SHU9119 (trifluoroacetate salt

一种黑素皮质素受体1（MC1R）激动剂和黑素皮质素受体4（MC4R）拮抗剂（置换黑素皮质素的半数抑制浓度IC50分别为1.2纳摩尔和2.9纳摩尔）；可在表达人源MC1R的人胚肾293（HEK293）细胞中诱导环磷酸腺苷（cAMP）的生成（半数有效浓度EC50=1.11纳摩尔），但在表达人源MC4R的细胞中会抑制cAMP的生成；通过干扰大鼠体内的黑素皮质素信号传导，增加大鼠的食物摄入量、体重、脂肪量和瘦体重，同时使血糖、胰岛素和瘦素水平升高（每天脑室内注射24纳摩尔，持续7天）；可使小鼠的体重和脂肪量增加。An MC1R agonist and MC4R antagonist (IC50s = 1.2 and 2.9 nM, respectively, for displacement of melanocortin); induces cAMP formation in HEK293 cells expressing human MC1R (EC50 = 1.11 nM), but inhibits cAMP formation in cells expressing human MC4R; increases food intake, body weight, fat mass, and lean mass, with concomitant increases in blood glucose, insulin, and leptin levels via disrupted melanocortin signaling in rats (24 nmol, i.c.v. per day for seven days); increases in body weight and fat mass in mice.