SNT-207858

SNT-207858 is a selective and orally available melanocortin MC-4 receptor antagonist with a 170-fold selectivity vs. MC-3 and a 40-fold selectivity versus MC-5. SNT-207858 has an IC50 of 8 nM (binding) and 5 nM (function) on the MC-4 receptor.

Signaling Pathways >> GPCR/G Protein >> Melanocortin Receptor

Research Areas >> Metabolic Disease

Research Areas >> Cancer

IC50: 8 nM (binding, MC-4), 5 nM (function, MC-4)[1]

Subcutaneous injection or oral treatment by gavage of SNT-207858 distinctly increase food intake in healthy mice. In mice subcutaneously implanted with C26 adenocarcinoma cells, repeated oral administration (starting the day after tumor implantation) of SNT-207858 almost completely prevents tumor induced weight loss, and diminished loss of lean body mass and fat mass[1].

Mice[1] Twelve weeks old male CD-1 mice are dosed by gavage with SNT207858 at 60 mg/kg. At 1, 3, and 6 hrs post-dose, mice are euthanized and blood is collected[1].

[1]. Weyermann P, et al. Orally available selective melanocortin-4 receptor antagonists stimulate food intake and reduce cancer-induced cachexia in mice. PLoS One. 2009;4(3):e4774.

Setmelanotide | Bremelanotide Acetate | JNJ-10229570 | ACTH [1-17] | MC-4R Agonist 1 | PF-00446687 | SNT-207707 | β-MSH (human) trifluoroacetate salt