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-N2309
    Kainic acid
    		Agonist 99.96%
    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.
    Kainic acid
  • HY-B1102
    Evans Blue
    		99.86%
    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.
    Evans Blue
  • HY-107522
    DL-TBOA
    		Inhibitor 99.54%
    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.
    DL-TBOA
  • HY-10914
    UCPH-101
    		98.61%
    UCPH-101 is an excitatory amino acid transporter subtype 1 (EAAT1) inhibitor with an IC50 of 0.66 μM.
    UCPH-101
  • HY-12741
    LDN-212320
    		Activator 98.92%
    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]
    LDN-212320
  • HY-182941
    Parawixin10
    Parawixin10 (Compound 2) is an N-acylpolyamine. Parawixin10 fails to enhance glutamate uptake in radioligand uptake assays of EAAT1, EAAT2 or EAAT3. Parawixin10 exhibits no positive allosteric modulatory activity in radioligand uptake assays of EAAT1−EAAT3, nor can it improve neuronal survival rates in mice in a dose-dependent and statistically significant manner. Parawixin10 has no neuroprotective activity.
    Parawixin10
  • HY-182601
    MC-100093
    		Activator
    MC-100093 is an orally active, blood-brain barrier-permeable GLT-1 expression upregulator. MC-100093 upregulates the expression of GLT-1 and xCT in rats, and alleviates fentanyl-induced GLT-1 downregulation, IL-6 upregulation and motor hyperactivity. MC-100093 upregulates GLT-1 expression and enhances glutamate uptake in astrocyte-neuron co-culture systems. MC-100093 reduces ethanol consumption and preference, and exerts gender-specific antidepressant-like effects. MC-100093 can be used in studies related to fentanyl overdose, mood disorders and alcohol use disorders.
    MC-100093
  • HY-183588
    HCM-01
    		Activator
    HCM-01 is an Excitatory amino acid transporter 2 (EAAT2) activator with oral effectiveness and blood-brain barrier penetration.HCM-01 binds to the allosteric site of EAAT2, increases EAAT2 expression in astrocytes, enhances glutamate-handling capacity, and modulates glutamate homeostasis.HCM-01 acts as an antioxidant, improves oxidative/antioxidative balance and increases total antioxidant capacity. HCM-01 can be used for the research of Alzheimer's disease.
    HCM-01
  • HY-107521
    TFB-TBOA
    		Inhibitor 99.96%
    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.
    TFB-TBOA
  • HY-100784
    Dihydrokainic acid
    		Inhibitor 99.0%
    Dihydrokainic acid is a glutamate transporters (especially GLT1) inhibitor. Dihydrokainic acid targets GLT1 with high affinity, effectively inhibiting its transport function. Dihydrokainic acid exerts its effect by inhibiting the uptake of glutamate, leading to an increase in extracellular glutamate concentration, thereby affecting neuronal excitability and neurotransmission. Dihydrokainic acid is mainly applied in the field of neuroscience for research on glutamate-related neural functions, epilepsy, learning, and memory.
    Dihydrokainic acid
  • HY-B1190
    Cefadroxil
    		Activator 99.54%
    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
  • HY-107523A
    WAY-213613 hydrochloride
    		Inhibitor 99.78%
    WAY-213613 (hydrochloride) 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.
    WAY-213613 hydrochloride
  • HY-107661
    Arundic Acid
    		Activator 98.0%
    Arundic Acid is an orally effective astrocyte function modulator and neuroprotective agent. Arundic Acid increases the expression and function of the astrocytic glutamate transporter EAAT1 by activating the ERK, Akt and NF-κB pathways. Arundic Acid attenuates retinal ganglion cell death in a normal-tension glaucoma model. Arundic Acid exerts neuroprotective effects in a mouse model of Parkinson's disease. Arundic Acid is a S100β protein synthesis inhibitor that prevents neurological deficits and brain tissue damage after intracerebral hemorrhage in rats. Arundic Acid downregulates neuroinflammation and astrocytic dysfunction after status epilepticus in immature rats. Arundic Acid is applicable to research related to Parkinson's disease, cerebral ischemia, glaucoma, intracerebral hemorrhage and epilepsy.
    Arundic Acid
  • HY-107523
    WAY-213613
    		Inhibitor 99.97%
    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
    WAY-213613
  • HY-162455
    NA-014
    		Agonist 99.49%
    NA-014 is an excitatory amino acid transporter 2 (EAAT2)-selective positive allosteric modulator. NA-014 increases EAAT2-mediated glutamate uptake. NA-014 can be used for the research of epilepsy, neuropathic pain, stroke, drugs of abuse disorders.
    NA-014
  • HY-114381
    GT 949
    		Agonist 99.55%
    GT 949 is a selective excitatory amino acid transporter-2 (EAAT2) positive allosteric modulator with an EC50 of 0.26 nM.
    GT 949
  • HY-21045
    5-Fluoro-L-tryptophan
    		Inhibitor 99.99%
    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.
    5-Fluoro-L-tryptophan
  • 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-101310
    SYM 2081
    		98.0%
    SYM 2081 is a kainate receptor agonist. SYM 2081 is a substrate of EAAT1 (Km of 54 μM). SYM 2081 inhibits EAAT2-mediated glutamate transport (Kb is 3.4 μM in Xenopus oocytes), modulates Apoptotic signaling pathways (increases Bcl-2 and decreases Bax/caspase-3 expression). SYM 2081 exhibits neuroprotective activity. SYM 2081 can be used in the study of hypoxic-ischemic brain damage and inflammatory or neuropathic pain.
    SYM 2081
  • HY-W585874
    Nε-(Carboxyethyl)lysine
    		Modulator 99.9%
    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
Cat. No. Product Name / Synonyms Application Reactivity
EAAT Isoform Comparison

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