JKC 363 TFA

Names

[ Name ]:
JKC 363 TFA

[Synonym ]:
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-

Biological Activity

[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.

Chemical & Physical Properties

[ Density]:
1.6±0.1 g/cm3

[ Molecular Formula ]:
C₆₉H₉₁N₁₉O₁₆S₂

[ Molecular Weight ]:
1506.708

[ Exact Mass ]:
1505.633301

[ PSA ]:
603.20000

[ LogP ]:
-3.67

[ Index of Refraction ]:
1.731

[ Storage condition ]:
-20°C

Related Compounds

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