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Submit ReviewFenoprofen calcium is a melanocortin 3 (MC3) receptor positive allosteric modulator (PAM; allosteric enhancer) (pEC50 = 8.69); decreases the EC50 of α-MSH at MC3R. Stimulates ERK1/2 activation at MC3-5R, with highest ERK1/2 activation observed at 3 and 10 μM for MC3R, 1 μM for MC4R, and 3 μM for MC5R. Exhibits biased signaling at MC3-5R, selectively activating ERK1/2 cascade but not canonical cAMP signaling. Antiarthritic.
| 分子量 | 261.31 |
| 公式 | C15H13O3.0.5Ca |
| 储存 | Store at RT |
| 纯度 | ≥98% (HPLC) |
| CAS Number | 34597-40-5 |
| PubChem ID | 64746 |
| InChI Key | VHUXSAWXWSTUOD-UHFFFAOYSA-L |
| Smiles | CC(C1=CC=CC(OC2=CC=CC=C2)=C1)C([O-])=O.CC(C3=CC=CC(OC4=CC=CC=C4)=C3)C([O-])=O.[Ca+2] |
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.
参考文献是支持产品生物活性的出版物。
Yuan et al (2019) Fenoprofen-an old drug rediscovered as a biased allosteric enhancer for melanocortin receptors. ACS Chem.Neurosci. 10 1066 PMID: 30168706
Montero-Melendez et al (2017) Old drugs with new skills: fenoprofen as an allosteric enhancer at melanocortin receptor 3 Cell Mol.Life Sci. 74 1335 PMID: 27853832
关键词: Fenoprofen calcium, Fenoprofen calcium supplier, 71720-56-4, 71720564, Melanocortin, 3, MC3, receptor, positive, allosteric, modulators, PAMs, enhancers, biased, signaling, antiarthritic, anti-inflamatory, NSAID, Receptors, 6926, Tocris Bioscience
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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.