hmc5r

Setmelanotide (RM-493) is a selective melanocortin-4 receptor agonist with EC50 values of 0.27 and 0.28 nM for human and rat MC4R. Setmelanotide enhances cAMP signaling, demonstrates functional selectivity, activates sympathetic preganglionic neurons to influence blood pressure, and is widely used to probe MC4R-MRAP2 interactions. Setmelanotide contributes to obesity-related research by modulating hunger and satiety circuits, reversing risperidone-induced weight gain in mice, and helping characterize MC4R variants in pediatric metabolic disorders. The anti-inflammatory actions of Setmelanotide in astrocytoma cells and the utility in combination with calorie restriction further highlight its broad value in metabolic and neuroendocrine research.

Setmelanotide Acetate(920014-72-8 free base) (RM-493 Acetate) is a selective agonist of melanocortin 4 receptor (MC4R)(human and rat MC4R with EC50s of 0.27 nM and 0.28 nM, respectively).

SHU 9119 acetate is a well-known antagonist of human melanocortin 3 and 4 (hMC3R, hMC4R) receptors and a partial hMC5R agonist. The IC50 values of human MC3R, MC4R and MC5R is 0.23, 0.06, and 0.09 nM respectively.

PG-931 TFA, a potent and selective agonist of the melanocortin 4 (MC4) receptor (IC50=0.58 nM) compared to the hMC3R (IC50=55 nM) and hMC5R (IC50=2.4 nM), is an analog of SHU 9119. This compound has demonstrated efficacy in reversing hemorrhagic shock and preventing multiple organ damage in vivo [2].

hMC1R agonist 1, with an EC 50 of 3 nM, exhibits at least 300-fold higher selectivity for hMC1R compared to hMC3R (EC 50 >902 nM), hMC4R (EC 50 >915 nM), and hMC5R (EC 50 >1000 nM). This compound demonstrates potential for therapeutic applications in targeting the melanocortin family [1].