Melanocortin Receptor

Dersimelagon (MT-7117) is an orally active, selective agonist for the melanocortin 1 receptor (MC1R), demonstrating EC50 values of 8.16 nM (h), 3.91 nM (cm), 1.14 nM (m), and 0.251 nM (r) across species such as human, cynomolgus monkey, mouse, and rat, respectively. It exhibits strong affinity for human MC1R and MC4R, with Ki values of 2.26 nM and 32.9 nM, respectively. This compound is applied in the study of skin pigmentation.

a-MSH, amide Acetate as an endogenous neuropeptide. It 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)

Nonapeptide-1 acetate salt (158563-45-2 free base) (Melanostatine-5 acetate salt) , a peptide hormone, is a potent α-Melanocyte-stimulating hormone (α-MSH) antagonist, with an IC50 of 11 nM. Nonapeptide-1 acetate salt (158563-45-2 free base) , a peptide hormone, is a potent α-Melanocyte-stimulating hormone (α-MSH) antagonist, with an IC50 of 11 nM.

Neuropeptide EI, rat acetate Displays functional MCH-antagonist and MSH-agonist activity in different behavioral paradigms.

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

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.

ACTH 11-24 acetate(4237-93-8 free base) (Adrenocorticotropic Hormone (11-24) acetate) is a fragment of adrenocorticotrophin, induces cortisol release. ACTH (11-24) has been identified as a competitive antagonist of ACTH (1-39) and ACTH (1-10) in isolated adrenal cells.

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).

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.

Beta-MSH (1-22) (human) acetate (Beta-MSH (1-22) (human) acetate (17908-57-5 Free base)) , is an endogenous melanocortin-4 receptor (MC4-R) agonist.

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

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.

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

PF-07258669 is a selective melanocortin 4 receptor (MC4) antagonist used in the study of cachexia and loss of appetite.

Adrenocorticotropic Hormone (ACTH) (4-10) TFA (Acth (4-10)) is an agonist of potent melanocortin(MC4R) receptor .

[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.

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

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

TCMCB07 TFA is a cyclic nonapeptide and an orally active, brain-penetrating antagonist of the melanocortin receptor 4 (MC4R), playing a significant role in managing cachexia [1].

Setmelanotide (BIM-22493) is a selective agonist of melanocortin 4 receptor (MC4R)(human and rat MC4R with EC50s of 0.27 nM and 0.28 nM, respectively).

Adrenocorticotropic Hormone (ACTH) (4-10) is an agonist of potent melanocortin(MC4R) receptor .

MCL0020 is a potent and selective melanocortin MC4 receptor antagonist (IC50 values are 11.63, 1115 and > 10 000 nM at MC4, MC3 and MC1 receptors respectively). Significantly reverses stress-induced anorexia but has no effect on food intake in free-feeding rats. Exhibits anxiolytic-like activity in vivo.

TCMCB07, a cyclic nonapeptide, serves as an orally active, brain-penetrant antagonist of the melanocortin receptor 4 (MC4R), with significant implications in the management of cachexia [1].

Ac-DArg-c[Cys-Glu-His-DPhe-Arg-Trp-Cys]-NH2 is a synthetic cyclic octapeptide that exhibits melanocortin-4 receptor (MC4R) agonism and has been shown to significantly elevate heart rate and blood pressure [1].

Tetrapeptide-1 is a bioactive peptide renowned for its antioxidant properties and has been cited as an ingredient in cosmetics [1].

AP1189 acetate is a biased agonist at melanocortin 1 and melanocortin 3 receptors.

Melanotan (MT)-II, a synthetic melanocortin receptor agonist, is a synthetic analogue of the peptide hormone α-melanocyte-stimulating hormone (α-MSH).

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.

MC-4R Agonist 2 (Example 1), a melanocortin 4 receptor (MC4R) agonist, is employed in the research of conditions such as obesity, diabetes, inflammation, and erectile dysfunction [1].

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

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].

ACTH (7-38) (human) is a fragment (7-38) of the full human adrenocorticotropic hormone (ACTH (1-39)), also referred to as corticotropin inhibitory peptide (CIP). It acts as an antagonist to the ACTH receptor and possesses no corticosteroid activity [1].

N,N′-Diferuloylputrescine acts as a pigment inhibitor, showing a 57% reduction in pigmentation. It also considerably diminishes the protein expression of MITF and displays potent antioxidant properties as a radical scavenger against reactive oxygen species [1].

MC-4R Agonist 2 hydrochloride (Example 1) serves as an MC4R agonist, with applications in researching obesity, diabetes, inflammation, and erectile dysfunction. [1]

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