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Potent 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)
|Storage||Store at -20°C|
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||Soluble to 1 mg/ml in water|
References are publications that support the biological activity of the product.
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
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
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Keywords: MSG 606, MSG 606 supplier, MSG606, potent, MC1, receptors, melanocortin, antagonists, partial, agonists, MC3, MC5, hyperalgesia, Melanocortin, Receptors, 5954, Tocris Bioscience
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