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Submit ReviewL-161,982
说明： Selective EP4 receptor antagonist
化学名： N-[[4'-[[3-Butyl-1,5-dihydro-5-oxo-1-[2-(trifluoromethyl)phenyl]-4H-1,2,4-triazol-4-yl]methyl][1,1'-biphenyl]-2-yl]sulfonyl]-3-methyl-2-thiophenecarboxamide
纯度： ≥99% (HPLC)
生物活性 for L-161,982
L-161,982 is an EP4 receptor antagonist that is selective over all other members of the prostanoid receptor family (Ki values are 0.024, 0.71, 1.90, 5.10, 5.63, 6.74, 19 and 23 μM for human EP4, TP, EP3, DP, FP, IP, EP1 and EP2 receptors respectively). Suppresses PGE2-induced bone formation in rats and prevents the nociceptive response induced by Misoprostol (Cat. No. 2297) in formalin-injected mice.
化合物库 for L-161,982
L-161,982 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 L-161,982
| 分子量 | 654.72 |
| 公式 | C32H29F3N4O4S2 |
| 储存 | Desiccate at +4°C |
| 纯度 | ≥99% (HPLC) |
| CAS Number | 147776-06-5 |
| PubChem ID | 9961192 |
| InChI Key | MMDNKTXNUZFVKD-UHFFFAOYSA-N |
| Smiles | CCCCC1=NN(C(=O)N1CC1=CC=C(C=C1)C1=C(C=CC=C1)S(=O)(=O)NC(=O)C1=C(C)C=CS1)C1=C(C=CC=C1)C(F)(F)F |
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 L-161,982
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 65.47 | 100 |
制备储备液 for L-161,982
以下数据基于产品分子量 654.72。 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 | 1.53 mL | 7.64 mL | 15.27 mL |
| 5 mM | 0.31 mL | 1.53 mL | 3.05 mL |
| 10 mM | 0.15 mL | 0.76 mL | 1.53 mL |
| 50 mM | 0.03 mL | 0.15 mL | 0.31 mL |
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产品说明书 for L-161,982
参考文献 for L-161,982
参考文献是支持产品生物活性的出版物。
Machwate et al (2001) Prostaglandin receptor EP4 mediates the bone anabolic effects of PGE2. Mol.Pharmacol. 60 36 PMID: 11408598
Oliva et al (2006) Role of periaqueductal grey prostaglandin receptors in formalin-induced hyperalgesia. Eur.J.Pharmacol. 530 40 PMID: 16360148
Balzary et al (2006) Lipopolysaccharide induces epithelium- and prostaglandin E2-dependent relaxation of mouse isolated trachea through activation of cyclooxygenase (COX)-1 and COX-2. J.Pharmacol.Exp.Ther. 317 806 PMID: 16464966
If you know of a relevant reference for L-161,982, please let us know.
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关键词: L-161,982, L-161,982 supplier, Selective, EP4, receptors, antagonists, Prostanoid, prostaglandins, prostacyclins, eicosanoids, L161982, Receptors, 2514, Tocris Bioscience
3 篇 L-161,982 的引用文献
引用文献是使用了 Tocris 产品的出版物。 L-161,982 的部分引用包括：
Chia et al (2011) Protection of protease-activated receptor 2 mediated vasodilatation against angiotensin II-induced vascular dysfunction in mice. BMC Pharmacol 11 10 PMID: 21955547
Sun et al (2011) Lubiprostone reverses the inhibitory action of mor. on mucosal secretion in human small intestine. Dig Dis Sci 56 330 PMID: 21181441
Guillem-Llobat et al (2016) Aspirin prevents colorectal cancer metastasis in mice by splitting the crosstalk between platelets and tumor cells. Oncotarget 7 32462 PMID: 27074574
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