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].

Product Specifications

UNSPSC

12352209

Target

Melanocortin Receptor

Type

Peptides

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Neurological Disease

Assay Protocol

https://www.medchemexpress.com/jkc363-tfa.html

Solubility

10 mM in DMSO

Smiles

C(C=1C=2C(NC1)=CC=CC2)[C@@H]3NC(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H](CC4=CC5=C(C=C4)C=CC=C5)NC(=O)[C@H](CC6=CN=CN6)NC(=O)[C@H](CCC(O)=O)NC(=O)CCSSC[C@@H](C(=O)N7[C@H](C(=O)N8[C@H](C(N[C@H](C(N[C@@H](CC(O)=O)C(N)=O)=O)CCCCN)=O)CCC8)CCC7)NC(=O)CNC3=O.xOC(C(F)(F)F)=O

Molecular Formula

C69H91N19O16S2.xC2HF3O2

Molecular Weight

1506.71 (free base)

References & Citations

[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.