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Submit ReviewJTC 801
说明： Selective NOP antagonist
化学名： N-(4-Amino-2-methyl-6-quinolinyl)-2-[(4-ethylphenoxy)methyl]benzamide hydrochloride
纯度： ≥98% (HPLC)
生物活性 for JTC 801
JTC 801 is a high affinity, selective NOP receptor antagonist (Ki = 8.2 nM). Displays approximately 12.5-, 129- and 1055-fold selectivity over human μ-, κ- and δ-opioid receptors respectively. Exhibits anti-nociceptive effects in acute pain models in vivo. Orally active.
化合物库 for JTC 801
JTC 801 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 JTC 801
| 分子量 | 447.96 |
| 公式 | C26H25N3O2.HCl |
| 储存 | Desiccate at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 244218-51-7 |
| PubChem ID | 5311339 |
| InChI Key | NQLIYKXNAXKMBL-UHFFFAOYSA-N |
| Smiles | Cl.CCC1=CC=C(OCC2=CC=CC=C2C(=O)NC2=CC3=C(N)C=C(C)N=C3C=C2)C=C1 |
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 JTC 801
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 44.8 | 100 | |
| ethanol | 8.96 | 20 |
制备储备液 for JTC 801
以下数据基于产品分子量 447.96。 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 | 2.23 mL | 11.16 mL | 22.32 mL |
| 5 mM | 0.45 mL | 2.23 mL | 4.46 mL |
| 10 mM | 0.22 mL | 1.12 mL | 2.23 mL |
| 50 mM | 0.04 mL | 0.22 mL | 0.45 mL |
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产品说明书 for JTC 801
参考文献 for JTC 801
参考文献是支持产品生物活性的出版物。
Shinkai et al (2000) 4-Aminoquinolines: novel nociceptin antagonists with analgesic activity. J.Med.Chem 43 4667 PMID: 11101358
Yamada et al (2002) Pharmacological profiles of a novel opioid receptor-like1 (ORL1) receptor antagonist, JTC-801. Br.J.Pharmacol. 135 323 PMID: 11815367
Tamai et al (2005) Anti-allodynic and anti-hyperalgesic effects of nociceptin receptor antagonist, JTC-801, in rats after spinal nerve injury and inflammation. Eur.J.Pharmacol. 510 223 PMID: 15763246
If you know of a relevant reference for JTC 801, please let us know.
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关键词: JTC 801, JTC 801 supplier, Selective, NOP, antagonists, Nociceptin, Receptors, ORL1, OP4, Opioids, JTC801, 2481, Tocris Bioscience
3 篇 JTC 801 的引用文献
引用文献是使用了 Tocris 产品的出版物。 JTC 801 的部分引用包括：
Delaney et al (2012) Role of nociceptin/orphanin FQ and NOP receptors in the response to acute and repeated restraint stress in rats. J Neuroendocrinol 24 1527 PMID: 22835008
Mahmoud et al (2010) Modulation of silent and constitutively active nociceptin/orphanin FQ receptors by potent receptor antagonists and Na+ ions in rat sympathetic neurons. Mol Pharmacol 77 804 PMID: 20159949
Zhang et al (2015) Nociceptin/orphanin FQ peptide receptor antagonist JTC-801 reverses pain and anxiety symptoms in a rat model of post-traumatic stress disorder. PLoS One 172 571 PMID: 24666365
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