Excitatory amino acid transporter 2 (EAAT2) is the major glutamate transporter and functions to remove glutamate from synapses. An increase in EAAT2 protein expression and function may provide a means to prevent insufficient glutamate reuptake and consequently reduce neuronal damage. 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.


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L-CCG-IV

cis-α-(Carboxycyclopropyl)glycine (L-CCG III) is a potent, competitive glutamate uptake inhibitor. cis-α-(Carboxycyclopropyl)glycine is a substrate of glutamate transporters (GluT) (EC50: 13 μM, 2 μM for EAAT 1 and EAAT 2, respectively). cis-α-(Carboxycyclopropyl)glycine inhibits a Na+-dependent high-affinity L-glutamate uptake in glial plasmalemmal vesicles (GPV) and synaptosomes[1][2].

  • CAS Number: 117857-95-1
  • MF: C6H9NO4
  • MW: 159.14000
  • Catalog: EAAT2
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DL-TBOA

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[1][2][3].

  • CAS Number: 205309-81-5
  • MF: C11H13NO5
  • MW: 478.449
  • Catalog: EAAT2
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

LDN 212320

LDN-212320(OSU-0212320) is a glutamate transporter EAAT2 activator; enhances EAAT2 levels by > 6 fold at concentrations < 5 μM after 24 h.IC50 value: 1.83 uM(EC50) [2]Target: EAAT2 activatorin vitro: LDN/OSU-0212320 increased EAAT2 protein levels in a dose-dependent(EC50=1.83 ± 0.27 μM) and time-dependent manner. LDN/OSU-0212320 increased EAAT2 protein levels and glutamate uptake function, but did not affect EAAT1 or EAAT3 protein levels. LDN/OSU-0212320 treatment markedly prevented neuronal loss and degeneration, as assessed by MAP2 immunostaining [2]. in vivo: After a single i.p. 40-mg/kg dose of LDN/OSU-0212320, EAAT2 protein levels and associated glutamate uptake increased by approximately 1.5- to 2-fold at 2 hours and by approximately 2- to 3-fold between 8 and 24 hours after injection. Even 72 hours after injection, an approximately 1.5-fold increase in EAAT2 protein levels could still be detected (data not shown). In addition, we found that LDN/OSU-0212320–induced EAAT2 protein levels and glutamate uptake were dose dependent [2].Small-molecule activator of glutamate transporter EAAT2 translation provides neuroprotectionBy Kong, Qiongman; Chang, Ling-Chu; Takahashi, Kou; Liu, Qibing; Schulte, Delanie A.; Lai, Liching; Ibabao, Brian; Lin, Yuchen; Stouffer, Nathan; Das Mukhopadhyay, Chitra; et alFrom Journal of Clinical Investigation (2014), 124(3), 1255-1267. Structure-activity relationship study of pyridazine derivatives as glutamate transporter EAAT2 activatorsBy Xing, Xuechao; Chang, Ling-Chu; Kong, Qiongman; Colton, Craig K.; Lai, Liching; Glicksman, Marcie A.; Lin, Chien-Liang Glenn; Cuny, Gregory D. From Bioorganic & Medicinal Chemistry Letters (2011), 21(19), 5774-5777.

  • CAS Number: 894002-50-7
  • MF: C17H15N3S
  • MW: 293.38600
  • Catalog: EAAT2
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

L-Aspartic acid,3-hydroxy-, (3S)-

L-threo-3-Hydroxyaspartic acid is a potent EAAT inhibitor with Kis of 11, 19 and 14 μM for EAAT1, EAAT2 and EAAT3, respectively in HEK293 cell lines[1].

  • CAS Number: 7298-99-9
  • MF: C4H7NO5
  • MW: 149.10
  • Catalog: EAAT2
  • Density: 1.738 g/cm3
  • Boiling Point: 368.7ºCat 760 mmHg
  • Melting Point: N/A
  • Flash Point: 176.8ºC

TFB-TBOA

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[1].

