JKC363 (TFA)

JKC363 TFA, a selective melanocortin MC4 receptor antagonist, has a 90-fold higher affinity at the MC4 receptor (IC50=0.5 nM) than at the MC3 receptor (44.9 nM). JKC363 TFA blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect[1][2].

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[1]Kim MS, et al. Effects of melanocortin receptor ligands on thyrotropin-releasing hormone release: evidence for the differential roles of melanocortin 3 and 4 receptors. J Neuroendocrinol. 2002;14(4):276-282.|[2]Bellasio S, et al. Melanocortin receptor agonists and antagonists modulate nociceptive sensitivity in the mouse formalin test. Eur J Pharmacol. 2003;482(1-3):127-132.