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TFB-TBOA

Catalog #: 2532
13 Citations Datasheet
Catalog # Availability Size / Price Qty
2532/1
2532/10
TFB-TBOA | CAS No. 480439-73-4 | Glutamate (EAAT) Transporter Inhibitors
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Description: Potent and selective EAAT1 and EAAT2 blocker

Chemical Name: (3S)-3-[[3-[[4-(Trifluoromethyl)benzoyl]amino]phenyl]methoxy]-L-aspartic acid

Purity: ≥98%

Product Details
Citations (13)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

TFB-TBOA is a potent and selective glial glutamate transporter EAAT1 and EAAT2 inhibitor (IC50 values are 17, 22 and 300 nM for EAAT2, EAAT1 and EAAT3, respectively). Exhibits selectivity for EAAT1 and EAAT2 over EAAT4 and EAAT5, and a wide range of neuronal receptors and transporters. In HEK293 cells expressing human EAAT1, 2, and 3, TFB-TBOA exhibited selectivity for hEAAT1 and hEAAT2 over hEAAT3 (respective IC50 values are 3.6, 10, and 120 nM), while in tsA201 cells expressing rat EAAT4, [3H]-d-Asp uptake was inhibited with an IC50 of 40 nM. Attenuates glutamate-stimulated intracellular Na+ elevation in astrocytes in vitro (IC50 = 43 nM). Induces severe convulsions in vivo.

Technical Data

M.Wt:
426.35
Formula:
C19H17F3N2O6
Solubility:
Soluble to 50 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
480439-73-4

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

  1. Glial glutamate transporter and glutamine synthetase regulate GABAergic synaptic strength in the spinal dorsal horn.
    Jiang E, Yan X, Weng HR
    J. Neurochem., 2012;121(4):526-36.
  2. Functional Indicators of Glutamate Transport in Single Striatal Astrocytes and the Influence of Kir4.1 in Normal and Huntington Mice

    J Neurosci, 2016;36(18):4959-75.
  3. Retinoic acid mediates the expression of glutamate transporter-1 in rat astrocytes through genomic RXR action and non-genomic protein kinase C signaling pathway.
    Chan TJ, Her LS, Liaw HJ, Chen MC, Tzeng SF
    J. Neurochem., 2012;121(4):537-50.
  4. Inhibitory effects of (2S, 3S)-3-[3-[4-(trifluoromethyl)benzoylamino]benzyloxy]aspartate (TFB-TBOA) on the astrocytic sodium responses to glutamate.
    Bozzo and Chatton
    Brain Res., 2010;1316
  5. Physical and functional interaction of NCX1 and EAAC1 transporters leading to glutamate-enhanced ATP production in brain mitochondria.
    Magi et al.
    PLoS One, 2012;7:e34015
  6. Effects of a novel glutamate transporter blocker, (2S, 3S)-3-{3-[4-(trifluoromethyl)benzoylamino]benzyloxy}aspartate (TFB-TBOA), on activities of hippocampal neurons.
    Tsukada et al.
    Neuropharmacology, 2005;48:479
  7. Elucidation of glutamate transporter functions using selective inhibitors.
    Shimamoto and Shigeri
    CNS Agents Med.Chem., 2006;6:59
  8. Type I Interferon Receptor Signaling in Astrocytes Regulates Hippocampal Synaptic Plasticity and Cognitive Function of the Healthy CNS
    S Hosseini, K Michaelsen, G Grigoryan, C Chhatbar, U Kalinke, M Korte
    Cell Rep, 2020;31(7):107666.

Product Datasheets

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Citations for TFB-TBOA

The citations listed below are publications that use Tocris products. Selected citations for TFB-TBOA include:

13 Citations: Showing 1 - 10

  1. Loss of excitatory amino acid transporter restraint following chronic intermittent hypoxia contributes to synaptic alterations in nucleus tractus solitarii.
    Authors: Martinez Et al.
    J.Neurophysiol.  2020;123:2122
  2. Extracellular S100β Disrupts Bergman Glia Morphology and Synaptic Transmission in Cerebellar Purkinje Cells.
    Authors: Belozor Et al.
    Brain Sci  2019;9
  3. M�ller Glial Cells Participate in Retinal Waves via Glutamate Transporters and AMPA Receptors.
    Authors: Zhang Et al.
    Cell Rep  2019;27:2871
  4. Gene expression, proteome and calcium signaling alterations in immortalized hippocampal astrocytes from an Alzheimer's disease mouse model.
    Authors: Rocchio Et al.
    Cell Death Dis  2019;10:24
  5. Neural Circuit-Specialized Astrocytes: Transcriptomic, Proteomic, Morphological, and Functional Evidence.
    Authors: Chai Et al.
    Neuron  2017;95:531
  6. Structure and allosteric inhibition of excitatory amino acid transporter 1.
    Authors: Canul-Tec
    Nature  2017;
  7. Transient Oxygen/Glucose Deprivation Causes a Delayed Loss of Mitochondria and Increases Spontaneous Calcium Signaling in Astrocytic Processes.
    Authors: O'Donnell Et al.
    J Neurosci  2016;36:7109
  8. High-frequency voltage oscillations in cultured astrocytes.
    Authors: Fleischer Et al.
    PLoS One  2015;3
  9. The PRKAA1/AMPKα1 pathway triggers autophagy during CSF1-induced human monocyte differentiation and is a potential target in CMML.
    Authors: Obba Et al.
    Mol Pain  2015;11:1114
  10. PacT. induces acute pain via directly activating toll like receptor 4.
    Authors: Yan Et al.
    Physiol Rep  2015;11:10

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