Chemical Name: α-Methyl-3-phenoxybenzeneacetic acid hemicalcium salt
Biological ActivityFenoprofen 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Fenoprofen-an old drug rediscovered as a biased allosteric enhancer for melanocortin receptors.
Yuan et al.
ACS Chem.Neurosci., 2019;10:1066
Old drugs with new skills: fenoprofen as an allosteric enhancer at melanocortin receptor 3
Montero-Melendez et al.
Cell Mol.Life Sci., 2017;74:1335
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