ACTH (1-17), an adrenocorticotropin analogue, is a potent human melanocortin 1 (MC1) receptor agonist with a Ki of 0.21 nM.
Terrein is a melanogenesis inhibitor[1]. Terrein induces apoptosis in breast cancer cell lines [2]. Terrein is an inhibitor of quorum sensing and c-di-GMP in Pseudomonas aeruginosa[3].
Chlorophorin is a inhibitor of Melanocortin Receptor. Chlorophorin reduces tyrosinase activity and inhibits a-melanocyte-stimulating hormone-induced melanin production in B16F10 melanoma cells[1].
MC-4R Agonist 1 is an agonist of human melanocortin-4 receptor (MC-4R), used in the research of obesity, diabetes, and sexual dysfunction.
[D-Trp8]-γ-MSH is a potent and selective agonist of melanocortin 3 (MC3) receptor, with IC50s of 6.7 nM, 600 nM and 340 nM for hMC3, hMC4 and hMC5, respectively in CHO cells. [D-Trp8]-γ-MSH could provide protection against multiple inflammatory disorders such as rheumatoid arthritis and colitis[1][2].
MSG606 is a potent human MC1 receptor antagonist (IC50=17 nM). MSG606 also partial agonist at human MC3 and MC5 receptors (EC50 values are 59 and 1300 nM, respectively). MSG606 exhibits binding affinity for A375 melanoma cells in vitro. MSG606 reverses morphine-induced hyperalgesia in female mice, with no effect in male mice.
α-MSH (free acid) is a MC3R and MC4R agonist with a 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[1].
(D-Phe7)-α-MSH is an α-MSH analogue[1].
(±)-Eriodictyol ((±)-Huazhongilexone), a flavonoid, is a potent melanogenesis inhibitor with an IC50 of 48 μM. (±)-Eriodictyol suppresses tyrosinase, TRP-1, and TRP-2 mRNA expression. (±)-Eriodictyol has strong anti-plasmin activities[1].
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[1].
(p-Iodo-Phe7)-ACTH (4-10) is a adrenocorticotrophic hormone (ACTH) derivative, which is produced and secreted by the anterior pituitary gland. (p-Iodo-Phe7)-ACTH (4-10) serves as a melanocortin (MC) receptor antagonist and inhibits α-melanocyte-stimulating hormone (α-MSH)-induced excessive grooming behavior in rats[1].
PF-00446687 is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 ± 1 nM[1]. Pf-446687 is brain penetrant[2].
SNT-207858 is a selective and orally available melanocortin MC-4 receptor antagonist with a 170-fold selectivity vs. MC-3 and a 40-fold selectivity versus MC-5. SNT-207858 has an IC50 of 8 nM (binding) and 5 nM (function) on the MC-4 receptor.
MPCI is a selective melanocortin-4 receptor antagonist.
IIIM-8 is a melanogenesis inhibitor. IIIM-8 inhibits pigment production both in vitro and in vivo without incurring any cytotoxicity in Human Adult Epidermal Melanocytes (HAEM). IIIM-8 can be used for hyperpigmentation disorders research[1].
Nonapeptide-1 (Melanostatine-5), a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer[1][2][3].
N,N′-Diferuloylputrescine is a inhibitor of pigmentation with 57% reduction. N,N′-Diferuloylputrescine significantly reduces the protein level of MITF. N,N′-Diferuloylputrescine has strong antioxidant activities as radical scavengers against reactive oxygen species[1].
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[1][2].
PG106 is a potent and selective human melanocortin 3 (hMC3) receptor antagonist (IC50=210 nM) and has noactivity at hMC4 receptors (EC50=9900 nM) and hMC5 receptor[1].
Alsactide, a heptadecapeptide analogue, is an adrenocorticotropic hormone (ACTH) agonist. Alsactide can be used in research of central nervous system[1].
ML00253764 is a selective melanocortin receptor 4 (MC4R) antagonist, can induce apoptosis by inhibiting ERK1/2 and Akt phosphorylation, and has anticancer activity[1].
Defensin NP-3A (NP-3A; Corticostatin 1) is a human granulocyte peptide, with anti-ACTH activity. Defensins are antimicrobial peptides with and cytotoxic activity[1][2].
Bremelanotide (PT-141) is an analogue of α-melanocyte-stimulating hormone (α-MSH). Bremelanotide activates the mPOA and other hypothalamic and limbic regions of the brain involved in sexual behavior. Bremelanotide can be used for researching hypoactive sexual desire disorders[1].