Afamelanotide is an analog of the peptide hormone alpha-melanocyte stimulating hormone (alpha-MSH), which tends to induce skin tanning.
CAT No: 10-101-67
CAS No:75921-69-6 (net)
Synonyms/Alias:Afamelanotide acetate;1566590-77-9;scenesse;Melanotan-1;Melanotan-1 acetate;CHEMBL4297213;TS-09692;
Chemical Name:(4S)-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-acetamido-3-hydroxypropanoyl]amino]-3-(4-hydroxyphenyl)propanoyl]amino]-3-hydroxypropanoyl]amino]hexanoyl]amino]-5-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-6-amino-1-[(2S)-2-[[(2S)-1-amino-3-methyl-1-oxobutan-2-yl]carbamoyl]pyrrolidin-1-yl]-1-oxohexan-2-yl]amino]-2-oxoethyl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-5-carbamimidamido-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-3-(1H-imidazol-4-yl)-1-oxopropan-2-yl]amino]-5-oxopentanoic acid;acetic acid
Afamelanotide acetate is a synthetic peptide analogue of alpha-melanocyte-stimulating hormone (α-MSH), designed to mimic and enhance the activity of endogenous melanocortin peptides. Structurally, it features a modified sequence that confers increased stability and receptor selectivity, making it a valuable tool in the study of melanocortin signaling pathways. As a potent agonist of the melanocortin 1 receptor (MC1R), afamelanotide acetate is distinguished by its capacity to modulate pigmentary responses and cellular pathways linked to photoprotection, immune regulation, and oxidative stress. Its unique biochemical profile has established it as a critical reagent for researchers investigating peptide-receptor interactions, melanogenesis, and related physiological mechanisms.
Peptide receptor research: In the context of receptor pharmacology, afamelanotide acetate serves as a selective agonist for MC1R, enabling detailed analysis of melanocortin receptor function in various cellular and molecular systems. Scientists utilize this peptide to characterize receptor binding affinities, downstream signaling events, and cross-talk with other G protein-coupled receptors. Its high receptor specificity and robust agonistic activity make it particularly suitable for dissecting the molecular determinants of MC1R-mediated responses in both in vitro and ex vivo models.
Melanogenesis studies: The compound is widely employed in experimental studies of melanogenesis, the process by which melanin pigments are synthesized in melanocytes. Through its activation of MC1R, afamelanotide acetate stimulates cAMP-dependent signaling cascades that upregulate key enzymes such as tyrosinase, thereby promoting melanin production. Researchers leverage this property to investigate the regulation of pigmentation at the genetic, enzymatic, and cellular levels, as well as to model pigmentary disorders in controlled laboratory settings.
Photobiology and oxidative stress research: Afamelanotide acetate is instrumental in elucidating the cellular mechanisms underlying photoprotection and oxidative stress responses. By inducing melanin synthesis, it allows researchers to study the protective effects of increased pigmentation against ultraviolet (UV) radiation and related oxidative damage. Experimental protocols frequently incorporate the peptide to assess DNA repair processes, antioxidant defense mechanisms, and the modulation of reactive oxygen species in skin models and cultured cells.
Immunomodulation investigations: Beyond its pigmentary effects, afamelanotide acetate contributes to the study of immune regulation within the skin and other tissues. Melanocortin peptides are known to exert anti-inflammatory and immunomodulatory actions via MC1R and related receptors. Researchers employ this peptide to probe the impact of melanocortin signaling on cytokine production, immune cell recruitment, and inflammation-associated gene expression, providing insights into the broader physiological roles of the melanocortin system.
Peptide drug discovery and development: Due to its structural stability and receptor selectivity, afamelanotide acetate serves as a model compound in the design and optimization of novel melanocortin-based peptides. Medicinal chemists and peptide engineers utilize it as a reference standard to evaluate structure-activity relationships, receptor subtype selectivity, and metabolic stability of new analogues. Its well-characterized pharmacological profile aids in the iterative process of developing next-generation research peptides targeting the melanocortin family of receptors.
Vitiligo is characterized by depigmented patches of skin due to loss of cutaneous melanocytes. Many recent studies have demonstrated defects in the melanocortin system in patients with vitiligo, including decreased circulating and lesional skin levels of α-melanocyte-stimulating hormone (α-MSH). Afamelanotide is a potent and longer-lasting synthetic analogue of naturally occurring α-MSH.
Grimes P E, Hamzavi I, Lebwohl M, et al. The efficacy of afamelanotide and narrowband UV-B phototherapy for repigmentation of vitiligo[J]. JAMA dermatology, 2013, 149(1): 68-73.
Narrowband UV-B (NB-UV-B) phototherapy is used extensively to treat vitiligo. Afamelanotide, an analogue of α-melanocyte-stimulating hormone, is known to induce tanning of the skin.
Lim H W, Grimes P E, Agbai O, et al. Afamelanotide and narrowband UV-B phototherapy for the treatment of vitiligo: a randomized multicenter trial[J]. JAMA dermatology, 2015, 151(1): 42-50.
Erythropoietic protoporphyria is a severe photodermatosis that is associated with acute phototoxicity. Patients with this condition have excruciating pain and a markedly reduced quality of life. We evaluated the safety and efficacy of an α-melanocyte-stimulating hormone analogue, afamelanotide, to decrease pain and improve quality of life.
Langendonk J G, Balwani M, Anderson K E, et al. Afamelanotide for erythropoietic protoporphyria[J]. New England Journal of Medicine, 2015, 373(1): 48-59.
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