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DL-TBOA

CAT: 0804-HY-107522-01Size: 5 mgDry Ice: NoHazardous: No
CAT#:0804-HY-107522-01Size:5 mg
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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].
CAS Number
[205309-81-5]
UNSPSC
12352005
Hazard Statement
H302, H312, H332
Target
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
99.54
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 Formula
C11H13NO5
Molecular Weight
239.23
Precautions
H302, H312, H332
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)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
EAAT1; EAAT2; EAAT3

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