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Submit Review(±)-J 113397 is a potent and selective NOP receptor antagonist (IC50 values are 2.3, 1400, 2200 and > 10000 nM for NOP, κ, μ and δ-opioid receptors respectively). Inhibits nociceptin/orphanin FQ-induced hyperalgesia in the mouse tail-flick test.
(±)-J 113397 is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。
分子量 | 399.57 |
公式 | C24H37N3O2 |
储存 | Desiccate at RT |
纯度 | ≥98% (HPLC) |
CAS Number | 217461-40-0 |
PubChem ID | 90488772 |
InChI Key | NLSVMRCGZVSAFK-SDNSQTLOSA-N |
Smiles | CCN1C4=C(C=CC=C4)N([C@@H]2CCN(CC3CCCCCCC3)C[C@H]2CO)C1=O.CCN5C8=C(C=CC=C8)N([C@H]6CCN(CC7CCCCCCC7)C[C@@H]6CO)C5=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.
溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
---|---|---|---|
溶解性 | |||
DMSO | 19.98 | 50 | |
ethanol | 19.98 | 50 |
以下数据基于产品分子量 399.57。 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 |
---|---|---|---|
0.5 mM | 5.01 mL | 25.03 mL | 50.05 mL |
2.5 mM | 1 mL | 5.01 mL | 10.01 mL |
5 mM | 0.5 mL | 2.5 mL | 5.01 mL |
25 mM | 0.1 mL | 0.5 mL | 1 mL |
参考文献是支持产品生物活性的出版物。
Kawamoto et al (1999) Discovery of the first potent and selective small molecule opioid receptor-like (ORL1) antagonist: 1-[(3R,4R)-1-cyclooctylmethyl-3-hydroxymethyl-4-piperidyl]-3-ethyl-1,3-dihydro-2H-benzimidazol-2-one (J-113397). J.Med.Chem. 42 5061 PMID: 10602690
Ozaki et al (2000) In vitro and in vivo pharmacological characterization of J-113397, a potent and selective non-peptidyl ORL1 receptor antagonist. Eur.J.Pharmacol. 402 45 PMID: 10940356
Marti et al (2007) The nociceptin/orphanin FQ receptor antagonist J-113397 and L-DOPA additively attenuate experimental Parkinsonism through overinhibition of nigrothalamic pathway. J.Neurosci. 27 1297 PMID: 17287504
If you know of a relevant reference for (±)-J 113397, please let us know.
关键词: (±)-J 113397, (±)-J 113397 supplier, Potent, selective, NOP, antagonists, Nociceptin, Receptors, ORL1, OP4, Opioid, J113397, 2598, Tocris Bioscience
引用文献是使用了 Tocris 产品的出版物。 (±)-J 113397 的部分引用包括:
Wen et al (2011) Pharmacological mechanisms underlying the antinociceptive and tolerance effects of the 6,14-bridged oripavine compound 030418. Acta Pharmacol Sin 32 1215 PMID: 21863064
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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!
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Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.