Cat. No. 5954
Biological ActivityPotent human MC1 receptor antagonist (IC50 = 17 nM). Also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). Exhibits binding affinity for A375 melanoma cells in vitro. Reverses morphine-induced hyperalgesia in female mice, with no effect in male mice. γMSH analog.
(Modifications: X = Butanoic acid, Gly-11 = C-terminal amide, Phe-4 = D-Phe, Trp-6 = D-Trp, carba sulfide bridge between X-1 - Cys-7)
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Arout et al (2015) Spinal and supraspinal N-methyl-D-aspartate and melanocortin-1 receptors contribute to a qualitative sex difference in morphine-induced hyperalgesia. Physiol.Behav. 147 364. PMID: 25982086 .
Cai et al (2013) An unusual conformation of γ-melanocyte-stimulating hormone analogues leads to a selective human melanocortin 1 receptor antagonist for targeting melanoma cells. Biochemistry 52 752. PMID: 23276279.
Juni et al (2010) Sex-specific mediation of opioid-induced hyperalgesia by the melanocortin-1 receptor. Anesthesiology 112 181. PMID: 19996949.
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Keywords: MSG 606, supplier, MSG606, potent, MC1, receptors, melanocortin, antagonists, partial, agonists, MC3, MC5, hyperalgesia, Tocris Bioscience, Melanocortin (MC) Receptor Antagonist products
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