TargetMol

DL-TBOA

Product Code:
 
TAR-T11055
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1

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Further Information

Bioactivity:
DL-TBOA inhibited [14C] glutamate uptake in COS-1 cells expressing human EAAT1 and EAAT2, with Ki values of 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. DL-TBOA is an effective non-transportable excitatory amino acid transporter inhibitor with IC50 of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter 1 (EAAT1, EAAT2 and EAAT3), respectively.
CAS:
205309-81-5
Formula:
C11H13NO5
Molecular Weight:
239.22
Pathway:
Metabolism
Purity:
0.98
SMILES:
OC([C@@H](N)[C@@H](C(O)=O)OCC1=CC=CC=C1)=O.[Relative stereochemistry]
Target:
transporter

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-?-Benzyloxyaspartic acid (DL-TBOA) differentially affects SN38- and oxaliplatin-induced death of drug-resistant colorectal cancer cells. BMC Cancer. 2015 May 16;15:411.