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说明： Potent and selective NMDA antagonist; acts at the glycine site
别名： GV 150526A
化学名： 4,6-Dichloro-3-[(1E)-3-oxo-3-(phenylamino)-1-propenyl]-1H-indole-2-carboxylic acid sodium salt
纯度： ≥98% (HPLC)
生物活性 for Gavestinel
Gavestinel is a highly potent and selective non-competitive antagonist acting at the strychnine-insensitive glycine binding site of the NMDA receptor-channel complex (Kd = 0.8 nM). Displays > 1000-fold selectivity over NMDA, AMPA and kainate binding sites. Orally bioavailable and active in vivo.
许可信息
Sold with the permission of GlaxoSmithKline
化合物库 for Gavestinel
Gavestinel 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 Gavestinel
| 分子量 | 397.19 |
| 公式 | C18H11Cl2N2O3Na |
| 储存 | Desiccate at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 153436-38-5 |
| PubChem ID | 16759177 |
| InChI Key | GRSDSTMFQHAESM-UHDJGPCESA-M |
| Smiles | [Na+].[O-]C(=O)C1=C(\C=C\C(=O)NC2=CC=CC=C2)C2=C(N1)C=C(Cl)C=C2Cl |
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 Gavestinel
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 15.89 | 40 |
制备储备液 for Gavestinel
以下数据基于产品分子量 397.19。 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 |
|---|---|---|---|
| 0.4 mM | 6.29 mL | 31.47 mL | 62.94 mL |
| 2 mM | 1.26 mL | 6.29 mL | 12.59 mL |
| 4 mM | 0.63 mL | 3.15 mL | 6.29 mL |
| 20 mM | 0.13 mL | 0.63 mL | 1.26 mL |
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产品说明书 for Gavestinel
参考文献 for Gavestinel
参考文献是支持产品生物活性的出版物。
Di Fabio et al (1997) Substituted indole-2-carboxylates as in vivo potent antagonists acting at the strychnine-insensitive glycine binding site. J.Med.Chem. 40 841 PMID: 9083472
Mugnaini et al (2000) Receptor binding characteristics of the novel NMDA receptor glycine site antagonist [3H]GV150526A in rat cerebral cortical membranes. Eur.J.Pharmacol. 391 233 PMID: 10729363
Kajbaf et al (2003) Pharmacokinetics, metabolism and excretion of the glycine antagonist GV150526A in rat and dog. Xenobiotica. 33 415 PMID: 12745876
If you know of a relevant reference for Gavestinel, please let us know.
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关键词: Gavestinel, Gavestinel supplier, Potent, selective, glycine, site, antagonists, Orally, available, active, vivo, Glutamate, NMDA, Receptors, N-Methyl-D-Aspartate, iGluR, Ionotropic, GV150526A, GlaxoSmithKline, GSK, GV, 150526A, 2348, Tocris Bioscience
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Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*请注意，Tocris 仅会向正规科研企业/机构地址发送文献。
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