM; 24 hours) decreases p53 induction by SN38 and oxaliplatin[4]. Cell Viability Assay[4] Cell Line:
In Vivo	DL-TBOA ammonium (10 nmol; i.c.v.) to morphine-dependent rats significantly facilitates the expression of naloxone-precipitated somatic signs and conditioned place aversion[5]. Animal Model:
Name	DL-TBOA ammonium
CAS	2093503-71-8
Formula	C11H16N2O5
Molar Mass	256.26
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[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.

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