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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. 了解 Tocris 化合物库的更多信息。
分子量 | 415.19 |
公式 | C16H13BrF2N2O4 |
储存 | Desiccate at RT |
纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
1eq. NaOH | 41.51 | 100 | |
DMSO | 41.51 | 100 |
以下数据基于产品分子量 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.
浓度/溶剂体积/质量 | 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 |
参考文献是支持产品生物活性的出版物。
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.
关键词: WAY 213613, WAY 213613 supplier, Potent, non-, EAAT2, inhibitors, inhibits, Excitatory, Amino, Acid, Transporters, GLT-1, Glutamate, Monoamine, Neurotransmitter, WAY213613, 2652, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 WAY 213613 的部分引用包括:
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
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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.