EAATs, or excitatory amino acid transporters, are the main extracellular glutamate transporters in the nervous system. In addition to demonstrating an impressive capacity to control extracellular glu concentrations in the environment, this family of five carriers (EAAT1-5) also exhibits the capacity to control the temporal and spatial profile of glu after vesicular release. Ionotropic and metabotropic receptor activation at the synaptic, perisynaptic, and spillover levels is mediated by this dynamic form of regulation. EAATs possess a thermodynamically uncoupled ligand gated anion channel activity in addition to a secondary active, electrogenic process, both of which have been shown to be important for controlling cellular activity.
In the removal of glutamate, the glial glutamate transporter EAAT2 is crucial. Transcriptional or translational activation can cause an upregulation of EAAT2. Potential targets for the treatment of excitotoxicity include EAAT2.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V104499 | (R)-AS-1 | 2506367-95-7 | (R)-AS-1 is a selective positive allosteric modulator of agonist amino acid transporter 2 (EAAT2) with EC50 of 11 nM. |
|
V74182 | (±)-HIP-A | 227619-64-9 | (±)-HIP-A is a potent, noncompetitive excitatory amino acid (AA) transporter (EAAT) blocker that effectively blocks Glu uptake (IC50=17-18 μM). |
|
V74186 | (±)-HIP-B | 227619-65-0 | (±)-HIP-B is a potent, noncompetitive excitatory amino acid (AA) transporter (EAAT) blocker that can effectively block Glu uptake (IC50=17-18 μM). |
|
V74191 | (±)-threo-3-Methylglutamic acid ((+/-)-3--Methylglutamic acid) | 63088-04-0 | (±)-threo-3-Methylglutamic acid is a potent EAAT2/4 inhibitor. |
|
V126985 | 5-Fluoro-L-tryptophan | 16626-02-1 | 5-Fluoro-L-tryptophan is a competitive inhibitor of vesicle glutamate transporter (VGLUT). |
|
V131340 | Cefadroxil-13C6 | Cefadroxil-13C6 is a 13C-labeled cefadroxil. | |
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V87148 | DA-023 | 2585643-97-4 | DA-023 (Compound 4) is a selective EAAT2 positive allosteric modulator (PAM) with EC50 of 1 nM. |
|
V74184 | DL-TBOA | 205309-81-5 | DL-TBOA is a potent, non-transportable inhibitor of excitatory amino acid (AA) transporters, with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid (AA) transporter 1 (EAAT1), EAAT2 and EAAT3, respectively. |
|
V74188 | DL-TBOA ammonium | 2093503-71-8 | DL-TBOA ammonium is a potent non-transportable excitatory amino acid (AA) transporter inhibitor (antagonist) with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid (AA) transporter 1 (EAAT1), EAAT2 and EAAT3 respectively. |
|
V74190 | EAAT2 activator 1 | 892415-28-0 | EAAT2 activator 1 is a potent activator of excitatory amino acid (AA) transporter 2 (EAAT2). |
|
V134865 | EAAT2 activator 2 | EAAT2 activator 2 is an excitatory amino acid transporter 2 (EAAT2) regulator that can cross the blood-brain barrier (Ki=28.7 nM). | |
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V74185 | L-threo-3-Hydroxyaspartic acid (L(-)-THREO-3-Hydroxyaspartic acid) | 7298-99-9 | L-threo-3-Hydroxyaspartic acid is a potent EAAT inhibitor (antagonist) with Ki of 11, 19 and 14 μM for EAAT1, EAAT2 and EAAT3 respectively in HEK293 cells. |
|
V118903 | MS-153 | 130775-79-0 | MS-153 is a glutamate transporter activator and can be used as a neuroprotective agent. |
|
V87147 | NA-014 | NA-014 (40) is a selective EAAT2 positive modulator with an EC50 value of 3 nM. | |
|
V107200 | Nε-(Carboxyethyl)lysine | 5746-03-2 | Nε-(carboxyethyl)lysine is an advanced glycation end product (AGE). |
|
V142223 | Parawixin10 | Parawixin10 is an N-acylpolyamine. | |
|
V143649 | QBS10072S dihydrochloride | 1802735-31-4 | QBS10072S dihydrochloride is a bifunctional chemotherapeutic drug that can cross the blood-brain barrier (BBB). Its molecular structure contains a LAT1 targeting domain and a cytotoxic domain. |
|
V145025 | SLC1A1/EAAT3-IN-1 | 2387446-20-8 | SLC1A1/EAAT3-IN-1 is a selective EAAT3 inhibitor with an IC50 value of 7.2 μM for hEAAT3 and approximately 250 μM for EAAT1, 2, and 4. |
|
V84452 | TAOA AM Ester trimethyl lock | ||
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V74187 | TFB-TBOA (CF3-Bza-TBOA) | 480439-73-4 | TFB-TBOA (CF3-Bza-TBOA) is a potent glutamate transporter blocker that can effectively inhibit the activity of glial transporters. |
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