| Bioactivity | 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]. |
| Name | JKC363 TFA |
| Shortening | {Mpa}-EH-{D-2-Nal}-RWGCPPKD (Disulfide bridge:Mpa1-Cys8) |
| Formula | C71H93F3N19O18S2 |
| Molar Mass | 1620.73 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [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. |