Potent human MC1
receptor antagonist (IC50
= 17 nM). Also partial agonist at human MC3
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. γ
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All Tocris products are intended for laboratory research use only.
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.