Cat. No. 3426
Biological ActivityPotent and selective melanocortin MC4 receptor antagonist (IC50 values are 0.5 and 44.9 nM at MC4 and MC3 respectively) that antagonizes the effects of α-MSH. Suppresses thyrotropin-releasing hormone (TRH) release, attenuates food intake and reduces formalin-induced pain in vivo.
(Modifications: Disulfide bridge between 1 - 8, X-1 = Mpr, X-4 = D-2-Nal, Asp-12 = C-terminal amide)
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
References are publications that support the products' biological activity.
Verty et al (2004) Evidence for an interaction between CB1 cannabinoid and melanocortin MCR-4 receptors in regulating food intake. Endocrinology 145 3224. PMID: 15033920.
Bellasio et al (2003) Melanocortin receptor agonists and antagonists modulate nociceptive sensitivity in the mouse formalin test. Eur.J.Pharmacol. 482 127. PMID: 14660013.
Kim et al (2002) Effects of melanocortin receptor ligands on thyrotropin-releasing hormone release: evidence for the differential roles of melanocortin 3 and 4 receptors. J.Neuroendocrinol. 14 276. PMID: 11963824.
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Keywords: JKC 363, supplier, Potent, selective, MC4R, receptor, antagonists, Receptors, Melanocortin, JKC363, Tocris Bioscience, Melanocortin (MC) Receptor Antagonist products
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