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

EAAT

Excitatory amino acid transporter ; Glutamate transporter;

EAAT

Related Products

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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-146242
    SN05
    		Inhibitor 98.03%
    SN05 is a potent amino acid transport (AAT) inhibitor with Ki values of 2.77 μM, 0.73 μM, 0.87 μM, 3.7 μM, 7.25 μM, 7.23 μM and 2.22 μM for hASCT1, rASCT2, hASCT2, EAAT1, EAAT2, EAAC1 and EAAT5, respectively. SN05 can be used in the study of cancer.
    SN05
  • HY-W585874
    Nε-(Carboxyethyl)lysine
    		Modulator 99.97%
    Nε-(Carboxyethyl) lysine is an advanced glycation end product (AGE). Nε-(Carboxyethyl) lysine induces cross-linking between proteins, thereby affecting protein structure and function and causing protein denaturation. Nε-(Carboxyethyl) lysine binds to the RAGE receptor, affects cell signal transduction, and regulates processes such as inflammatory responses, cell proliferation, and apoptosis. Nε-(Carboxyethyl) lysine affects glutamate transporters, reduces glutamate uptake and S100β protein secretion, influences neurotransmission in the nervous system, and exhibits diabetes-related neurotoxicity.
    Nε-(Carboxyethyl)lysine
  • 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-B1190A
    Cefadroxil hydrate
    		Activator 99.0%
    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 hydrate
  • HY-130125
    SLC1A1/EAAT3-IN-1
    		Inhibitor 98.63%
    SLC1A1/EAAT3-IN-1 (Compound 3e) is a selective EAAT3 inhibitor with an IC50 of 7.2  μM for hEAAT3 over EAAT1,2,4 (IC50: ∼ 250 μM). SLC1A1/EAAT3-IN-1 can be used for psychiatric disorders such as obsessive compulsive disorder and schizophrenia research.
    SLC1A1/EAAT3-IN-1
  • HY-124619
    GPI-1046
    		Inducer 99.79%
    GPI-1046 is an orally active, antibiotic-free immunophilin ligand that reduces ethanol intake by upregulating glutamate transporter 1 (GLT1) in the prefrontal cortex (PFC) and nucleus accumbens core (NAc-core). GPI-1046 improves human immunodeficiency virus (HIV)-associated sensory neuropathy (HIV-SN) by attenuating store-operated calcium (SOC) entry. GPI-1046 has neuroprotective activity.
    GPI-1046
  • HY-168773
    (R)-AS-1
    		Modulator 99.90%
    (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
  • HY-B1190R
    Cefadroxil (Standard)
    		Activator
    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-146241
    SN40
    		Inhibitor 99.26%
    SN40 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 can be used for researching anticancer.
    SN40
  • HY-162454
    DA-023
    		Modulator 98.01%
    DA-023 (Compound 4) is a selective positive allosteric modulator (PAM) of EAAT2 with an EC50 value of 1 nM.
    DA-023
  • 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-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-100801R
    L-threo-3-Hydroxyaspartic acid (Standard)
    Prilocaine (hydrochloride) (Standard) is the analytical standard of Prilocaine (hydrochloride). This product is intended for research and analytical applications. Prilocaine hydrochloride, an amino amide, is a Na/K-ATPase inhibitor. Prilocaine has neurotoxic effects.
    L-threo-3-Hydroxyaspartic acid (Standard)
  • HY-133177
    MS-153
    		Activator
    MS-153 is a glutamate transporter activator that can be used as a neuroprotective agent.
    MS-153
  • 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-164401A
    QBS10072S dihydrochloride
    QBS10072S dihydrochloride is a LAT1-selective substrate with blood-brain barrier permeability that inhibits tumor growth. QBS10072S dihydrochloride enters LAT1-expressing tumor cells via LAT1-mediated active transport, induces interstrand DNA cross-linking and cell apoptosis, and reduces leptomeningeal dissemination. QBS10072S dihydrochloride can be used in studies related to glioblastoma multiforme, diffuse intrinsic pontine glioma, triple-negative breast cancer brain metastases, and aggressive T-cell lymphoma.
    QBS10072S dihydrochloride
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
EAAT Isoform Comparison

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