ACTH (1-39) is agonist of melanocortin receptor 2 (MC2R) with an EC50 of 57 pM in HeLa cells expressing the mouse receptor.

Bremelanotide acetate is a melanocortin agonist.

Melanotan I, a synthetic analog of α-MSH, is an agonist of melanocortin receptors with Ki values of 0.085, 0.4, 3.8 and 5.1 nM for MC1, MC3, MC4 and MC5 receptors respectively.

Melanotan II, an analog of α-melanocyte stimulating hormone, is agonist of MC3-R/MC4-R melanocortin that induces melanogenesis and thus increases skin pigmentation.

THIQ is the first selective agonist of the melanocortin-4 receptor (MC4R), with high affinity and potency for hMC4R (IC50=1.2 nM, EC50=2.1 nM) and rMC4R (IC50=0.6 nM, EC50=2.9 nM). THIQ maintains low potency at MC1R, MC3R and MC5R. THIQ plays a role in eliciting erectile activity in rodents. THIQ acts as a pharmacoperone of the MC4R rescuing the cell surface expression and signaling of some intracellularly retained MC4R mutants .

(-)-Isodocarpin is a natural product isolated and purified from the herbs of Isodon japonicus.