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DL-TBOA

Catalog No. T11055   CAS 205309-81-5

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.

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DL-TBOA Chemical Structure
DL-TBOA, CAS 205309-81-5
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Biological Description
Chemical Properties
Storage & Solubility Information
Description 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.
Targets&IC50 EAAT2:6 μM , EAAT3:6 μM , EAAT5:3.2 μM , EAAT1:70 μM , EAAT4:4.4 μM , EAAT1 (human):(ki)42 μM , EAAT2 (human):5.7 μM
In vitro DL-TBOA reversed the loss of viability caused by oxaliplatin. DL-TBOA (350 μM; 24 hours; HCT116 and LoVo cell lines) treatment can reduce the induction of p53 by SN38 and oxaliplatin. DL-TBOA (70-350 μM; 48 hours; HCT116 and LoVo cell lines) treatment concentration-dependently enhanced SN38-induced loss of vitality.
Molecular Weight 239.22
Formula C11H13NO5
CAS No. 205309-81-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

TargetMolReferences and Literature

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.

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Keywords

DL-TBOA 205309-81-5 Metabolism transporter DLTBOA DL TBOA inhibitor inhibit

 

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