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(Deamino-Cys11,D-2-Nal14,Cys18)-β-MSH (11-22) amide

CAS No.: 436083-30-6

(Deamino-Cys11,D-2-Nal14,Cys18)-β-MSH (11-22) amide also called JKC-363, a selective melanocortin MC4 receptor antagoni
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CAS 436083-30-6
Sequence 3-Mercaptopropionyl-Glu-His-D-2-Nal-Arg-Trp-Gly-Cys-Pro-Pro-Lys-Asp-NH2 (Disulfide bond)
Sequence Single 3-Mercaptopropionyl-EH-D-2-Nal-RWGCPPKD-NH2(Disulfide bond)
Molecular Formula C69H91N19O16S2
Molecular Weight 1506.73
Synonyms JKC-363
Technology Synthetic
Storage -20°C, avoid light, cool and dry place
Application Obesity Research|Pituitary & Hypothalamic Hormones
Description (Deamino-Cys11,D-2-Nal14,Cys18)-β-MSH (11-22) amide also called JKC-363, 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.
References 1.  Use of the Hmb backbone-protecting group in the synthesis of difficult sequences. R.G.Simmonds, Int. J. Pept. Protein Res., 47, 36 (1996) 2.  Evidence for an interaction between CB1 cannabinoid and melanocortin MCR-4 receptors in regulating food intake. A.N.A.Verty et al., Endocrinology, 145, 3224 (2004) 3.  Melanocortins and agouti-related protein modulate the excitability of two arcuate nucleus neuron populations by alteration of resting potassium conductances. M.A.Smith et al., J. Physiol., 578, 425 (2007) 4.  Agouti-related protein antagonizes glucocorticoid production induced through melanocortin 4 receptor activation in bovine adrenal cells: a possible autocrine control. M.Doghman et al., Endocrinology, 145, 541 (2004) 5.  Effects of melanocortin receptor ligands on thyrotropin-releasing hormone release: evidence for the differential roles of melanocortin 3 and 4 receptors. Kim MS, et al. J Neuroendocrinol. 2002;14(4):276-282. 6.  Melanocortin receptor agonists and antagonists modulate nociceptive sensitivity in the mouse formalin test. Bellasio S, et al. Eur J Pharmacol. 2003;482(1-3):127-132.