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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
An unusual conformation of γ-melanocyte-stimulating hormone analogues leads to a selective human melanocortin 1 receptor antagonist for targeting melanoma cells.
Cai et al.
Sex-specific mediation of opioid-induced hyperalgesia by the melanocortin-1 receptor.
Juni et al.
Spinal and supraspinal N-methyl-D-aspartate and melanocortin-1 receptors contribute to a qualitative sex difference in morphine-induced hyperalgesia.
Arout et al.
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