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- 详细信息
- 文献和实验
- 技术资料
- 英文名：
DL-TBOA
- CAS号：
205309-81-5
- 保质期：
1年
- 保存条件：
-20°C
- 库存：
30⁺瓶
- 供应商：
上海睿安生物19121878899
- 规格：
10mg/瓶
Tocris货号1223-10mg现货DL-TBOA上海睿安生物R&D Systems-Tocris官方正式授权代理19121878899
Tocris货号1223-50mg现货DL-TBOA上海睿安生物R&D Systems-Tocris官方正式授权代理19121878899
Description:Selective non-transportable inhibitor of EAATs
Chemical Name:DL-threo-β-Benzyloxyaspartic acid
Purity:≥98%
Biological Activity
DL-TBOA is a competitive, non-transportable blocker of excitatory amino acid transporters (IC50 values are 6 μM, 6 μM and 70 μM, for EAAT2, EAAT3 and EAAT1, respectively). DL-TBOA also inhibits EAAT4 and EAAT5 (Ki values are 4.4 μM and 3.2 μM respectively). DL-TBOA displays high selectivity for EAATs over ionotropic and metabotropic glutamate receptors. In [3H]-d-Asp uptake assays in HEK293 cells expressing human EAAT2, EAAT1 and EAAT3, Ki values are 2.2, 2.9, and 9.3 μM, respectively. In a FLIPR Membrane Potential (FMP) assay, Km values are 0.59, 1.8 and 2.8 μM for human EAAT2, EAAT3 and EAAT1, respectively. DL-TBOA augments SN 38 (Cat. No. 2684) induced colorectal cancer cell death in drug-resistant cell lines. DL-TBOA enhances synaptic activity in the frog labyrinth.Technical Data
M.Wt:239.23
Formula:C11H13NO5
Solubility:Soluble to 100mM in DMSO and to 5mM in water with gentle warming
Purity:≥98%
Storage:Desiccate at -20°C
CAS No:205309-81-5
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
- Interplay between synchronization of multivesicular release and recruitment of additional release sites support short-term facilitation at hippocampal mossy fiber to CA3 pyramidal cells synapses.
Chamberland S, Evstratova A, Toth K
J Neurosci, 2014;34(33):11032-47. - Blood glutamate EAAT2-cell grabbing therapy in cerebral ischemia
M Pérez-Mato, R Iglesias-R, A Vieites-Pr, A Dopico-Lóp, B Argibay, H Fernández-, A da Silva-C, A Pérez-Díaz, C Correa-Paz, A Günther, P Ávila-Góme, M Isabel Loz, A Baumann, J Castillo, T Sobrino, F Campos
EBioMedicine, 2018;0(0):. - Impaired K(+) binding to glial glutamate transporter EAAT1 in migraine
P Kovermann, M Hessel, D Kortzak, JC Jen, J Koch, C Fahlke, T Freilinger
Sci Rep, 2017;7(1):13913. - High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. - Alterations of gene expression and glutamate clearance in astrocytes derived from an MeCP2-null mouse model of Rett syndrome.
Okabe Y, Takahashi T, Mitsumasu C, Kosai K, Tanaka E, Matsuishi T
PLoS ONE, 2012;7(4):e35354. - Up-regulation of GLT1 reverses the deficit in cortically evoked striatal ascorbate efflux in the R6/2 mouse model of Huntington's disease.
Miller BR, Dorner JL, Bunner KD, Gaither TW, Klein EL, Barton SJ, Rebec GV
J. Neurochem., 2012;121(4):629-38. - RANTES-mediated control of excitatory amino acid release in mouse spinal cord.
Di Prisco S, Summa M, Chellakudam V, Rossi PI, Pittaluga A
J. Neurochem., 2012;121(3):428-37. - Sustained Na+/H+ exchanger activation promotes gliotransmitter release from reactive hippocampal astrocytes following oxygen-glucose deprivation.
Cengiz P, Kintner D, Chanana V, Yuan H, Akture E, Kendigelen P, Begum G, Fidan E, Uluc K, Ferrazzano P, Sun D
PLoS ONE, 2014;9(1):e84294. - Inhibition of uptake unmasks rapid extracellular turnover of glutamate of nonvesicular origin.
Jabaudon et al.
Proc.Natl.Acad.Sci.U.S.A., 1999;96:8733 - Effects of threo-β-hydroxyaspartate derivatives on excitatory amino acid transporters (EAAT4 and EAAT5).
Shigeri et al.
J.Neurochem., 2001;79:297 - DL-threo-β-benzyloxyaspartate, a potent blocker of excitatory amino acid transporters.
Shimamoto et al.
Mol.Pharmacol., 1998;53:195 - Syntheses of optically pure β-hydroxyaspartate derivatives as glutamate transporter blockers.
Shimamoto et al.
Bioorg.Med.Chem.Lett., 2000;10:2407 - The glutamate transport inhibitor DL-Threo--Benzyloxyaspartic acid (DL-TBOA) differentially affects SN38- and oxaliplatin-induced death of drug-resistant colorectal cancer cells.
