β-Melanocyte Stimulating Hormone (MSH), human is a melanocortin (MC) receptor agonist.
(-)-Isodocarpin (Isodocarpin), a diterpenoid, is a potent melanogenesis inhibitor with an IC50 of 0.19 μM in B16 4A5 cells. (-)-Isodocarpin inhibits the expression of tyrosinase, tyrosine-related protein (TRP)-1, and TRP-2 mRNA[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].
Tetrapeptide-1 is a bioactive peptide with antioxidant effect and has been reported used as a cosmetic ingredient[1].
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].
Setmelanotide acetate (RM-493 acetate) is a selective melanocortin 4 receptor (MC4R) agonist with EC50s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively[1].
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.
MC-4R Agonist 2 hydrochloride (Example 1) is a MC4R agonist. MC-4R Agonist 2 hydrochloride can be used in the study of obesity, diabetes, inflammation, and erectile dysfunction[1].
MC-4R Agonist 2 (Example 1) is a MC4R agonist. MC-4R Agonist 2 can be used in the study of obesity, diabetes, inflammation, and erectile dysfunction[1].
BMS-470539 dihydrochloride is a highly potent and selective melanocortin-1 receptor (MC-1R) agonist with an IC50 of 120 nM, an EC50 of 28 nM. BMS-470539 dihydrochloride does not activate MC-3R and is a very weak partial agonist at MC-4R and MC-5R. BMS-470539 dihydrochloride has potently anti-inflammatory properties[1][2][3].
PF-07258669 is a melanocortin-4 receptor (MC4) antagonist. PF-07258669 can be used for the research of cachexia, anorexia, or anorexia nervosa[1].
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].
Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID). Fenoprofen can be used to to relieve symptoms of arthritis (osteoarthritis and rheumatoid arthritis), such as inflammation, swelling, stiffness, and joint pain. Fenoprofen is an allosteric enhancer for melanocortin receptors. Fenoprofen also increases ERK1/2 activation[1][2].
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.
Ac-DArg-c[Cys-Glu-His-DPhe-Arg-Trp-Cys]-NH 2 is a cyclic octapeptide with MC4R agonism. Ac-DArg-c[Cys-Glu-His-DPhe-Arg-Trp-Cys]-NH 2 significantly increases heart rate and blood pressure[1].
Bremelanotide Acetate is a melanocortin agonist.IC50 value:Target: melanocortinin vivo: Bremelanotide is a novel drug candidate for the treatment of male and female sexual dysfunction. Bremelanotide has shown promise in effectively treating erectile dysfunction (ED) without the cardiovascular effects found in ED drugs currently available. Bremelanotide works through a mechanism of action involving the central nervous system rather than directly on the vascular system. As a result, it may offer significant safety and efficacy benefits over currently available products.
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.
α-Melanocyte-Stimulating Hormone (MSH), amide TFA is an endogenous neuropeptide, with anti-inflammatory and antipyretic activities. α-MSH is a post-translational derivative of pro-opiomelanocortin (POMC), acts as an endogenous melanocortin receptor 4 (MC4R) agonist[1][2].
ACTH (3-24) (human, bovine, mouse, ovine, porcine, rabbit, rat) is the 3-24 fragment of adrenocorticotropic hormone (ACTH). ACTH (3-24) (human, bovine, mouse, ovine, porcine, rabbit, rat) can be used for research of a variety of diseases, including cancer, immune diseases, cardiovascular disease[1].
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].
(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].
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[1][2].
Setmelanotide (RM-493;BIM-22493;IRC-022493) is a melanocortin 4 receptor (MC4R) agonist with an EC50 of 0.27 nM for human MC4R.
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].
Melanotan I acetate is a potent non-selective melanocortin receptor (MCR) agonist. Melanotan I acetate is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH) that stimulates melanogenesis. Melanotan I acetate can induce skin tanning by mimicking the actions of a-MSH on the melanocortin type 1 receptors (MC1R) of melanocytes. Melanotan I acetate can be used for sunlight-induced skin cancers research[1][2][3].
Neuropeptide EI, rat displays functional melanin concentrating hormone (MCH)-antagonist and melanocyte-stimulating hormone (MSH) agonist activity in different behavioral paradigms[1].
Adrenocorticotropic Hormone (ACTH) (1-39), rat is a potent melanocortin 2 (MC2) receptor agonist.