SHU9119

SHU9119 is a synthetic cyclic heptapeptide that acts as a potent antagonist of the human melanocortin 3 and 4 receptors (MC3R and MC4R), with IC50 values of approximately 0.23 nM for MC3R and 0.06 nM for MC4R. It also functions as a partial agonist at the melanocortin 5 receptor (MC5R) with an EC50 of about 0.12 nM[1][2][6]. Mechanistically, by antagonizing MC3R and MC4R, it increases food intake, body weight, fat mass, promotes lipogenesis and triglyceride storage genes (such as SCD1, LPL, ACCα, FAS), increases triglyceride synthesis, and induces insulin resistance when administered centrally in vivo[2][6]. The compound was developed through modifications to MTII analogs to achieve selective antagonism at these receptors[3]. Its primary use is in research settings to study energy homeostasis and metabolic disorders such as obesity.

Other names

Ac-Nle(4)-c(Asp(5)-2'-Nal(7)-Lys(10))alpha-MSH(4-10)-NH2acetyl-norisoleucyl(4)-cyclo(aspartyl(5)-2'-naphthylalanyl(7)-lysyl(10))alpha-MSH(4-10)-amide