Melanocortin Receptor 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.

Resomelagon (AP1189) is a potent, orally active melanocortin receptor (MR) agonist about MC₁ and MC₃. Resomelagon induces ERK1/2 phosphorylation and Ca²⁺ mobilization. Resomelagon has anti-inflammatory activity. Resomelagon can be used for obesity and chronic inflammation research.

ACTH (1-17) TFA, an adrenocorticotropin analogue, is a potent human melanocortin 1 (MC1) receptor agonist with a K_i of 0.21 nM.

Tetracosactide acetate (Tetracosactrin acetate ) is the acetate salt form of Tetracosactide (HY-P0060). Tetracosactide acetate is an analogue of adrenocorticotrophic hormone (ACTH). Tetracosactide acetate is the agonist for melanocortin-4 receptor (MC4R) that activates human MC4R with an EC₅₀ of 0.65 nM. Tetracosactide acetate can stimulate the release of corticosteroids such as cortisol from the adrenal gland. Tetracosactide acetate is currently used for the research of ulcerative colitis and Crohn's disease, juvenile/adult rheumatoid arthritis and osteoarthrosis.

γ-1-Melanocyte Stimulating Hormone (MSH), amide is a 11-amino acid peptide. γ-1-Melanocyte Stimulating Hormone (MSH) regulates sodium (Na⁺) balance and blood pressure through activation of the melanocortin receptor 3 (MC3-R).

γ1-MSH is a melanocortin MC3 receptor agonist, with a K_i of 34 nM for the rat MC3 receptor. γ1-MSH displays ~40-fold selectivity over MC4 (K_i=1318 nM).

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

MK-0493 hydrochloride is a potent, orally active and selective agonist of the melanocortin receptor 4 (MC4R), demonstrating significant reductions in energy intake.

[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.

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

Adrenocorticotropic Hormone (ACTH) (4-10), human is a melanocortin 4 (MC4R) receptor agonist.

Setmelanotide monoacetate (RM-493 monoacetate) is a blood-brain barrier-permeable, selective MC4R agonist with a K_i value of 2.1 nM for hMC4R. Setmelanotide monoacetate activates the CaMKK2/AMPK signaling pathway. Setmelanotide monoacetate mediates body weight homeostasis, feeding regulation and energy expenditure modulation; it reduces food intake, induces weight loss, decreases obesity severity, increases daytime activity and energy expenditure, lowers levels of leptin, triglycerides, fasting insulin and diastolic blood pressure, improves insulin sensitivity, glucose tolerance and fatty liver condition, and reverses respiratory depression. Setmelanotide monoacetate is applicable to research related to obesity, hyperinsulinemia, fatty liver and respiratory depression.

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.

MC4-NN2-0453, a α-MSH analog, is a selective MC4R agonist. MC4-NN2-0453 can be used for obesity research.

γ-2-MSH (41-58), amide is derived from γ-2-MSH. γ-2-MSH is a twelve amino acid peptide that is derived from the N-terminal fragment of proopiomelanocortin (POMC) and contains the His-Phe-Arg-Trp motif common to all melanocortin endogenous agonist ligands.

Resomelagon (AP1189) acetate is a potent, orally active melanocortin receptor (MR) agonist about MC₁ and MC₃. Resomelagon acetate induces ERK1/2 phosphorylation and Ca²⁺ mobilization. Resomelagon acetate has anti-inflammatory activity. Resomelagon acetate can be used for obesity and chronic inflammation research.

Melanotan I (MT-I; [Nle4,D-Phe7]-α-MSH) acetate is an α-MSH (HY-P0252) analog, synthetic melanotropic peptide, and melanocortin receptor (MCR) agonist. Melanotan I acetate induces skin tanning by mimicking the action of α-MSH on the melanocortin 1 receptor (MC1R) in melanocytes. As an appetite suppressant, Melanotan I acetate impairs the ability of insulin to inhibit endogenous glucose production, suppresses leptin secretion from adipose tissue, and thereby reduces voluntary feed intake in ewes. Melanotan I acetate can be used in research related to UV-induced skin damage, polymorphic light eruption, ruminant feeding, and sexual dysfunction.

(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.

Neuropeptide EI, rat displays functional melanin concentrating hormone (MCH)-antagonist and melanocyte-stimulating hormone (MSH) agonist activity in different behavioral paradigms.

Dersimelagon phosphate 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 phosphate shows good affinity for hMC1R and hMC4R with K_i values of 2.26, 32.9 nM, respectively. Dersimelagon phosphate can be used for the research of skin pigmentation.