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Submit ReviewWAY 213613 is a potent, non-substrate inhibitor of EAAT2 (GLT-1) that displays > 44-fold selectivity over EAAT1 and EAAT3 (IC50 values are 85, 3787 and 5004 nM for EAAT2, EAAT3 and EAAT1 respectively). Another study has found WAY 213613 has 12 - 26-fold selectivity for EAAT2 over EAAT1, EAAT3 and EAAT4 (IC50 values are 0.071, 0.86, 1.5 and 1.9 nM for EAAT2, EAAT1, EAAT4 and EAAT3, respectively). Exhibits no activity towards ionotropic and metabotropic glutamate receptors.
WAY 213613 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
M. Wt | 415.19 |
Formula | C16H13BrF2N2O4 |
Storage | Desiccate at RT |
Purity | ≥99% (HPLC) |
CAS Number | 868359-05-1 |
PubChem ID | 11531745 |
InChI Key | BNYDDAAZMBUFRG-ZDUSSCGKSA-N |
Smiles | FC1=C(F)C=C(OC2=CC=C(NC(C[C@H](N)C(O)=O)=O)C=C2)C(Br)=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
1eq. NaOH | 41.51 | 100 | |
DMSO | 41.51 | 100 |
The following data is based on the product molecular weight 415.19. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2.41 mL | 12.04 mL | 24.09 mL |
5 mM | 0.48 mL | 2.41 mL | 4.82 mL |
10 mM | 0.24 mL | 1.2 mL | 2.41 mL |
50 mM | 0.05 mL | 0.24 mL | 0.48 mL |
References are publications that support the biological activity of the product.
Dunlop et al (2005) Characterization of novel aryl-ether, biaryl, and fluorene aspartic acid and diaminopropionic acid analogs as potent inhibitors of the high-affinity glutamate transporter EAAT2. Mol.Pharmacol. 68 974 PMID: 16014807
Beart and Shea (2007) Transporters for L-glutamate: an update on their molecular pharmacology and pathological involvement. Br.J.Pharmacol. 150 5 PMID: 17088867
Fu et al (2018) Chemoenzymatic synthesis and pharmacological characterization of functionalized aspartate analogues as novel excitatory amino acid transporter inhibitors. J.Med.Chem. 61 7741 PMID: 30011368
If you know of a relevant reference for WAY 213613, please let us know.
Keywords: WAY 213613, WAY 213613 supplier, Potent, non-, EAAT2, inhibitors, inhibits, Excitatory, Amino, Acid, Transporters, GLT-1, Glutamate, Monoamine, Neurotransmitter, WAY213613, 2652, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for WAY 213613 include:
Falcucci et al (2019) Novel positive allosteric modulators of glutamate transport have neuroprotective properties in an in vitro excitotoxic model. ACS Chem Neurosci 10 3437 PMID: 31257852
Dumont et al (2014) Differential regulation of glutamate transporter subtypes by pro-inflammatory cytokine TNF-α in cortical astrocytes from a rat model of amyotrophic lateral sclerosis. Evid Based Complement Alternat Med 9 e97649 PMID: 24836816
Brancaccio et al (2017) Astrocytes Control Circadian Timekeeping in the Suprachiasmatic Nucleus via Glutamatergic Signaling. Neuron 93 1420 PMID: 28285822
Do you know of a great paper that uses WAY 213613 from Tocris? Please let us know.
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Huntington's disease (HD) is a severe monogenic neurodegenerative disorder, which is characterized by the prevalent loss of GABAergic medium spiny neurons (MSN) in the striatum. This poster summarizes the effects of mutant huntingtin aggregation implicated in the pathology of HD, as well as highlighting the use of iPSCs for HD modeling.