JKC363
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].
Product Specifications
CAS Number
436083-30-6
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.html
Purity
99.55
Solubility
DMSO : 50 mg/mL (ultrasonic)
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
Molecular Formula
C69H91N19O16S2
Molecular Weight
1506.71
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
Blue Ice
Storage Conditions
-80°C, 2 years; -20°C, 1 year (Powder, sealed storage, away from moisture and light)
Scientific Category
Peptides
Clinical Information
No Development Reported
Isoform
MC4R
Available Sizes
Frequently Asked Questions
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