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Submit ReviewRP 67580
说明： Potent and selective NK1 antagonist
化学名： (3aR,7aR)-Octahydro-2-[1-imino-2-(2-methoxyphenyl)ethyl]-7,7-diphenyl-4H-isoindol
纯度： ≥97% (HPLC)
生物活性 for RP 67580
RP 67580 is a potent and selective tachykinin NK1 receptor antagonist (Ki values are 2.9 nM and > 10 μM for rat NK1, and rat NK2 and NK3 receptors respectively). Displays higher affinity at rat and mouse than human receptors. Antinociceptive in vivo, possibly partly via inhibition of calcium channels.
化合物库 for RP 67580
RP 67580 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 RP 67580
| 分子量 | 438.57 |
| 公式 | C29H30N2O2 |
| 储存 | Store at -20°C |
| 纯度 | ≥97% (HPLC) |
| CAS Number | 135911-02-3 |
| PubChem ID | 107686 |
| InChI Key | VWBOQFANCXZMAU-LOSJGSFVSA-N |
| Smiles | [H][C@@]13[C@@](CN(C(CC4=C(OC)C=CC=C4)=N)C3)([H])C(CCC(C5=CC=CC=C5)1C2=CC=CC=C2)=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 RP 67580
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| ethanol | 43.86 | 100 | |
| DMSO | 21.93 | 50 |
制备储备液 for RP 67580
以下数据基于产品分子量 438.57。 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 | 2.28 mL | 11.4 mL | 22.8 mL |
| 5 mM | 0.46 mL | 2.28 mL | 4.56 mL |
| 10 mM | 0.23 mL | 1.14 mL | 2.28 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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产品说明书 for RP 67580
参考文献 for RP 67580
参考文献是支持产品生物活性的出版物。
Beaujouan et al (1993) Higher potency of RP 67580, in the mouse and the rat compared with other nonpeptide and peptide tachykinin NK1 antagonists. Br.J.Pharmacol. 108 793 PMID: 7682138
Fong et al (1992) Molecular basis for the species selectivity of the neurokinin-1 receptor antagonists CP-96,345 and RP67580. J.Biol.Chem. 267 25668 PMID: 1281470
Garret et al (1991) Pharmacological properties of a potent and selective nonpeptide substance P antagonist. Proc.Natl.Acad.Sci.U.S.A. 88 10208 PMID: 1719549
Rupniak et al (1993) Antinociceptive activity of NK1 receptor antagonists: non-specific effects of racemic RP67580. Br.J.Pharmacol. 110 1607 PMID: 8306108
If you know of a relevant reference for RP 67580, please let us know.
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关键词: RP 67580, RP 67580 supplier, Potent, selective, NK1, antagonists, Tachykinin, Receptors, Neurokinin, RP67580, Receptor, 1635, Tocris Bioscience
4 篇 RP 67580 的引用文献
引用文献是使用了 Tocris 产品的出版物。 RP 67580 的部分引用包括：
Russell et al (2012) Activation of PAR(2) receptors sensitizes primary afferents and causes leukocyte rolling and adherence in the rat knee joint. Br J Pharmacol 167 1665 PMID: 22849826
Wang et al (2014) Innervation of enteric mast cells by primary spinal afferents in guinea pig and human small intestine. Am J Physiol Gastrointest Liver Physiol 307 G719 PMID: 25147231
Wang et al (2008) TRPV1-mediated protection against endotoxin-induced hypotension and mortality in rats. J Neurosci 294 R1517 PMID: 18337316
Zhong and Wang (2009) Protease-activated receptor 2-mediated protection of myocardial ischemia-reperfusion injury: role of transient receptor potential vanilloid receptors. Am J Physiol Regul Integr Comp Physiol 297 R1681 PMID: 19812353
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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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