WAY-213613
Based on 3 publication(s) in Google Scholar
WAY-213613 is a potent and selective human EAAT2 inhibitor. WAY-213613 has potent EAAT2 inhibitory activity with an IC50 value of 85 nM. WAY-213613 can be used for the research of central nervous system
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.97%
- CAS 番号: 868359-05-1
- 分子式: C16H13BrF2N2O4
- 分子量:415.19
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
MedChemExpress(MCE)の使用を引用している文献 WAY-213613
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WB
生物活性
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EAAT2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.08 μM
Compound: 16 table 1
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Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 2
Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 2
|
[PMID: 16165356] |
| HEK293 | IC50 |
3.8 μM
Compound: 16 table 1
|
Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 3
Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 3
|
[PMID: 16165356] |
| HEK293 | IC50 |
5 μM
Compound: 16 table 1
|
Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 1
Inhibitory concentration against glutamate uptake in HEK cells expressing human Excitatory amino acid transporter 1
|
[PMID: 16165356] |
| Oocyte | IC50 |
130 nM
Compound: 16 table 1
|
Inhibitory concentration against glutamate uptake in oocytes expressing in human Excitatory amino acid transporter 2
Inhibitory concentration against glutamate uptake in oocytes expressing in human Excitatory amino acid transporter 2
|
[PMID: 16165356] |
WAY-213613 (0-100 μM) has inhibitory activity for human EAAT1, EAAT2 and EAAT3 subtype with IC50 values of 5004 nM, 85 nM and 3787 nM, respectively[1].
WAY-213613 (3, 30, 300 nM) has the inhibitory effect on synaptosomal L-[3H] glutamate uptake with Ki values of 15 nM, 41 nM and 55 nM in the presence of 3, 30 and 300 nM, respectively[1].
WAY-213613 (0-100 μM) produces a concentration-dependent
block of glutamate-induced currents in EAAT1-, EAAT2- or
EAAT3-injected oocytes, with IC50 values of 48, 0.13 and 4.0 μM, respectively[1].
WAY-213613 (0.5–50 μM) exhibits good selectivity over ionotropic receptors and EAAT2 and potent activity toward blocking NMDA-stimulated responses[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 868359-05-1
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性状 Solid
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分子量 415.19
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分子式 C16H13BrF2N2O4
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Color White to off-white
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SMILES
BrC(C=C(F)C(F)=C1)=C1OC2=CC=C(NC(C[C@H](N)C(O)=O)=O)C=C2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Nat Commun
2022 Jun 9;13(1):3329. PMID: 35680945 -
Physiol Behav
Acupuncture waggle needling alleviates spastic movement disorder in post-stroke rats via GLT-1 activation to modulate Glu/GABA-Gln cycle. [Abstract]2025 Nov 1:301:115059. PMID: 40783057 -
Ann Transl Med
Astrocytic histone deacetylase 2 facilitates delayed depression and memory impairment after subarachnoid hemorrhage by negatively regulating glutamate transporter-1. [Abstract]2020 Jun;8(11):691. PMID: 32617311
WAY-213613 purchased from MedChemExpress. Usage Cited in: Ann Transl Med. 2020 Jun;8(11):691. [Abstract]
The SAH mice are intraperitoneally administered with HDAC2 inhibitor (2 mg/kg) and GLT-1 inhibitor (WAY-213613, 1 mg/kg) two weeks after surgery once every other day. The expression of GLT-1, HDAC2, p-GluN2B and p-GluA1 in hippocampus is detected after SAH at 8 weeks.
溶剤 & 溶解度
DMSO : ≥ 100 mg/mL (240.85 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (272 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Dunlop J, et al. 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. 2005 Oct;68(4):974-82. Epub 2005 Jul 13. [Content Brief]
[2]. Simmons DA, et al. A small molecule p75NTR ligand, LM11A-31, reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression. PLoS One. 2014 Aug 25;9(8):e102136. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4085 mL | 12.0427 mL | 24.0854 mL | 60.2134 mL |
| 5 mM | 0.4817 mL | 2.4085 mL | 4.8171 mL | 12.0427 mL | |
| 10 mM | 0.2409 mL | 1.2043 mL | 2.4085 mL | 6.0213 mL | |
| 15 mM | 0.1606 mL | 0.8028 mL | 1.6057 mL | 4.0142 mL | |
| 20 mM | 0.1204 mL | 0.6021 mL | 1.2043 mL | 3.0107 mL | |
| 25 mM | 0.0963 mL | 0.4817 mL | 0.9634 mL | 2.4085 mL | |
| 30 mM | 0.0803 mL | 0.4014 mL | 0.8028 mL | 2.0071 mL | |
| 40 mM | 0.0602 mL | 0.3011 mL | 0.6021 mL | 1.5053 mL | |
| 50 mM | 0.0482 mL | 0.2409 mL | 0.4817 mL | 1.2043 mL | |
| 60 mM | 0.0401 mL | 0.2007 mL | 0.4014 mL | 1.0036 mL | |
| 80 mM | 0.0301 mL | 0.1505 mL | 0.3011 mL | 0.7527 mL | |
| 100 mM | 0.0241 mL | 0.1204 mL | 0.2409 mL | 0.6021 mL |