EAAT2

EAAT2 activator 1 (3-[(2-Chloro-6-fluorobenzyl)thio]-6-pyridin-2-ylpyridazine) is a thiopyridazine derivative that has been found to increase EAAT2 protein levels in astrocytes.

DL-TBOA is an inhibitor of excitatory amino acid transporter proteins, inhibiting excitatory amino acid transporter protein 1 (EAAT1), EAAT2, and EAAT3.

GT 949 is a selective excitatory positive allosteric modulator of amino acid transporter-2 (EAAT2) with an EC50 of 0.26 nM.

WAY-213613 is a potent and selective nonsubstrate reuptake inhibitor of GLT-1/EAAT2 (IC50: 85 nM EAAT2), displaying 59- and 44-fold selectivity over EAAT1 and EAAT3 (IC50s: 5 and 3.8 μM, respectively). WAY-213613 shows no activity at ionotropic and metabotropic glutamate receptors.

LDN-212320 (OSU-0212320) is a glutamate transporter EAAT2 activator. It also enhances EAAT2 levels by > 6 fold at concentrations < 5 μM after 24 h.

EAAT2 activator2 (Compound 4(SF-2)) is a brain-penetrant modulator of excitatory amino acid transporter 2 (EAAT2) with a Ki of 28.7 nM. This compound enhances EAAT2-mediated glutamate uptake and improves synaptic glutamate clearance. EAAT2 activator2 holds potential for research into neurodegenerative diseases, such as amyotrophic lateral sclerosis and Alzheimer's disease.

WAY-213613 hydrochloride is a potent, selective nonsubstrate reuptake inhibitor of GLT-1/EAAT2 with IC 50 of 85 nM. WAY-213613 hydrochloride inhibits EAAT1 and EAAT3 with IC50 values of 5 and 3.8 microM, respectively. WAY-213613 hydrochloride shows no activity at ionotropic and metabotropic glutamate receptors. It is a potential tool for the elucidation of EAAT2 function and can be used for the research of central nervous system [1] [2].

(R)-AS-1 is a selective positive allosteric modulator of excitatory amino acid transporter 2 (EAAT2), with an EC50 of 11 nM. At doses of 60 and 90 mg/kg, (R)-AS-1 enhances spontaneous locomotor activity in mice. It demonstrates anticonvulsant properties in mouse seizure models induced by maximal electroshock (MES), pentylenetetrazole (PTZ), or electric current stimulation (32 or 44 mA), with ED50 values of 66.3, 36.3, 15.6, and 41.6 mg/kg, respectively. This compound is applicable in neurological disease research.

DL-TBOA ammonium is a potent, non-transportable inhibitor of excitatory amino acid transporters. Its inhibitory effects are demonstrated by IC50 values of 70 μM, 6 μM, and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2, and EAAT3, respectively. Additionally, DL-TBOA ammonium significantly hampers the uptake of [14C]glutamate in COS-1 cell lines expressing human EAAT1 and EAAT2, evident by Ki values of 42 μM and 5.7 μM, respectively. Furthermore, this compound competitively blocks EAAT4 and EAAT5, with Ki values of 4.4 μM and 3.2 μM, respectively.

SN40 is a potent amino acid transport (AAT) inhibitor relevant for anticancer research, with Kis of 7.29 μM, 2.42 μM, 2.94 μM, 5.55 μM, 24.43 μM and 5.55 μM for human ASCT1, rat ASCT2, human ASCT2, EAAT1, EAAT2, EAAC1 and EAAT5, respectively [1].

SN05 is a potent inhibitor of amino acid transport (AAT) that can be used in anticancer research. The Ki values of SN05 for human ASCT1, rat ASCT2, human ASCT2, EAAT1, EAAT2, EAAC1 and EAAT5 is 2.77 μM, 0.73 μM, 0.87 μM, 3.7 μM, 7.25 μM, 7.23 μM and 2.22 μM, respectively [1].

NA-014 (40) is a selective positive modulator of EAAT2 with an EC50 value of 3 nM.

SLC1A1/EAAT3-IN-1 (Compound 3e) is a selective EAAT3 inhibitor with an IC50 of 7.2 μM for hEAAT3, while its IC50 values for EAAT1, EAAT2, and EAAT4 are approximately 250 μM. It is utilized in research related to psychiatric disorders such as obsessive-compulsive disorder and schizophrenia.

EAAT2(GLT1)-selective non-transportable inhibitor of L-glutamate and L-aspartate uptake

glial glutamate transporter EAAT1 and EAAT2 inhibitor

WAY-855 is an EAAT2-preferring, nonsubstrate inhibitor of high-affinity glutamate uptake.

GTS511 is a EAAT2 Activator. Pharmacokinetic profiles (PK) of GTS511 show a >6 h half-life and higher bioavailability in plasma and the brain under all three routes of administration in rats. GTS511 can be further developed to treat neurological disorders caused by excitotoxicity

GT951 is a EAAT2 activator.

GTS467 is a EAAT2 Activator.

SN40 hydrochloride is a potent DNA-PK inhibitor (IC50 = 13 nM). It sensitizes cells to radiation by blocking NHEJ repair, significantly enhancing DNA damage and cell death in cancer research.

DA-023 (Compound 4) acts as a selective positive allosteric modulator (PAM) of EAAT2, exhibiting an EC 50 value of 1 nM [1].