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Submit ReviewGR 203040
说明： Potent and selective NK1 antagonist
化学名： (2S,3S)-N-[[2-Methoxy-5-(1H-tetrazol-1-yl)phenyl]methyl]-2-phenyl-3-piperidinamine dihydrochloride
纯度： ≥98% (HPLC)
生物活性 for GR 203040
GR 203040 is a potent and selective NK1 receptor antagonist. Potently inhibits substance P binding to NK1 receptors (pKi = 10.1 to 10.5). Displays antiemetic activity in vivo.
许可信息
Sold for research purposes under agreement from GlaxoSmithKline
化合物库 for GR 203040
GR 203040 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 GR 203040
| 分子量 | 437.37 |
| 公式 | C20H24N6O.2HCl |
| 储存 | Store at -20°C |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 168398-02-5 |
| PubChem ID | 127944 |
| InChI Key | DZYPLFAASKBQBS-ICSRJNTNSA-N |
| Smiles | COC1=CC=C(N4N=NN=C4)C=C1CN[C@@H]2[C@H]([C@]3=CC=CC=C3)NCCC2.Cl.Cl |
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 GR 203040
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| water | 8.75 | 20 | |
| DMSO | 8.75 | 20 |
制备储备液 for GR 203040
以下数据基于产品分子量 437.37。 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 | 11.43 mL | 57.16 mL | 114.32 mL |
| 1 mM | 2.29 mL | 11.43 mL | 22.86 mL |
| 2 mM | 1.14 mL | 5.72 mL | 11.43 mL |
| 10 mM | 0.23 mL | 1.14 mL | 2.29 mL |
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产品说明书 for GR 203040
参考文献 for GR 203040
参考文献是支持产品生物活性的出版物。
Beattie et al (1995) The pharmacology of GR203040, a novel, potent and selective non-peptide tachykinin NK1 receptor antagonist. Br.J.Pharmacol. 116 3149 PMID: 8719789
Gardner et al (1995) The broad-spectrum anti-emetic activity of the novel non-peptide tachykinin NK1 receptor antagonist GR203040. Br.J.Pharmacol. 116 3158 PMID: 8719790
Ward et al (1995) Discovery of an orally bioavailable NK1 receptor antagonist, (2S,3S)-(2-methoxy-5-tetrazol-1-ylbenzyl)(2-phenylpiperidin-3-yl)amine (GR203040), with potent antiemetic activity. J.Med.Chem. 38 4985 PMID: 8544174
If you know of a relevant reference for GR 203040, please let us know.
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关键词: GR 203040, GR 203040 supplier, GR203040, potent, selective, tachykinin, NK1, receptor, antagonists, antagonism, antiemetics, Receptor, 4647, Tocris Bioscience
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该领域的文献
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*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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