CCZ01048 TFA, a α-MSH analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 TFA shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 TFA is a promising candidate for PET imaging of malignant melanoma.

CCZ01048, a α-melanocyte-stimulating hormone (α-MSH) analogue, exhibits high binding affinity to melanocortin 1 receptor (MC1R) with a Ki of 0.31 nM. CCZ01048 shows rapid internalization into B16F10 melanoma cells and high in vivo stability. CCZ01048 is a promising candidate for PET imaging of malignant melanoma.

JKC363 TFA, a selective melanocortin MC4 receptor antagonist, has a 90-fold higher affinity at the MC4 receptor (IC50=0.5 nM) than at the MC3 receptor (44.9 nM). JKC363 TFA blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect.

MSG606 TFA is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 TFA also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 TFA exhibits binding affinity for A375 melanoma cells in vitro. MSG606 TFA reverses morphine-induced hyperalgesia in female mice, with no effect in male mice.

MCL0020 is a potent and selective melanocortin MC4 receptor antagonist, with an IC50 of 11.63 nM. MCL0020 dose-dependently and significantly attenuates restraint stress-induced anorexia without affecting food intake.

Setmelanotide (RM-493, BIM-22493, CAM 4072) is a cyclic peptide full agonist of melanocortin-4 receptor (MC4R) with an EC50 of 0.27 nM and a Ki of 2.1 nM.

α-MSH (free acid) is a MC3R and MC4R agonist with an EC50 of 0.16±0.09 nM and 5.6±6.8 nM, respectively. α-MSH (free acid) activates cAMP generation at MC3R and MC4R.

(EC50=3 nM). hMC1R agonist 1 shows at least 300-fold selectivity for hMC1R over hMC3R (b>EC50=902 nM), hMC4R (b>EC50=915 nM), and hMC5R (b>EC50=>1000 nM). hMC1R agonist 1 has the potential for the therapeutic intervention of melanocortin family.

A peptide, non-selective melanocortin receptor agonist for treatment for female sexual dysfunction; selectively stimulates solicitational behaviors in the female rat, without affecting lordosis, pacing, or other sexual behaviors, does not cause generalized motor activation; a peptide analogue of α-MSH.

BL-6020/979 (SNT207979) is an orally available, selective, potent MC4R antagonist with IC50 of 19 nM; weakly binds to MC-3 and MC-5 receptors with IC50 of 2.7 uM and 0.89 uM, respectively, >10,000-fold selectivity over MC-1R; demonstrates in animal models and presents a promising candidate suitable for further development towards a first-in-class treatment option for cachexia.

Resomelagon (AP1189) is a potent, orally active melanocortin receptor (MR) agonist. Resomelagon induces ERK1/2 phosphorylation and Ca2+ mobilization. Resomelagon has anti-inflammatory activity. Resomelagon can be used for obesity and chronic inflammation research.

PF-07258669 is a melanocortin-4 receptor (MC4) antagonist. PF-07258669 can be used for the research of cachexia, anorexia, or anorexia nervosa.

CRN04894 is a highly potent, selective, orally available melanocortin 2 receptor (MC2R antagonist) antagonist with Ki of 2.1 nM.

SNT-207707 (SNT207707) is a potent, selective, BBB-penetrating, and orally active melanocortin-4 (MC-4) receptor antagonist with binding/fuaction IC50 of 8/5 nM, respectively.

SNT-207858 (SNT207858) is a potent, selective, BBB-penetrating, and orally active melanocortin-4 (MC-4) receptor antagonist with binding/fuaction IC50 of 22/11 nM, respectively.

TCMCB07 is a synthetic, cyclic nonapeptide peptide antagonist of the melanocortin-4 receptor (MC4R), ameliorates cancer- and chronic kidney disease-associated cachexia.