  • CAS Number: 480439-73-4
  • MF: C19H17F3N2O6
  • MW: 426.34300
  • Catalog: EAAT2
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

DL-TBOA ammonium

DL-TBOA ammonium 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 ammonium 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 ammonium blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively[1][2][3].

  • CAS Number: 2093503-71-8
  • MF: C11H16N2O5
  • MW: 256.26
  • Catalog: EAAT2
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

WAY 213613

WAY-213613 is a potent, selective human EAAT2 inhibitor (IC50, 85 nM), exhibits 59- and 45-fold selectivity over human EAAT1 and EAAT3. Inhibits glutamate uptake in rat cortical synaptosomes[1].

  • CAS Number: 868359-05-1
  • MF: C16H13BrF2N2O4
  • MW: 415.19
  • Catalog: EAAT2
  • Density: 1.665g/cm3
  • Boiling Point: 565.634ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 295.885ºC

(±)-threo-3-Methylglutamic acid

(±)-threo-3-Methylglutamic acid is a potent EAAT2/4 inhibitor. (±)-threo-3-Methylglutamic acid also is an ionotropic glutamate receptor agonist. (±)-threo-3-Methylglutamic acid inhibits glutamate uptake by rod outer segments[1][2].

  • CAS Number: 63088-04-0
  • MF: C6H11NO4
  • MW: 161.15600
  • Catalog: EAAT2
  • Density: 1.329g/cm3
  • Boiling Point: 329.4ºC at 760 mmHg
  • Melting Point: N/A
  • Flash Point: 153ºC

GT 949

GT 949 is a selective excitatory amino acid transporter-2 (EAAT2) positive allosteric modulator with an EC50 of 0.26 nM[1].

  • CAS Number: 460330-27-2
  • MF: C30H37N7O2
  • MW: 527.66
  • Catalog: EAAT2
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

3-HYDROXY-4,5,6,6A-TETRAHYDRO-3AH-PYRROLO[3,4-D]ISOXAZOLE-4-CARBOXYLIC ACID

(±)-HIP-A is a non-competitive excitatory amino acid transporter (EAAT) blocker that effectively blocks Glu uptake (IC50=17-18 μM). (±)-HIP-A is also a lead compound against ischemia-induced neuronal degeneration. (±)-HIP-A can be used in the study of neurological diseases[1].

  • CAS Number: 227619-64-9
  • MF: C6H8N2O4
  • MW: 172.14
  • Catalog: EAAT2
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

HIP-B

(±)-HIP-B is a non-competitive excitatory amino acid transporter (EAAT) blocker that effectively blocks Glu uptake (IC50=17-18 μM). (±)-HIP-B is also a lead compound against ischemia-induced neuronal degeneration. (±)-HIP-B can be used in the study of neurological diseases[1].

  • CAS Number: 227619-65-0
  • MF: C6H8N2O4
  • MW: 172.14
  • Catalog: EAAT2
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

EAAT2 activator 1

EAAT2 activator 1 is the potent activator of excitatory amino acid transporter 2 (EAAT2). EAAT2 is the major glutamate transporter and functions to remove glutamate from synapses. EAAT2 activator 1 increases EAAT2 protein levels dose-dependently[1].

  • CAS Number: 892415-28-0
  • MF: C16H11ClFN3S
  • MW: 331.80
  • Catalog: EAAT2
  • Density: N/A
  • Boiling Point: N/A
  • Melting Point: N/A
  • Flash Point: N/A

Dihydrokainic acid

Dihydrokainic acid (DHK) is a glutamate transporter GLT1 (EAAT2) inhibitor. Dihydrokainic acid impairs novel object recognition (NOR) memory performance in mice. Dihydrokainic acid also shows epileptogenic effects[1].

  • CAS Number: 52497-36-6
  • MF: C10H17NO4
  • MW: 215.25
  • Catalog: EAAT2
  • Density: 1.187g/cm3
  • Boiling Point: 416.6ºC at 760mmHg
  • Melting Point: 285 °C (dec.)
  • Flash Point: N/A