SNT-207707 is a selective, potent and orally active melanocortin MC-4 receptor antagonist with an IC50 of 8 nM (binding) and 5 nM (function) on the MC-4 receptor.
JKC363, 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). JKC-363 blocks the stimulatory effect of α-MSH on TRH release. Anti-hyperalgesic effect[1][2].
ACTH (7-38) (human) is the 7-38 fragment of human ACTH (1-39). human ACTH (1-39), known as a corticotropin inhibitory peptide (CIP), is an antagonist of the ACTH receptor and has no any corticosteroid activity[1].
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].
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].
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.
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].
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].
PG-931, an analog of SHU 9119 (HY-P0227), is a potent melanocortin 4 (MC4) receptor (IC50=0.58 nM) agonist and is more selective than for the hMC3R (IC50=55 nM) or the hMC5R (IC50=2.4 nM). PG-931 can reverse haemorrhagic shock and prevent multiple organ damage in vivo[2].
HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats[1][2][3].
MK-0493 is a potent, orally active and selective agonist of the melanocortin receptor 4 (MC4R), demonstrating significant reductions in energy intake[1].
Dersimelagon is a melanocortin receptor agonist.
γ1-MSH is a melanocortin MC3 receptor agonist, with a Ki of 34 nM for the rat MC3 receptor. γ1-MSH displays ~40-fold selectivity over MC4 (Ki=1318 nM)[1].
HS024 is a selective MC4 receptor antagonist, with Kis of 0.29, 3.29, 5.45, and 18.6 nM for MC4, MC5, MC3, and MC1, respectively. HS024 increase food intake[1].
JNJ-10229570 is an antagonist of melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R), which inhibits sebaceous gland differentiation and the production of sebum-specific lipids. JNJ-10229570 inhibits the binding of 125I-NDP-α-MSH to cells expressing human MC1R and MC5R, with IC50 values of 270 nM and 200 nM, respectively.
(Nle4)-α-MSH is a synthetic analogue of α-MSH (HY-P0252), a melanocyte-stimulating hormone. (Nle4)-α-MSH reversibly darkens frog skins and also exhibits prolonged activity after heat-alkali treatment[1].
TCMCB07, a cyclic nonapeptide peptide, is an orally active and brain-penetrant melanocortin receptor 4 (MC4R) antagonist. TCMCB07 plays an important role in cachexia[1].
ACTH (1-17), an adrenocorticotropin analogue, is a potent human melanocortin 1 (MC1) receptor agonist with a Ki of 0.21 nM.
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-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].
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].