MC5R Antagonist

JNJ-10229570 is an antagonist of melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R), which inhibits sebaceous gland differentiation and the production of sebum-specific lipids. JNJ-10229570 inhibits the binding of ¹²⁵I-NDP-α-MSH to cells expressing human MC1R and MC5R, with IC₅₀ values of 270 nM and 200 nM, respectively.

Nonapeptide-1 (Melanostatine-5) acetate salt, a peptide hormone, is a selective antagonist of MC1R (K_i: 40 nM). Nonapeptide-1 acetate salt is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC₅₀: 2.5 nM and 11 nM, respectively). Nonapeptide-1 acetate salt inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer.

Nonapeptide-1 (Melanostatine-5), a peptide hormone, is a selective antagonist of MC1R (K_i: 40 nM). Nonapeptide-1 is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC₅₀: 2.5 nM and 11 nM, respectively). Nonapeptide-1 inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer.

Ac-c-Pro-Pro-Lys-Asp-NH2 is a selective human melanocortin 5 receptor (hMC5R) antagonist with an IC₅₀ of 10 nM.