JKC 363

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Cat.No. 3426 - JKC 363 | Mpr-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys-Pro-Pro-Lys-Asp-NH2 | CAS No. 436083-30-6
Description: Potent and selective MC4 receptor antagonist
Datasheet
Citations
Reviews
Literature

Biological Activity

Potent and selective melanocortin MC4 receptor antagonist (IC50 values are 0.5 and 44.9 nM at MC4 and MC3 respectively) that antagonizes the effects of α-MSH. Suppresses thyrotropin-releasing hormone (TRH) release, attenuates food intake and reduces formalin-induced pain in vivo.

Technical Data

M. Wt 1506.72
Formula C69H91N19O16S2
Sequence XEHXRWGCPPKD

(Modifications: Disulfide bridge between 1 - 8, X-1 = Mpr, X-4 = D-2-Nal, Asp-12 = C-terminal amide)

Storage Store at -20°C
CAS Number 436083-30-6
PubChem ID 90488844
InChI Key DBHQKXPXPFYXHK-DUOXTXSESA-N
Smiles NCCCC[C@H](NC(=O)[C@@H]1CCCN1C(=O)[C@@H]1CCCN1C(=O)[C@@H]1CSSCCC(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC2=CNC=N2)C(=O)N[C@H](CC2=CC3=CC=CC=C3C=C2)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC2=CNC3=C2C=CC=C3)C(=O)NCC(=O)N1)C(=O)N[C@@H](CC(O)=O)C(N)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solubility Soluble to 1 mg/ml in water

Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

Kim et al (2002) Effects of melanocortin receptor ligands on thyrotropin-releasing hormone release: evidence for the differential roles of melanocortin 3 and 4 receptors. J.Neuroendocrinol. 14 276 PMID: 11963824

Bellasio et al (2003) Melanocortin receptor agonists and antagonists modulate nociceptive sensitivity in the mouse formalin test. Eur.J.Pharmacol. 482 127 PMID: 14660013

Verty et al (2004) Evidence for an interaction between CB1 cannabinoid and melanocortin MCR-4 receptors in regulating food intake. Endocrinology 145 3224 PMID: 15033920


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Keywords: JKC 363, JKC 363 supplier, Potent, selective, MC4R, receptor, antagonists, Receptors, Melanocortin, JKC363, 3426, Tocris Bioscience

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