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Melanotan-1, also known as afamelanotide, is a synthetic peptide that mimics the natural hormone alpha-melanocyte-stimulating hormone (α-MSH). It works by stimulating melanocytes in the skin to produce more melanin, leading to a darker skin tone. Its primary medical use is in treating erythropoietic protoporphyria (EPP), a rare disorder that causes extreme sensitivity to sunlight. By increasing melanin levels, Melanotan-1 helps improve the skin’s natural protection against UV radiation. Unlike Melanotan II, it has a more targeted action and fewer side effects.
Molecular Formula:C78H111N21O19
Molecular Weight:1646.85g/mol
CAS Number:75921-69-6
Melanotan1 (MT1/Afamelanotide) is a synthetic analog of αMSH (alphamelanocyte-stimulating hormone), engineered for increased receptor affinity and longer plasma half-life, enabling potent skin tanning with minimal sun exposure .
【1】 Mechanism of Action
Acts primarily on MC1R receptors on melanocytes to boost eumelanin production, offering UV protection and reduced erythema .
Also engages MC3R/MC4R/MC5R, potentially influencing appetite, sexual function, and immune modulation .
【2】Pharmacokinetics & Human Trials
Subcutaneous dosing shows effective absorption (absorption t₁/₂: 0.8–1.7 h; beta phase: 0.07–0.79 h), with sustained pigmentation lasting 3+ weeks after a 10-dose regimen【https://pubmed.ncbi.nlm.nih.gov/9113347/】.
Phase I human studies (AZ, 0.08–0.16 mg/kg with UV exposure) demonstrated faster, deeper tanning and 47% fewer sunburn cells, with minimal side effects (nausea, flushing) 【https://pubmed.ncbi.nlm.nih.gov/15262693/】.
【3】 Clinical Uses in Photosensitivity Disorders
Shows promise for actinic keratoses, prevention of squamous cell carcinoma, and disorders like erythropoietic protoporphyria (EPP) and polymorphic light eruption.
Notably used under the brand name Scenesse (afamelanotide) in the EU/US for EPP, offering monthly subcutaneous implants to enhance UV tolerance 【https://en.wikipedia.org/wiki/Afamelanotide?utm_source=chatgpt.com】.
Sunless, sustained tanning with protective eumelanin increase
Reduces sunburn risk and UV damage indicators
Helps manage photosensitivity disorders, improving patient quality of life
Minimal side effects: only occasional flushing, nausea
Implant format (Scenesse) offers monthly dosing convenience
Emerging evidence for anti-inflammatory and immunomodulatory effects
Exploring chemopreventive effects for skin cancer, leveraging melanin’s photoprotective properties 【https://pmc.ncbi.nlm.nih.gov/articles/PMC3394601/?utm_source=chatgpt.com】
As MC1R agonists modulate inflammation and innate immunity, MT1 is being investigated for IBD, rheumatoid arthritis, and dermatitis【https://pmc.ncbi.nlm.nih.gov/articles/PMC10265466/?utm_source=chatgpt.com】.
Original studies with MT2 showed aphrodisiac and appetite-suppressing effects; ongoing efforts aim to isolate analogs maintaining tanning while minimizing hormonal side effects.
Novel implantable or depot formulations, including patch systems, are being tested to ensure long-term, controlled melanin induction【https://en.wikipedia.org/wiki/Afamelanotide?utm_source=chatgpt.com】.
Continuous pharmacovigilance for mole/nevi changes, potential melanoma risk, and long-term safety .
Dermatology & Cosmetic Tanning: Controlled pigmentation with UV safety benefits
Photosensitivity Treatment: EPP, polymorphic light eruption, actinic keratoses, porphyria
UV Damage Prevention: Reduction in sunburn and photodamage
Immunomodulation Research: Potential in chronic inflammatory conditions
Neuroendocrine Investigations: Appetite, libido, and systemic hormonal effects
Melanotan1, especially as afamelanotide (Scenesse), offers a science-backed method for safe pigmentation, UV protection, and management of rare skin disorders. It stands distinct from unregulated market agents in its clinically tested, implantable form. Although off-label and over-the-counter versions exist, concerns remain about product purity, side effects, and legal status .
ALL ARTICLES AND PRODUCT INFORMATION PROVIDED ON THIS WEBSITE ARE FOR INFORMATONAL AND EDUCATIONAL PURPOSES ONLY.
The products offered on this website are furnished for in-vitro studies only. In-vitro studies(Latin: in glass) are performed outside of the body. These products are not medicines or drugs and have not been approved by the FDA to prevent, treat or cure any medical condition, ailment or disease. Bodily introduction of any kind into humans or animals is strictly forbidden by law.
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