Setmelanotide TFA (RM-493 TFA; BIM-22493 TFA; IRC-022493 TFA) is a selective melanocortin 4 receptor (MC4R) agonist with EC50s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively[1]. EC50: 5.8 nM (hMC1R), 5.3 nM (hMC3R), 0.27 nM (hMC4R), 0.28 nM (rMC4R), 1600 nM (hMC5R)[1]Ki:3.9 nM (hMC1R), 10 nM (hMC3R), 2.1 nM (hMC4R), 430 nM (hMC5R), 2.7 nM (rMC4R)[1]
[1]. Kumar KG, et al. Analysis of the therapeutic functions of novel melanocortin receptor agonists in MC3R- and MC4R-deficient C57BL/6J mice. Peptides. 2009 Oct;30(10):1892-900.