436083-30-6

436083-30-6 structure

Name: JKC 363 TFA
Chemical Name: jkc 363
CAS Number: 436083-30-6
Molecular Formula: C₆₉H₉₁N₁₉O₁₆S₂
Molecular Weight: 1506.708
Catalog: Research Areas Neurological Disease
Create Date: 2017-03-19 08:10:35
Modify Date: 2024-01-08 10:32:57
JKC363, 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). JKC-363 blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect[1][2].

Name	jkc 363
Synonyms	1-{[(4R,10S,13S,16R,19S,22S)-13-(3-Carbamimidamidopropyl)-22-(2-carboxyethyl)-19-(1H-imidazol-4-ylmethyl)-10-(1H-indol-3-ylmethyl)-16-(2-naphthylmethyl)-6,9,12,15,18,21,24-heptaoxo-1,2-dithia-5,8,11,1 ;4,17,20,23-heptaazacyclohexacosan-4-yl]carbonyl}-L-prolyl-L-prolyl-L-lysyl-L-α-asparagine L-α-Asparagine, 1-[[(4R,10S,13S,16R,19S,22S)-13-[3-[(aminoiminomethyl)amino]propyl]-22-(2-carboxyethyl)-19-(1H-imidazol-4-ylmethyl)-10-(1H-indol-3-ylmethyl)-16-(2-naphthalenylmethyl)-6,9,12,15,18, 21,24-heptaoxo-1,2-dithia-5,8,11,14,17,20,23-heptaazacyclohexacos-4-yl]carbonyl]-L-prolyl-L-prolyl-L-lysyl-

Description	JKC363, 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). JKC-363 blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect[1][2].
Related Catalog	Research Areas >> Neurological Disease Signaling Pathways >> GPCR/G Protein >> Melanocortin Receptor
References	[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.