Dersimelagon is an agonist of melanocortin receptor 1 (MC1R). It selectively induces cAMP accumulation in HEK293 cells expressing human MC1R (EC50 = 8.16 nM) over HEK293 cells expressing human MC2R (EC50 = >10,000 nM) but also induces cAMP accumulation in HEK293 cells expressing human MC4R (EC50 = 79.6 nM)....

Description: Dersimelagon (MT-7117) is an orally active, selective agonist for the melanocortin 1 receptor (MC1R), with EC50 values of 8.16 nM (h), 3.91 nM (cm), 1.14 nM (m), and 0.251 nM (r) in human, cynomolgus monkey, mouse, and rat, respectively. It exhibits strong affinity for human MC1R and MC4R, with Ki...