melanocortin

THIQ is a selective melanocortin-4 receptor (MC4R) agonist (hMC4R and rMC4R with IC50 of 1.2 nM and 0.6 nM , respectively).

HS024 is a highly potent melanocortin MC4 receptor antagonist (Ki values are 0.29, 18.6, 5.45 and 3.29 nM for cloned human MC4, MC1, MC3 and MC5 receptors respectively). Increases food intake, and blocks α-MSH- and MTII-induced hypotension and bradycardia in rats, following central administration in vivo.

PF-07258669 is a small-molecule compound and a melanocortin 4 receptor (MC4R) antagonist (IC50 = 13 nM, Ki = 0.46 nM) with high selectivity, oral bioavailability, and favorable pharmacokinetic properties. This compound can be used for research on diseases such as cachexia and anorexia.

Undecylenoyl phenylalanine (Sepiwhite msh QD) is a novel depigmenting agent, which possibly acts as an alpha-melanocyte-stimulating hormone antagonist, thus inhibiting melaninogenesis.

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 exhibits good affinity for hMC1R and hMC4R, with Ki values ​​of 2.26 and 32.9 nM, respectively. Dersimelagon can be used in the study of skin pigmentation[1].

Bivamelagon hydrochloride is a selective MC4R agonist (EC50=36.5 nM, Ki=65 nM) with the advantages of oral available and blood-brain barrier penetration, suitable for obesity and diabetes research.

ACTH (1-17) acetate is a potent agonist at the human melanocortin 1 (MC1) receptor with high affinity(Ki = 0.21 nM).

[D-Trp8]-γ-MSH acetate(321351-81-9 free base) is a selective melanocortin 3 (MC3) receptor agonist (IC50 values are 6.7, 340 and 600 nM for human MC3, MC5 and MC4 receptors respectively) and displays anti-inflammatory efficacy.

PG 106 acetate is an effective and selective antagonist of the human melanocortin 3 (hMC3) receptor with an IC50 of 210 nM. PG 106 acetate has no activity with the hMC5 receptor and hMC4 receptors with an EC50 of 9900 nM.

HS 014 acetate is a potent and selective melanocortin MC4 receptor antagonist (Ki values are 3.16, 108, 54.4 and 694 nM for cloned human MC4, MC1, MC3 and MC5 receptors respectively). Increases food intake in rats and nociception in mice following central

Fenoprofen (LILLY-5385) is a non-steroidal anti-inflammatory compound and a modifier enhancer of the melanocortin receptor, which increases ERK1/2 activation, inhibits biofilm formation, and alters biofilm structure, and is used in the treatment of acute pain and chronic arthritis.

MC-4R Agonist 1 is an agonist of the human melanocortin-4 receptor (MC-4R) and is useful in researching sexual dysfunction, obesity, and diabetes.

BMS-470539 dihydrochloride is a selective and highly potent melanocortin 1 receptor (MC-1 R) agonist with anti-inflammatory activity. BMS-470539 attenuates oxidative stress and neuronal apoptosis via the MC1R/cAMP/PKA/Nurr1 signaling pathway in a neonatal hypoxia-ischemia rat model.

Setmelanotide (RM-493) is a selective melanocortin-4 receptor agonist with EC50 values of 0.27 and 0.28 nM for human and rat MC4R. Setmelanotide enhances cAMP signaling, demonstrates functional selectivity, activates sympathetic preganglionic neurons to influence blood pressure, and is widely used to probe MC4R-MRAP2 interactions. Setmelanotide contributes to obesity-related research by modulating hunger and satiety circuits, reversing risperidone-induced weight gain in mice, and helping characterize MC4R variants in pediatric metabolic disorders. The anti-inflammatory actions of Setmelanotide in astrocytoma cells and the utility in combination with calorie restriction further highlight its broad value in metabolic and neuroendocrine research.

Setmelanotide Acetate(920014-72-8 free base) (RM-493 Acetate) is a selective agonist of melanocortin 4 receptor (MC4R)(human and rat MC4R with EC50s of 0.27 nM and 0.28 nM, respectively).

SHU 9119 acetate is a well-known antagonist of human melanocortin 3 and 4 (hMC3R, hMC4R) receptors and a partial hMC5R agonist. The IC50 values of human MC3R, MC4R and MC5R is 0.23, 0.06, and 0.09 nM respectively.

JNJ-10229570 (UNII-N9IX402L35) 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.

Afamelanotide acetate is a synthetic α-melanocyte stimulating hormone analogue and first-in-class melanocortin-1 receptor agonist, used to for Erythropoietic Protoporphyria.

Bremelanotide Acetate (PT-141 Acetate) is an agonist of melanocortin receptor (MCR) .

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

Nonapeptide-1 (Melanostatine™ 5) can inhibit the synthesis of melanin, which makes it of interest for treating certain skin conditions.

α-MSH (MSH, amide) is amide stimulates melanocortin 1 receptor that results in the activation of adenylyl cyclase.

Bivamelagon (LB54640) is an orally effective MC4R (melanocortin 4) agonist with the advantage of crossing the blood-brain barrier, suitable for studying hypothalamic obesity and diabetes.

IIIM-8 is a melanogenesis inhibitor that suppresses pigment production in both in vitro and in vivo settings, exhibiting no cytotoxic effects on Human Adult Epidermal Melanocytes (HAEM). It has potential applications in the study of hyperpigmentation disorders [1].