Introduction
Melanotan I, also known as afamelanotide, is a synthetic analogue of the naturally occurring hormone alpha-melanocyte-stimulating hormone (α-MSH). It is primarily used for its tanning effects and potential treatment of various skin conditions. This peptide has gained attention for its ability to promote skin pigmentation and protect against UV-induced skin damage.
Mechanism of Action
Melanotan I works by mimicking the action of α-MSH, a hormone that naturally occurs in the body and stimulates melanogenesis, the process of melanin production. When the skin is exposed to UV radiation, keratinocytes in the epidermis produce α-MSH in response to DNA damage. This hormone then binds to the melanocortin 1 receptor (MC1R) on melanocytes, which are the pigment-producing cells in the skin.
The binding of α-MSH to MC1R activates a signaling cascade that increases the production of cyclic adenosine monophosphate (cAMP) and cAMP-dependent protein kinase. This, in turn, enhances the activity of melanogenic enzymes, such as tyrosinase, leading to increased melanin production. Melanotan I, being a superpotent melanocortin, is designed to resist enzymatic breakdown, prolonging its duration of action at the MC1R compared to natural α-MSH.
By stimulating MC1R, Melanotan I promotes melanogenesis by increasing melanocyte proliferation and upregulating tyrosinase activity. This results in increased cutaneous eumelanin production, leading to darker skin pigmentation. The increased pigmentation provides a partial barrier to the penetration of UV radiation and visible light, offering protection against UV-induced damage.
Uses
Melanotan I has several clinical applications, primarily related to skin conditions and UV protection:
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Skin Tanning: Melanotan I is used to achieve a natural-looking tan without prolonged sun exposure. This can be particularly beneficial for individuals who want to avoid the risks associated with excessive UV exposure.
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Photoprotection: It has shown promise in preventing actinic keratoses and squamous cell carcinoma, especially in organ transplant recipients. Melanotan I can also help manage photosensitivity disorders such as erythropoietic protoporphyria (EPP), solar urticaria (SU), and polymorphic light eruption (PLE).
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Other Potential Uses: Melanotan I is being investigated for its potential to treat other skin conditions like vitiligo, where restoring pigmentation can improve quality of life. Additionally, it may have protective effects against neuroinflammation and could be used to regenerate DNA of skin exposed to UV damage.
Dosage Instructions
The dosage of Melanotan I can vary depending on the intended use and individual tolerance. Here are some general guidelines:
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Protective Dose: For individuals looking to protect their skin from UV damage, a dose of 0.25mg (0.05ml or 5 units) injected subcutaneously 30 minutes before sun exposure is recommended.
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Maintenance Dose: To maintain pigmentation, a dose of 0.25mg to 0.5mg (0.1ml or 10 units) injected subcutaneously daily for 10 days, followed by 1-2 times per week, is suggested. If intolerable side effects occur, reducing the dose is advised.
Reconstitution and Administration
Melanotan I typically comes in a lyophilized powder form and needs to be reconstituted before use. Here are the steps for reconstitution:
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Reconstitution: Inject 2ml of bacteriostatic water into the vial containing the powder. This will yield a solution with a concentration of 5mg/ml.
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Storage: Store the reconstituted solution at -20°C to maintain stability. Fresh preparation is advised because the chemical is unstable in solutions.
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Administration: Melanotan I is administered via subcutaneous injection. It is important to follow proper injection techniques to ensure safety and efficacy.
Side Effects
While Melanotan I is generally considered safe, some users may experience side effects, including:
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Headaches: Occasional headaches have been reported.
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Dizziness: Temporary changes in blood pressure, leading to feelings of lightheadedness or dizziness.
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Pigmentation Changes: Darkening of lips and gums may occur.
Product Name |
Melanotan I |
Active Ingredient |
Melanotan I |
Dosage Form |
Injection |
Strength |
10mg/vial |
Packaging |
10vials/Box Customizable version |
Manufacturer |
Sinopharmatech Co., Ltd. |
Storage Conditions
• Store in a refrigerated environment at 2°C-8°C, away from light
• Short-term transportation is possible at 15°C-25°C but should not exceed seven days
• Inspect the solution before use to ensure it is clear and free from particles or discoloration






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