Setmelanotide 是黑皮质素 4 受体 (MC4R) 的选择性激动剂（人和大鼠 MC4R，EC50 分别为 0.27 nM 和 0.28 nM）。

Setmelanotide is a selective agonist of melanocortin 4 receptor (MC4R)(human and rat MC4R with EC50s of 0.27 nM and 0.28 nM, respectively).

Melanocortin receptor agonists act in the brain to regulate food intake and body weight and, independently of these actions, affect insulin sensitivity. Setmelanotide exhibits agonist activity to human and rat MC4R(human and rat MC4R with Kis of 2.1 and 2.7 nM and EC50s of 0.27 and 0.28 nM, respectively)[1].

Inhibition of refeeding after an overnight fast by BIM-22493 is dependent on functional MC4R.glucose homeostasis acutely improved by BIM-22493. BIM-22493(Lepob/Lepob mice) exhibits significantly improved glucose clearance when compared to controls. Chronic BIM-22493 treatment was associated with significantly lower levels of serum insulin, glucose and HOMA-IR values, suggesting an improvement in insulin sensitivity[1]. Treatment with setmelanotide results in transient decreases in food intake (35%), with persistent weight loss over 8 weeks of treatment (13.5%) in a diet-induced obese nonhuman primate model[2].

920014-72-8

C49H68N18O9S2

1117.31

RM-493;IRC-022493;BIM-22493

DMSO:100 mg/mL (89.50 mM),Need ultrasonic
H2O:100 mg/mL (89.50 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years