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.
Shipping Conditions
Room temperature
Scientific Category
Peptides
Clinical Information
No Development Reported
Isoform
MC4R
Curated Selection
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