Melanocortin Receptor

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

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).

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

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

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.

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

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

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)

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

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.

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

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].

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.

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.

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

2-MNG (2-Mercaptonicotinoyl glycine) is a novel melanogenesis inhibitor that prevents the incorporation of certain melanin precursors into growing melanin by binding to them. 2-MNG inhibits two mechanisms of UV-induced skin pigmentation in vivo.

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

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

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.

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

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). It significantly reverses stress-induced anorexia without affecting food intake in free-feeding rats and exhibits anxiolytic-like activity in vivo.

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.

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.

Atumelnant (CRN04894) is a selective and potent MC2R antagonist that inhibits ACTH-stimulated corticosterone secretion in a dose-dependent manner for the study of congenital adrenocortical hyperplasia (CAH) and Cushing's disease (CD).

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).

[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.

Tetrapeptide-1, a bioactive peptide known for its antioxidant properties, is frequently cited as an ingredient in cosmetics [1].

Ac-DArg-c[Cys-Glu-His-DPhe-Arg-Trp-Cys]-NH2 is a synthetic cyclic octapeptide acting as a melanocortin-4 receptor (MC4R) agonist, significantly elevating heart rate and blood pressure [1].

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].

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

Melanostatin, frog TFA is a highly efficient α-melanocyte-stimulating hormone (α-MSH) release inhibitor, a 36-amino acid peptide isolated from the frog brain, which modulates the electrophysiological activity of frog melanocytes by regulating K+, Na+, and Ca2+ currents.

MC-4R Agonist 2 (Example 1), a melanocortin 4 receptor (MC4R) agonist, is used in research related to obesity, diabetes, inflammation, and erectile dysfunction [1].

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].

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 known as corticotropin inhibitory peptide (CIP). It functions as an antagonist to the ACTH receptor and lacks 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) is an MC4R agonist used in research on obesity, diabetes, inflammation, and erectile dysfunction. [1]