Setmelanotide Acetate

Setmelanotide acetate is a selective melanocortin 4 receptor (MC4R) agonist. It shows EC₅₀ values of 0.27 nM and 0.28 nM for human and rat MC4R respectively. It causes weight loss, improves hyperinsulinemia and fatty liver in diet induced obese mice. It is approved for use in chronic weight management of obesity due to proopiomelanocortin (POMC), proprotein convertase subtilisin/kexin type 1 (PCSK1), or leptin receptor (LEPR) deficiency.