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, also known as melanotan-1 or α-MSH analog, is a synthetic peptide that mimics the action of the naturally occurring alpha-melanocyte-stimulating hormone. As a potent and selective agonist of the melanocortin 1 receptor (MC1R), this compound has garnered significant attention in scientific research for its ability to stimulate melanin production and modulate various physiological processes. Its unique mechanism of action, coupled with a favorable stability profile, makes it a valuable tool for exploring the roles of melanocortin pathways in diverse biological contexts. Researchers have employed afamelanotide acetate in a variety of experimental models, leveraging its properties to elucidate both the molecular and systemic effects of melanocortin receptor activation.
Photoprotection research: In the field of photobiology, afamelanotide acetate is frequently utilized to investigate the mechanisms underlying skin pigmentation and the body's natural defense against ultraviolet (UV) radiation. By stimulating eumelanin synthesis in melanocytes, this peptide provides a model for studying how increased pigmentation can enhance cellular resistance to UV-induced DNA damage. Researchers often employ it in in vitro skin models or animal studies to assess changes in melanin content and to delineate the downstream protective signaling pathways activated by MC1R agonism. These investigations contribute to a deeper understanding of pigmentation biology and the development of novel photoprotective strategies.
Pigmentation disorders: Melanotan-1 is widely used in laboratory settings to explore the pathophysiology of pigmentary conditions such as vitiligo and melasma. By modulating melanocyte activity and melanin distribution, the peptide serves as a research tool for testing hypotheses regarding the reactivation of dormant melanocytes or the prevention of abnormal pigment loss. Studies employing afamelanotide acetate often focus on its potential to restore or redistribute pigmentation in cellular and animal models, thereby providing insights into the molecular dynamics of pigmentation disorders and the efficacy of targeted interventions.
Neuroprotection studies: Beyond its dermatological applications, afamelanotide acetate has been investigated for its neuroprotective properties. The melanocortin system is implicated in modulating inflammation and oxidative stress within the nervous system. Researchers utilize this peptide in experimental paradigms to examine its ability to attenuate neuronal damage, reduce pro-inflammatory cytokine expression, and support cellular survival under stress conditions. Such studies are instrumental in expanding our knowledge of melanocortin-mediated neuroprotection and its implications in neurodegenerative disease models.
Anti-inflammatory research: The anti-inflammatory effects of melanocortin agonists are another area of active investigation. Afamelanotide acetate can be employed in cell culture or animal models to study its impact on inflammatory signaling cascades, immune cell regulation, and tissue homeostasis. By activating MC1R and related receptors, the compound has been shown to modulate the expression of key inflammatory mediators, offering a research platform for exploring new therapeutic approaches to inflammatory and autoimmune conditions.
Metabolic regulation studies: In metabolic research, afamelanotide acetate is explored for its role in energy homeostasis and appetite regulation. The melanocortin pathway is a critical regulator of body weight and metabolism, and the peptide's ability to selectively activate MC1R provides a means to dissect the contributions of this pathway to feeding behavior, adiposity, and glucose metabolism. Experimental models utilizing melanotan-1 help clarify the molecular underpinnings of metabolic disorders and inform the development of novel interventions for obesity and related conditions.
In summary, afamelanotide acetate serves as a versatile research tool across multiple scientific disciplines. Its applications in photoprotection, pigmentation disorders, neuroprotection, anti-inflammatory research, and metabolic regulation underscore its importance in advancing our understanding of melanocortin biology. Scientists continue to leverage its unique properties to unravel complex physiological processes and to drive innovation in experimental therapeutics and basic biomedical research.
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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