Pedraz-Cuesta et al.
BMC Cancer, 2015;15:411 - Pre- and postsynaptic effects of glutamate in the frog labyrinth.
Rossi et al.
Neuroscience, 2018;385:198 - Pharmacological characterization of human excitatory amino acid transporters EAAT1, EAAT2 and EAAT3 in a fluorescence-based membrane potential assay.
Jensen and Bräuner-Osborne et al.
Biochem.Pharmacol., 2004;67:2115
Citations for DL-TBOA(部分:文献)
The citations listed below are publications that use Tocris products. Selected citations for DL-TBOA include:
59 Citations: Showing 1 - 10
- Differences in glutamate uptake between cortical regions impact neuronal NMDA receptor activation.
Authors: Romanos Et al.
Commun Biol 2019;2:127 - Pharmacological Dissection of Intrinsic Optical Signal Reveals a Functional Coupling between Synaptic Activity and Astrocytic Volume Transient.
Authors: Woo Et al.
Exp Neurobiol 2019;28:30 - Role of intraganglionic transmission in the trigeminovascular pathway.
Authors: Zhang Et al.
Mol Pain 2019;15:1744806919836570 - Novel positive allosteric modulators of glutamate transport have neuroprotective properties in an in vitro excitotoxic model.
Authors: Falcucci Et al.
ACS Chem Neurosci 2019;10:3437 - Mitochondrial Regulation of the Hippocampal Firing Rate Set Point and Seizure Susceptibility.
Authors: Styr Et al.
Neuron 2019;102:1009 - Glutamate as a potential "survival factor" in an in vitro model of neuronal hypoxia/reoxygenationinjury: leading role of the Na+/Ca2+ exchanger.
Authors: Piccirillo Et al.
Cell Death Dis 2018;9(7):731 - Pre- and postsynaptic effects of glutamate in the frog labyrinth.
Authors: Rossi
Neuroscience 2018;385:198 - Clustered Ca2+ Channels Are Blocked by Synaptic Vesicle Proton Release at Mammalian Auditory Ribbon Synapses.
Authors: Vincent Et al.
Cell Rep 2018;25:3451 - Synaptic phospholipids as a new target for cortical hyperexcitability and E/I balance in psychiatric disorders.
Authors: Thalman Et al.
Mol Psychiatry 2018;23(8):1699 - Activation of retinal glial (M�ller) cells by extracellular ATP induces pronounced increases in extracellular H+ flux.
Authors: Tchernookova Et al.
PLoS One 2018;13:e0190893
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文献和实验该产品被引用文献
Tocris货号1223-10mg现货DL-TBOA上海睿安生物R&D Systems-Tocris官方正式授权代理19121878899
Tocris货号1223-50mg现货DL-TBOA上海睿安生物R&D Systems-Tocris官方正式授权代理19121878899
Description:Selective non-transportable inhibitor of EAATs
Chemical Name:DL-threo-β-Benzyloxyaspartic acid
Purity:≥98%
Biological Activity
DL-TBOA is a competitive, non-transportable blocker of excitatory amino acid transporters (IC50 values are 6 μM, 6 μM and 70 μM, for EAAT2, EAAT3 and EAAT1, respectively). DL-TBOA also inhibits EAAT4 and EAAT5 (Ki values are 4.4 μM and 3.2 μM respectively). DL-TBOA displays high selectivity for EAATs over ionotropic and metabotropic glutamate receptors. In [3H]-d-Asp uptake assays in HEK293 cells expressing human EAAT2, EAAT1 and EAAT3, Ki values are 2.2, 2.9, and 9.3 μM, respectively. In a FLIPR Membrane Potential (FMP) assay, Km values are 0.59, 1.8 and 2.8 μM for human EAAT2, EAAT3 and EAAT1, respectively. DL-TBOA augments SN 38 (Cat. No. 2684) induced colorectal cancer cell death in drug-resistant cell lines. DL-TBOA enhances synaptic activity in the frog labyrinth.Technical Data
M.Wt:239.23
Formula:C11H13NO5
Solubility:Soluble to 100mM in DMSO and to 5mM in water with gentle warming
Purity:≥98%
Storage:Desiccate at -20°C
CAS No:205309-81-5
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
- Interplay between synchronization of multivesicular release and recruitment of additional release sites support short-term facilitation at hippocampal mossy fiber to CA3 pyramidal cells synapses.
Chamberland S, Evstratova A, Toth K
J Neurosci, 2014;34(33):11032-47. - Blood glutamate EAAT2-cell grabbing therapy in cerebral ischemia
M Pérez-Mato, R Iglesias-R, A Vieites-Pr, A Dopico-Lóp, B Argibay, H Fernández-, A da Silva-C, A Pérez-Díaz, C Correa-Paz, A Günther, P Ávila-Góme, M Isabel Loz, A Baumann, J Castillo, T Sobrino, F Campos
EBioMedicine, 2018;0(0):. - Impaired K(+) binding to glial glutamate transporter EAAT1 in migraine
P Kovermann, M Hessel, D Kortzak, JC Jen, J Koch, C Fahlke, T Freilinger
Sci Rep, 2017;7(1):13913. - High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. - Alterations of gene expression and glutamate clearance in astrocytes derived from an MeCP2-null mouse model of Rett syndrome.
