Melanocortin Receptor Agonist

α-MSH (α-Melanocyte-Stimulating Hormone), an endogenous neuropeptide, is an endogenous melanocortin receptor 4 (MC4R) agonist with anti-inflammatory and antipyretic activities. α-MSH is a post-translational derivative of pro-opiomelanocortin (POMC).

Setmelanotide (RM-493) is a selective melanocortin 4 receptor (MC4R) agonist with EC₅₀s of 0.27 nM and 0.28 nM for human and rat MC4R, respectively.

Melanotan I is a potent non-selective melanocortin receptor (MCR) agonist. Melanotan I is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH) that stimulates melanogenesis. Melanotan I can induce skin tanning by mimicking the actions of a-MSH on the melanocortin type 1 receptors (MC1R) of melanocytes. Melanotan I can be used for the research of sun-induced skin cancer, melanoma, inflammation and male erectile dysfunction.

Melanotan (MT)-II is a melanocortin receptor agonist. Melanotan (MT)-II activates melanocortin receptor 3 and melanocortin receptor 4, and stimulates the release of central endogenous oxytocin. Melanotan (MT)-II reverses recognition memory impairment, increased anxiety levels and reduced exploratory tendency in zebrafish exposed to short-term high-fat diet. Melanotan (MT)-II improves impaired social behavior indicators in mouse models of autism spectrum disorder. Melanotan (MT)-II induces weight loss, reduces food intake and exerts anorectic effects. Melanotan (MT)-II increases intracavernous pressure and erectile activity in brown rats. Melanotan (MT)-II can be used in studies related to memory impairment, anxiety, reduced exploratory behavior, autism spectrum disorder, obesity and erectile dysfunction.

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.

Bremelanotide (PT-141) Acetate is a melanocortin receptor agonist. Bremelanotide Acetate can activate MC4R and increases dopamine release. Bremelanotide Acetate induces appetitive sexual behaviors, female mounting behavior, and repetitive self-grooming. Bremelanotide Acetate can be used for the research of hypoactive sexual desire disorders.

Adrenocorticotropic Hormone (ACTH) (1-39), human is a melanocortin receptor agonist.

Bivamelagon (MC-4R Agonist 2) is an orally active MC4R agonist with EC₅₀ values of 0.562 nM (Luci assay) and 36.5 nM (cAMP assay), and a K_i of 65 nM. Bivamelagon can be used for the research of diseases such as obesity and diabetes.

Dersimelagon (MT-7117) is an orally active, selective melanocortin 1 receptor (MC1R) agonist with EC₅₀ values of 8.16, 3.91, 1.14 and 0.251 nM for human (h), cynomolgus monkey (cm), mouse (m) and rat (r) MC1R, respectively. Dersimelagon shows good affinity for hMC1R and hMC4R with K_i values of 2.26, 32.9 nM, respectively. Dersimelagon can be used for the research of skin pigmentation.

PF-00446687 is a potent, selective melanocortin-4 receptor (MC4R) agonist with EC50 of 12 ± 1 nM. Pf-446687 is brain penetrant.

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.

α-MSH (α-Melanocyte-Stimulating Hormone) TFA, an endogenous neuropeptide, is an endogenous melanocortin receptor 4 (MC4R) agonist with anti-inflammatory and antipyretic activities. α-MSH TFA is a post-translational derivative of pro-opiomelanocortin (POMC).

Fenoprofen (LILLY-53858) Calcium hydrate is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen Calcium hydrate is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen Calcium hydrate also increases ERK1/2 activation in HEK293T cells. Fenoprofen Calcium hydrate has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis.

Bremelanotide (PT-141) is a melanocortin receptor agonist. Bremelanotide can activate MC4R and increases dopamine release. Bremelanotide induces appetitive sexual behaviors, female mounting behavior, and repetitive self-grooming. Bremelanotide can be used for the research of hypoactive sexual desire disorders.

Tetracosactide (Tetracosactrin) is an analogue of adrenocorticotrophic hormone (ACTH). Tetracosactide is the agonist for melanocortin-4 receptor (MC4R) that activates human MC4R with an EC₅₀ of 0.65 nM. Tetracosactide can stimulate the release of corticosteroids such as cortisol from the adrenal gland. Tetracosactide is currently used for the research of ulcerative colitis and Crohn's disease, juvenile/adult rheumatoid arthritis and osteoarthrosis.

Adrenocorticotropic hormone (1-39), rat is a potent melanocortin 2 (MC2) receptor agonist.

MK-0493 is an orally active melanocortin-4 receptor (MC4R) agonist. MK-0493 reduces food intake, suppresses weight gain, elevates blood pressure at high doses, and exhibits preclinical erectile regulatory activity. MK-0493 can be used in research related to obesity.

RO27-3225 TFA is potent and selective melanocortin 4 receptor (MC4R) agonist with an EC₅₀ of 1 nM and 8 nM for MC4R and MC1R, respectively. RO27-3225 TFA shows ~30-fold selectivity for MC4R over MC3R. RO27-3225 TFA has neuroprotective and anti-inflammatory effects.

β-Melanocyte Stimulating Hormone (MSH), human, a 22-residue peptide, acts as an endogenous melanocortin-4 receptor (MC4-R) agonist.

Fenoprofen (LILLY-53858) is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits cyclooxygenase (COX). Fenoprofen is a melanocortin receptors (MCRs) positive allosteric modulator (PAM). Fenoprofen also increases ERK1/2 activation in HEK293T cells. Fenoprofen has anti-arthritic activities and can be used for the study of rheumatoid arthritis and osteoarthritis.