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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.
|Storage||Store at RT|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 261.31. 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.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||3.83 mL||19.13 mL||38.27 mL|
|5 mM||0.77 mL||3.83 mL||7.65 mL|
|10 mM||0.38 mL||1.91 mL||3.83 mL|
|50 mM||0.08 mL||0.38 mL||0.77 mL|
References are publications that support the biological activity of the product.
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
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Keywords: 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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Literature in this Area
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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Peptides Involved in Appetite Modulation Scientific Review
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.