melanocortin-1 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].

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

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

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.

β-Melanocyte Stimulating Hormone (MSH), human (Synonyms: Beta-MSH (1-22) (human)) β-Melanocyte Stimulating Hormone (MSH), human, a 22-residue peptide, acts as an endogenous melanocortin-4 receptor (MC4-R) agonist.

Adrenocorticotropic Hormone (ACTH) (1-39), rat, is a potent melanocortin 2 (MC2) receptor agonist. Peptide fragments of ACTH (1-39) were formed during in vitro incubation with membrane preparations, isolated by high-pressure liquid chromatography, and characterized by determining their amino acid composition and NH2-terminal residue.

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.

α-Melanocyte-stimulating hormone (α-MSH) is a 13-amino acid peptide hormone produced by post-translational processing of proopiomelanocortin (POMC) in the pituitary gland, as well as in keratinocytes, astrocytes, monocytes, and gastrointestinal cells.1It is an agonist of melanocortin receptor 3 (MC3R) and MC4R that induces cAMP production in Hepa cells expressing the human receptors (EC50s = 0.16 and 56 nM, respectively).2α-MSH (100 pM) reducesS. aureuscolony formation andC. albicansgerm tube formationin vitro.3It inhibits endotoxin-, ceramide-, TNF-α-, or okadaic acid-induced activation of NF-κB in U937 cells.1α-MSH reduces IL-6- or TNF-α-induced ear edema in mice.4It also prevents the development of adjuvant-induced arthritis in rats and increases survival in a mouse model of septic shock. Increased plasma levels of α-MSH are positively correlated with delayed disease progression and reduced death in patients with HIV.1 1.Catania, A., Airaghi, L., Colombo, G., et al.α-melanocyte-stimulating hormone in normal human physiology and disease statesTrends Endocrinol. Metab.11(8)304-308(2000) 2.Miwa, H., Gantz, I., Konda, Y., et al.Structural determinants of the melanocortin peptides required for activation of melanocortin-3 and melanocortin-4 receptorsJ. Pharmacol. Exp. Ther.273(1)367-372(1995) 3.Cutuli, M., Cristiani, S., Lipton, J.M., et al.Antimicrobial effects of a-MSH peptidesJ. Leukoc. Biol.67(2)233-239(2000) 4.Lipton, J.M., Ceriani, G., Macaluso, A., et al.Antiiinflammatory effect of the neuropeptide a-MSH in acute, chronic, and systemic inflammationAnn. N.Y. Acad. Sci.25(741)137-148(1994)

PF-00446687 is a selective agonist of melanocortin-4 receptor (MC4R) (EC50 of 12 ± 1 nM).

(p-Iodo-Phe7)-ACTH (4-10), a derivative of adrenocorticotrophic hormone (ACTH) produced by the anterior pituitary gland, functions as a melanocortin (MC) receptor antagonist and effectively inhibits α-melanocyte-stimulating hormone (α-MSH)-induced excessive grooming behavior in rats [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].

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

ACTH (1-17) TFA is a corticotrophin analogue and an effective human melanocortin 1 (MC1) receptor agonist with Ki value of 0.21 nM.

Adrenocorticotropic Hormone (ACTH) (1-39), rat (TFA), is a potent agonist of the melanocortin 2 receptor (MC2).

RO27-3225 TFA is a potent and selective agonist of melanocortin 4 receptor (MC4R; EC50: 1 nM and 8 nM for MC4R and MC1R) with neuroprotective and anti-inflammatory effects. RO27-3225 TFA shows ~30-fold selectivity for MC4R over MC3R.

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.

γ-1-Melanocyte Stimulating Hormone (MSH), amide, an 11-amino acid peptide, plays a critical role in regulating sodium (Na+) balance and blood pressure by activating melanocortin receptor 3 (MC3-R).

PG106 TFA is a potent, selective antagonist of the human melanocortin 3 (hMC3) receptor, displaying an IC50 value of 210 nM, while exhibiting negligible activity at the hMC4 receptors (EC50 = 9900 nM) and hMC5 receptor [1].

CCZ01048 TFA, an α-MSH analogue, demonstrates a strong binding affinity for the melanocortin 1 receptor (MC1R), displaying a K i value of 0.31 nM. It exhibits rapid internalization into B16F10 melanoma cells and maintains high in vivo stability. CCZ01048 TFA holds potential as an effective agent for PET imaging of malignant melanoma [1].

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

CCZ01048, an analogue of α-melanocyte-stimulating hormone (α-MSH), demonstrates a high binding affinity for the melanocortin 1 receptor (MC1R), with a Ki of 0.31 nM. It rapidly internalizes into B16F10 melanoma cells and exhibits notable in vivo stability, making it a promising candidate for PET imaging of malignant melanoma [1].