2. Signaling Pathways
  3. Membrane Transporter/Ion Channel
  4. EAAT

EAAT

Excitatory amino acid transporter ; Glutamate transporter;

EAAT

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Excitatory amino acid transporters or EAATs are the major transport mechanism for extracellular glutamate in the nervous system. This family of five carriers (EAAT1-5 ) not only displays an impressive ability to regulate ambient extracellular glu concentrations but also regulate the temporal and spatial profile of glu after vesicular release. This dynamic form of regulation mediates several characteristic of synaptic, perisynaptic, and spillover activation of ionotropic and metabotropic receptors. EAATs function through a secondary active, electrogenic process but also possess a thermodynamically uncoupled ligand gated anion channel activity, both of which have been demonstrated to play a role in regulation of cellular activity.

The glial glutamate transporter EAAT2 plays a major role in glutamate clearance. EAAT2 can be upregulated by transcriptional or translational activation.EAAT2 is a potential target for the prevention of excitotoxicity.

EAAT Isoform Specific Products:

EAAT Isoform Comparison
Cat. No. Product Name Effect Purity Chemical Structure
  • HY-162455
    NA-014
    		Agonist 99.49%
    NA-014 (40) is a selective EAAT2 positive allosteric modulator (PAM), with an EC50 of 3 nM.
    NA-014
  • HY-139692
    EAAT2 activator 1
    		Activator 98.91%
    EAAT2 activator 1 is the potent activator of excitatory amino acid transporter 2 (EAAT2). EAAT2 is the major glutamate transporter and functions to remove glutamate from synapses. EAAT2 activator 1 increases EAAT2 protein levels dose-dependently.
    EAAT2 activator 1
  • HY-100801
    L-threo-3-Hydroxyaspartic acid
    		98.80%
    L-threo-3-Hydroxyaspartic acid is a potent EAAT inhibitor with Kis of 11, 19 and 14 μM for EAAT1, EAAT2 and EAAT3, respectively in HEK293 cell lines.
    L-threo-3-Hydroxyaspartic acid
  • HY-146241B
    SN40 hydrochloride
    		Inhibitor 98.00%
    SN40 hydrochloride is a potent amino acid transport (AAT) inhibitor with Kis of 7.29 μM, 2.42 μM, 2.94 μM, 5.55 μM, 24.43 μM and 5.55 μM for rat ASCT2, human ASCT2, EAAT1, EAAT2, EAAC1 and EAAT5, respectively. SN40 hydrochloride can be used for researching anticancer.
    SN40 hydrochloride
  • HY-B1190R
    Cefadroxil (Standard)
    		Activator 98.85%
    Cefadroxil (Standard) is the analytical standard of Cefadroxil (HY-B1190). This product is intended for research and analytical applications. Cefadroxil is an orally active broad-spectrum cephalosporin antibiotic. Cefadroxil inhibits bacterial cell wall synthesis and enhances the expression of glutamate transporter-1. Cefadroxil is dependent on the intestinal peptide transporter PepT1 for small intestinal absorption. Cefadroxil has inhibitory and bactericidal activity against a variety of Gram-positive and Gram-negative bacteria and has analgesic effects on neuropathic pain.
    Cefadroxil (Standard)
  • HY-B1190S
    Cefadroxil-d4 hydrate
    		Activator
    Cefadroxil-d4 (hydrate) is the deuterium labeled Cefadroxil hydrate (HY-B1190A). Cefadroxil hydrate is an orally active broad-spectrum cephalosporin antibiotic. Cefadroxil hydrate inhibits bacterial cell wall synthesis and enhances the expression of glutamate transporter-1. Cefadroxil hydrate is dependent on the intestinal peptide transporter PepT1 for small intestinal absorption. Cefadroxil hydrate has inhibitory and bactericidal activity against a variety of Gram-positive and Gram-negative bacteria and has analgesic effects on neuropathic pain.
    Cefadroxil-d<sub>4</sub> hydrate
  • HY-164401
    QBS10072S
    QBS10072S is a bifunctional chemotherapeutic agent, through combination of a cytotoxin and a selective LAT1 transporter substrate. QBS10072S exhibits cytotoxicity in MDA-MB-231 cell and antitumor efficacy in mice. QBS10072S is blood-brain barrier (BBB) penetrable.
    QBS10072S
  • HY-162942
    SLC7A11-IN-3
    		Inhibitor
    SLC7A11-IN-3 (Compound 42711_11) is an inhibitor of SLC7A11.
    SLC7A11-IN-3
  • HY-B1190AR
    Cefadroxil hydrate (Standard)
    		Activator
    Cefadroxil (hydrate) (Standard) is the analytical standard of Cefadroxil hydrate (HY-B1190A). This product is intended for research and analytical applications.
