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 |
|---|---|---|---|---|
|
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. |
|
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). |
|
V4751 | Kainic acid | 487-79-6 | Kainic acid is a novel and potentexcitatory amino acid and an agonist at excitatory amino acid receptorsubtypes in the CNS. |
|
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. |
|
V87147 | NA-014 | NA-014 (40) is a selective EAAT2 positive modulator with an EC50 value of 3 nM. | |
|
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. |
|
V27803 | UCPH-101 | 1118460-77-7 | UCPH-101 is an inhibitor (blocker/antagonist) of excitatory amino acid (AA) transporter subtype 1 (EAAT1) with IC50 of 0.66 μM. |
|
V74189 | WAY-213613 hydrochloride | 2450268-84-3 | WAY-213613 ( HCl) is a potent and specific inhibitor of human EAAT2. |
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