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Submit ReviewZK 200775
说明： Competitive non-NMDA iGluR antagonist
别名： MPQX
化学名： [[3,4-Dihydro-7-(4-morpholinyl)-2,3-dioxo-6-(trifluoromethyl)-1(2H)-quinoxalinyl]methyl]phosphonic acid
纯度： ≥99% (HPLC)
生物活性 for ZK 200775
ZK 200775 is a competitive AMPA/kainate antagonist. In rat cortical membranes, displays high affinity for [3H]-AMPA (Ki = 120 nM) and [3H]-CNQX (Ki = 32 nM) binding sites and low affinity for kainate and NMDA channel-associated binding sites (IC50 values range from 2.5 to 11 μM). Inhibits currents induced by AMPA, Kainate and NMDA with IC50 values of 21 nM, 27 nM, and > 1 μM respectively. Displays anxiolytic, anticonvulsant and muscle relaxant activity in vivo.
化合物库 for ZK 200775
ZK 200775 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
技术数据 for ZK 200775
| 分子量 | 409.25 |
| 公式 | C14H15N3O6F3P |
| 储存 | Desiccate at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 161605-73-8 |
| PubChem ID | 208953 |
| InChI Key | WZMQMKNCWDCCMT-UHFFFAOYSA-N |
| Smiles | OP(O)(=O)CN1C(=O)C(=O)NC2=CC(=C(C=C12)N1CCOCC1)C(F)(F)F |
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 ZK 200775
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 40.93 | 100 | |
| ethanol | 20.46 | 50 |
制备储备液 for ZK 200775
以下数据基于产品分子量 409.25。 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 | 2.44 mL | 12.22 mL | 24.43 mL |
| 5 mM | 0.49 mL | 2.44 mL | 4.89 mL |
| 10 mM | 0.24 mL | 1.22 mL | 2.44 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.49 mL |
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产品说明书 for ZK 200775
参考文献 for ZK 200775
参考文献是支持产品生物活性的出版物。
Elger et al (2005) Novel α-amino-3-hydroxy-5-methyl-4-isoxazole propionate (AMPA) receptor antagonists of 2,3-benzodiazepine type: chemical synthesis, in vitro characterization, and in vivo prevention of acute neurodegeneration. J.Med.Chem. 48 4618 PMID: 15999999
Turski et al (1998) ZK200775: a phosphonate quinoxalinedione AMPA antagonist for neuroprotection in stroke and trauman Proc.Natl.Acad.Sci.USA. 95 10960
Kosowski et al (2004) Nicotine-induced DA release in the nucleus accumbens is inhibited by the novel AMPA antagonist ZK200775 and the NMDA antagonist CGP39551n Pychopharmacology 175 114
Sobolevsky (2009) X-ray structure, symmetry and mechanism of an AMPA-subtype glutamate receptor. Nature 462 745 PMID: 19946266
If you know of a relevant reference for ZK 200775, please let us know.
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关键词: ZK 200775, ZK 200775 supplier, Competitive, AMPA/kainate, antagonists, Glutamate, Receptors, iGluR, Ionotropic, ZK200775, MPQX, AMPA, Kainate, 2345, Tocris Bioscience
1 篇 ZK 200775 的引用文献
引用文献是使用了 Tocris 产品的出版物。 ZK 200775 的部分引用包括：
Lesne et al (2005) Akt-dependent expression of NAIP-1 protects neurons against amyloid-{beta} toxicity. J Biol Chem 280 24941 PMID: 15797869
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