    Cefadroxil hydrate (Standard)
  • HY-107524
    (±)-HIP-B
    		Inhibitor
    (±)-HIP-B is a non-competitive excitatory amino acid transporter (EAAT) blocker that effectively blocks Glu uptake (IC50=17-18 μM). (±)-HIP-B is also a lead compound against ischemia-induced neuronal degeneration. (±)-HIP-B can be used in the study of neurological diseases.
    (±)-HIP-B
  • HY-107522B
    DL-TBOA ammonium
    		Inhibitor
    DL-TBOA ammonium 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 ammonium 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 ammonium blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively.
    DL-TBOA ammonium
  • HY-100838
    cis-α-(Carboxycyclopropyl)glycine
    cis-α-(Carboxycyclopropyl)glycine (L-CCG III) is a potent, competitive glutamate uptake inhibitor. cis-α-(Carboxycyclopropyl)glycine is a substrate of glutamate transporters (GluT) (EC50: 13 μM, 2 μM for EAAT 1 and EAAT 2, respectively). cis-α-(Carboxycyclopropyl)glycine inhibits a Na+-dependent high-affinity L-glutamate uptake in glial plasmalemmal vesicles (GPV) and synaptosomes.
    cis-α-(Carboxycyclopropyl)glycine
  • HY-101227
    (±)-threo-3-Methylglutamic acid
    		Inhibitor
    (±)-threo-3-Methylglutamic acid is a potent EAAT2/4 inhibitor. (±)-threo-3-Methylglutamic acid also is an ionotropic glutamate receptor agonist. (±)-threo-3-Methylglutamic acid inhibits glutamate uptake by rod outer segments.
    (±)-threo-3-Methylglutamic acid
  • HY-162454
    DA-023
    		Modulator
    DA-023 (Compound 4) is a selective positive allosteric modulator (PAM) of EAAT2 with an EC50 value of 1 nM.
    DA-023
  • HY-100784R
    Dihydrokainic acid (Standard)
    		Inhibitor
    Dihydrokainic acid (Standard) is the analytical standard of Dihydrokainic acid. This product is intended for research and analytical applications. Dihydrokainic acid (DHK) is a glutamate transporter GLT1 (EAAT2) inhibitor. Dihydrokainic acid impairs novel object recognition (NOR) memory performance in mice. Dihydrokainic acid also shows epileptogenic effects.
    Dihydrokainic acid (Standard)
  • HY-107525
    (±)-HIP-A
    		Inhibitor
    (±)-HIP-A is a non-competitive excitatory amino acid transporter (EAAT) blocker that effectively blocks Glu uptake (IC50=17-18 μM). (±)-HIP-A is also a lead compound against ischemia-induced neuronal degeneration. (±)-HIP-A can be used in the study of neurological diseases.
    (±)-HIP-A
  • HY-B1190S2
    Cefadroxil-13C6
    		Activator
    Cefadroxil-13C6 (BL-S 578-13C6) is 13C labeled Cefadroxil (HY-B1190). Cefadroxil is an orally active broad-spectrum cephalosporin antibiotic. Cefadroxil inhibits bacterial cell wall synthesis and enhances the expression of glutamate transporter-1. Cefadroxil is dependent on the intestinal peptide transporter PepT1 for small intestinal absorption. Cefadroxil has inhibitory and bactericidal activity against a variety of Gram-positive and Gram-negative bacteria and has analgesic effects on neuropathic pain.
    Cefadroxil-<sup>13</sup>C<sub>6</sub>
  • HY-161062
    TAOA AM Ester trimethyl lock
    		Inhibitor
    TAOA AM Ester trimethyl lock is a high-affinity fluorescent prodrug-like inhibitor of the excitatory amino acid transporter (EAAT). It can penetrate the cell membrane and be activated by hydrolysis by endogenous cell esterases to form active EAAT inhibitors. TAOA AM Ester trimethyl lock can be used to study neurodegeneration and neuronal cell death.
    TAOA AM Ester trimethyl lock
  • HY-168773
    (R)-AS-1
    		Modulator
    (R)-AS-1 is a selective positive allosteric modulator of the excitatory amino acid transporter 2 (EAAT2), with an EC50 of 11 nM. (R)-AS-1 (at doses of 60 and 90 mg/kg) increases spontaneous locomotor activity in mice. Additionally, it demonstrates anticonvulsant activity in mouse models of seizures induced by maximal electroshock (MES), pentylenetetrazole (PTZ), or electrical stimuli (32 or 44 mA), with ED50s of 66.3, 36.3, 15.6, and 41.6 mg/kg, respectively. (R)-AS-1 can be used in neurological disease research.
    (R)-AS-1
Cat. No. Product Name / Synonyms Application Reactivity
EAAT Isoform Comparison

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