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说明： Potent kainate antagonist; displays selectivity for GluK1-containing receptors
化学名： (S)-1-(2-Amino-2-carboxyethyl)-3-(2-carboxy-5-phenylthiophene-3-yl-methyl)-5-methylpyrimidine-2,4-dione
纯度： ≥98% (HPLC)
生物活性 for ACET
ACET is a potent and selective GluK1 (formerly GluR5) containing kainate receptor antagonist (IC50 = 7 nM) that displays selectivity over GluK2 (formerly GluR6) containing kainate, NMDA, AMPA and group I mGlu receptors. Reversibly blocks induction of NMDA receptor-independent long term potentiation (LTP) in vitro at nanomolar concentrations.
Please refer to IUPHAR Guide to Pharmacology for the most recent naming conventions.
技术数据 for ACET
| 分子量 | 429.45 |
| 公式 | C20H19N3O6S |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 936095-50-0 |
| PubChem ID | 16125102 |
| InChI Key | LCZDCKMQSBGXAH-AWEZNQCLSA-N |
| Smiles | O=C(C(C)=CN1C[C@@H](C(O)=O)N)N(CC2=C(C(O)=O)SC(C3=CC=CC=C3)=C2)C1=O |
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.
溶解性数据 for ACET
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 8.59 | 20 | |
| 3eq. NaOH | 4.29 | 10 |
制备储备液 for ACET
以下数据基于产品分子量 429.45。 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 |
|---|---|---|---|
| 0.2 mM | 11.64 mL | 58.21 mL | 116.43 mL |
| 1 mM | 2.33 mL | 11.64 mL | 23.29 mL |
| 2 mM | 1.16 mL | 5.82 mL | 11.64 mL |
| 10 mM | 0.23 mL | 1.16 mL | 2.33 mL |
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产品说明书 for ACET
参考文献 for ACET
参考文献是支持产品生物活性的出版物。
Dolman et al (2007) Synthesis and pharmacological characterisation of N3-substituted willardiine derivatives: role of the substituent at the 5-position of the uracil ring in the development of highly potent and selective GLUK5 kainate receptor antagonis J.Med.Chem. 50 1558 PMID: 17348638
Dargan et al (2009) ACET is a highly potent and specific kainate receptor antagonist: Characterisation and effects on hippocampal mossy fibre function. Neuropharmacology 56 121 PMID: 18789344
If you know of a relevant reference for ACET, please let us know.
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关键词: ACET, ACET supplier, Potent, antagonists, GluR5-containing, kainate, receptors, Glutamate, Kainate, Receptors, iGluR, Ionotropic, GluK1, 2728, Tocris Bioscience
2 篇 ACET 的引用文献
引用文献是使用了 Tocris 产品的出版物。 ACET 的部分引用包括：
Granger and Nicoll (2014) LTD expression is independent of glutamate receptor subtype. J Virol 6 15 PMID: 25071549
Kiyama et al (2019) Essential Roles of Tbr1 in the Formation and Maintenance of the Orientation-Selective J-RGCs and a Group of OFF-Sustained RGCs in Mouse. Cell Rep 27 900 PMID: 30995485
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