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.

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.

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

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].

GTS467 is a EAAT2 Activator.

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.

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.

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].

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].

GT951 is a EAAT2 activator.

glial glutamate transporter EAAT1 and EAAT2 inhibitor

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

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

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

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

SN40 hydrochloride is a potent inhibitor of amino acid transport (AAT), exhibiting inhibitory constants (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. It is utilized in cancer research. [1]