melanocortin receptor

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].

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.

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.

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).

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

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

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].

MC-4R Agonist 2 hydrochloride (Example 1) is an MC4R agonist used in research on obesity, diabetes, inflammation, and erectile dysfunction. [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].

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].

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].

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].

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

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].

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).

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.

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

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.

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