2. Membrane Transporter/Ion Channel
  3. EAAT

EAAT

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 Related Products (31):

Cat. No. Product Name Effect Purity
  • HY-107522
    DL-TBOA Inhibitor
    DL-TBOA 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 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 blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively[1][2][3].
  • HY-12741
    LDN-212320 Activator 99.09%
    LDN-212320 (LDN-0212320) is a glutamate transporter (GLT-1)/excitatory amino acid transporter 2 (EAAT2) activator (at translational level). LDN-212320 (LDN-0212320) prevents nociceptive pain by upregulating astroglial GLT-1 expression in the hippocampus and ACC[1][2].
  • HY-10914
    UCPH-101 99.76%
    UCPH-101 is an excitatory amino acid transporter subtype 1 (EAAT1) inhibitor with an IC50 of 0.66 μM.
  • HY-N2309
    Kainic acid Agonist
    Kainic acid is a potent excitotoxic agent. Kainic acid hydrate also is an agonist for a subtype of ionotropic glutamate receptor. Kainic acid induces seizures[1][2].
  • HY-B1102
    Evans Blue
    Evans Blue (Direct Blue 53) is a potent inhibitor of L-glutamate uptake via the membrane bound excitatory amino acid transporter (EAAT). Evans Blue is a L-glutamate and kainate receptor-mediated currents inhibitor. Evans Blue has a strong affinity towards serum albumin, making it a high molecular weight protein tracer. Evans Blue is also used to study BBB (blood-brain barrier) permeability[1][2].
  • 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[1].
  • 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[1][2].
  • HY-21045
    5-Fluoro-L-tryptophan Inhibitor
    5-Fluoro-L-tryptophan is a competitive vesicular glutamate transporter (VGLUT) inhibitor. 5-Fluoro-L-tryptophan is promising for research of diseases associated with the neurotransmitter systems[1].
  • 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[1].
  • 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[1].
  • HY-107521
    TFB-TBOA Inhibitor
    TFB-TBOA (CF3-Bza-TBOA) is a potent glutamate transporter blocker that potently suppresses the activity of glial transporters. TFB-TBOA shows IC50 values of 22, 17, and 300 nM for glutamate transporters EAAT1, EAAT2, and EAAT3 respectively in an uptake assay using cells transiently expressing EAATs[1].
  • HY-162942
    SLC7A11-IN-3 Inhibitor
    SLC7A11-IN-3 (Compound 42711_11) is an inhibitor of SLC7A11[1].
  • HY-107523
    WAY-213613 Inhibitor
    WAY-213613 is a potent and selective human EAAT2 inhibitor. WAY-213613 has potent EAAT2 inhibitory activity with an IC50 value of 85 nM. WAY-213613 can be used for the research of central nervous system[1][2]
  • HY-162455
    NA-014 Agonist 99.49%
    NA-014 (40) is a selective EAAT2 positive allosteric modulator (PAM), with an EC50 of 3 nM[1].
  • HY-W585874
    Nε-(Carboxyethyl)lysine Modulator
    Nε-(Carboxyethyl)lysine is an advanced glycation end product (AGE). Nε-(Carboxyethyl)lysine causes cross-linking between proteins, affects the structure and function of proteins, and leads to protein denaturation. Nε-(Carboxyethyl)lysine binds to RAGE receptors, affects cell signaling, regulates processes such as inflammatory response, cell proliferation and apoptosis. Nε-(Carboxyethyl)lysine affects glutamate transporter, reduces glutamate uptake and S100B protein secretion, affects neurotransmission in the nervous system, and exhibits diabetic-related neurotoxicity[1][2].
  • 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[1].
  • 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[1].
  • 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[1].
  • HY-114381
    GT 949 Agonist 99.25%
    GT 949 is a selective excitatory amino acid transporter-2 (EAAT2) positive allosteric modulator with an EC50 of 0.26 nM[1].
  • 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[1].