Okabe Y, Takahashi T, Mitsumasu C, Kosai K, Tanaka E, Matsuishi T
PLoS ONE, 2012;7(4):e35354. - Up-regulation of GLT1 reverses the deficit in cortically evoked striatal ascorbate efflux in the R6/2 mouse model of Huntington's disease.
Miller BR, Dorner JL, Bunner KD, Gaither TW, Klein EL, Barton SJ, Rebec GV
J. Neurochem., 2012;121(4):629-38. - RANTES-mediated control of excitatory amino acid release in mouse spinal cord.
Di Prisco S, Summa M, Chellakudam V, Rossi PI, Pittaluga A
J. Neurochem., 2012;121(3):428-37. - Sustained Na+/H+ exchanger activation promotes gliotransmitter release from reactive hippocampal astrocytes following oxygen-glucose deprivation.
Cengiz P, Kintner D, Chanana V, Yuan H, Akture E, Kendigelen P, Begum G, Fidan E, Uluc K, Ferrazzano P, Sun D
PLoS ONE, 2014;9(1):e84294. - Inhibition of uptake unmasks rapid extracellular turnover of glutamate of nonvesicular origin.
Jabaudon et al.
Proc.Natl.Acad.Sci.U.S.A., 1999;96:8733 - Effects of threo-β-hydroxyaspartate derivatives on excitatory amino acid transporters (EAAT4 and EAAT5).
Shigeri et al.
J.Neurochem., 2001;79:297 - DL-threo-β-benzyloxyaspartate, a potent blocker of excitatory amino acid transporters.
Shimamoto et al.
Mol.Pharmacol., 1998;53:195 - Syntheses of optically pure β-hydroxyaspartate derivatives as glutamate transporter blockers.
Shimamoto et al.
Bioorg.Med.Chem.Lett., 2000;10:2407 - The glutamate transport inhibitor DL-Threo--Benzyloxyaspartic acid (DL-TBOA) differentially affects SN38- and oxaliplatin-induced death of drug-resistant colorectal cancer cells.
Pedraz-Cuesta et al.
BMC Cancer, 2015;15:411 - Pre- and postsynaptic effects of glutamate in the frog labyrinth.
Rossi et al.
Neuroscience, 2018;385:198 - Pharmacological characterization of human excitatory amino acid transporters EAAT1, EAAT2 and EAAT3 in a fluorescence-based membrane potential assay.
Jensen and Bräuner-Osborne et al.
Biochem.Pharmacol., 2004;67:2115
Citations for DL-TBOA(部分:文献)
The citations listed below are publications that use Tocris products. Selected citations for DL-TBOA include:
59 Citations: Showing 1 - 10
- Differences in glutamate uptake between cortical regions impact neuronal NMDA receptor activation.
Authors: Romanos Et al.
Commun Biol 2019;2:127 - Pharmacological Dissection of Intrinsic Optical Signal Reveals a Functional Coupling between Synaptic Activity and Astrocytic Volume Transient.
Authors: Woo Et al.
Exp Neurobiol 2019;28:30 - Role of intraganglionic transmission in the trigeminovascular pathway.
Authors: Zhang Et al.
Mol Pain 2019;15:1744806919836570 - Novel positive allosteric modulators of glutamate transport have neuroprotective properties in an in vitro excitotoxic model.
Authors: Falcucci Et al.
ACS Chem Neurosci 2019;10:3437 - Mitochondrial Regulation of the Hippocampal Firing Rate Set Point and Seizure Susceptibility.
Authors: Styr Et al.
Neuron 2019;102:1009 - Glutamate as a potential "survival factor" in an in vitro model of neuronal hypoxia/reoxygenationinjury: leading role of the Na+/Ca2+ exchanger.
Authors: Piccirillo Et al.
Cell Death Dis 2018;9(7):731 - Pre- and postsynaptic effects of glutamate in the frog labyrinth.
Authors: Rossi
Neuroscience 2018;385:198 - Clustered Ca2+ Channels Are Blocked by Synaptic Vesicle Proton Release at Mammalian Auditory Ribbon Synapses.
Authors: Vincent Et al.
Cell Rep 2018;25:3451 - Synaptic phospholipids as a new target for cortical hyperexcitability and E/I balance in psychiatric disorders.
Authors: Thalman Et al.
Mol Psychiatry 2018;23(8):1699 - Activation of retinal glial (M�ller) cells by extracellular ATP induces pronounced increases in extracellular H+ flux.
Authors: Tchernookova Et al.
PLoS One 2018;13:e0190893
文献支持
Tocris货号1223现货DL-TBOA上海睿安生物R&D Systems-Tocris官方正式授权代理19121878899
￥3752.01
