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Melanotan I

MT-1 · Afamelanotide · Scenesse

Sexual HealthPreclinical
From$0.05/mgCompare prices
MW
1646.8g/mol
Formula
C78H111N21O19

Melanotan I (MT-I) is a synthetic analog of alpha-melanocyte-stimulating hormone (α-MSH), classified as a melanotropic peptide that stimulates skin pigmentation. Researchers primarily study it for its potential to induce tanning without exposure to ultraviolet radiation, aiming to provide a safer alternative for achieving a tanned appearance. Key findings from pharmacokinetic trials indicate that subcutaneous administration of MT-I is fully bioavailable, leading to significant tanning effects that can persist for weeks after treatment, while minimal side effects were reported. Current research status highlights concerns regarding the unregulated use of MT-I and its analogs, with ongoing investigations into their safety and efficacy, as well as the implications of their use in various populations.

Chemical Profile

Chemical Profile

Chemical structure
Chemical Structure
FormulaC78H111N21O19
Molecular Weight1646.8 g/mol
CAS Number75921-69-6
PubChem CID16197727
ChEMBL IDCHEMBL4297789

Half-Life

SCSubcutaneous

~30 minutes to 1 hour

INIntranasal

Not applicable

POOral

Poor bioavailability

The pharmacokinetic profile is primarily characterized by rapid absorption and moderate bioavailability when administered subcutaneously.

Mechanism

Mechanism of Action

Melanotan I (MT-I) acts primarily through the activation of melanocortin receptors (MCRs), particularly the melanocortin-1 receptor (MC1R), which initiates the cAMP signaling pathway. This activation leads to increased melanogenesis, promoting the production of eumelanin and facilitating skin tanning while also potentially influencing other biological processes such as appetite regulation and sexual function. The precise details of its signaling mechanisms and downstream effects remain incompletely understood.

Research

19 Research Publications

548

Total Citations

3

Human/RCT

2.1

Avg. Influence

2025

Latest

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#01

Melanocortin peptide therapeutics: historical milestones, clinical studies and commercialization.

ReviewInfluence2.0
94
The study demonstrated that melanotan-I may provide a therapeutic tan with potential benefits for reducing skin cancer risk, while melanotan-II is being explored for its effects on erectile dysfunction.
0.16 mgkg-1intravenously (IV) and orally (PO)(human)2 weeks0.08 to 0.21 mg kg-1subcutaneously (SC)(human)2 weeks0.16 mg/kg/daysubcutaneous(human)two weeks0.03 nmol/hintracerebroventricular(sheep)days4 mgsubcutaneous(guinea pigs)one month
PubMed
#02

Melanotropic peptides: more than just 'Barbie drugs' and 'sun-tan jabs'?

ReviewInfluence1.0
68
Researchers observed that the public's pursuit of synthetic melanotan products poses health risks, including potential blood-borne virus transmission and complications in pigmented lesions.
0.16 mgkg-1intravenously (IV) and orally (PO)(human)2 weeks0.08 to 0.21 mg kg-1subcutaneously (SC)(human)2 weeks0.16 mg/kg/daysubcutaneous(human)two weeks0.03 nmol/hintracerebroventricular(sheep)days4 mgsubcutaneous(guinea pigs)one month
PubMed
#03

Vitiligo, from Pathogenesis to Therapeutic Advances: State of the Art.

Diotallevi Federico, et al. · International journal of molecular sciences · 2023

ReviewInfluence3.0
68
Researchers observed that vitiligo, a skin condition characterized by white patches due to the loss of pigment cells, affects about 1-2% of the population. The study highlights various factors contributing to this loss, including inflammation and autoimmunity, and discusses recent advancements in targeted treatments that show promise with fewer side effects.

Key findings

  1. 01Researchers found that vitiligo results from a complex interplay of factors leading to the loss of melanocytes, the cells responsible for skin color.
  2. 02The study proposed a comprehensive theory that integrates existing knowledge about the disease's causes.
  3. 03Researchers observed that advancements in understanding vitiligo have led to the development of more effective and safer treatment options.
PubMed
#04

Increased eumelanin expression and tanning is induced by a superpotent melanotropin [Nle4-D-Phe7]-alpha-MSH in humans.

Human
53
Researchers observed that administration of melanotan-I in humans resulted in a significant increase in eumelanin content in the skin, enhancing tanning effects.
0.16 mgkg-1intravenously (IV) and orally (PO)(human)2 weeks0.08 to 0.21 mg kg-1subcutaneously (SC)(human)2 weeks0.16 mg/kg/daysubcutaneous(human)two weeks0.03 nmol/hintracerebroventricular(sheep)days4 mgsubcutaneous(guinea pigs)one month
PubMed
#05

Vitiligo: Pathogenesis and New and Emerging Treatments.

Perez-Bootello Javier, et al. · International journal of molecular sciences · 2023

ReviewInfluence3.0
43
Researchers reviewed the complex disease vitiligo, which affects patients' quality of life and currently lacks a fully effective treatment. They analyzed various existing and emerging therapies, noting that while many options are available, none stand out as completely satisfactory, highlighting the need for ongoing drug development.

Key findings

  1. 01Researchers observed that vitiligo has a multifactorial nature impacting patients significantly.
  2. 02The study reviewed 116 articles on treatments, including phototherapy and various medications, assessing their mechanisms, efficacy, and safety.
  3. 03Despite multiple therapeutic options, there is no clearly superior treatment for vitiligo, emphasizing the necessity for further research and development.
PubMed
#06

Skin pigmentation and pharmacokinetics of melanotan-I in humans.

HumanInfluence3.0
42
Researchers observed that subcutaneous administration of melanotan-I in humans resulted in significant tanning effects and complete bioavailability compared to intravenous dosing.
0.16 mgkg-1intravenously (IV) and orally (PO)(human)2 weeks0.08 to 0.21 mg kg-1subcutaneously (SC)(human)2 weeks0.16 mg/kg/daysubcutaneous(human)two weeks0.03 nmol/hintracerebroventricular(sheep)days4 mgsubcutaneous(guinea pigs)one month
PubMed
#07

Melatonin receptor structure and signaling.

Okamoto Hiroyuki H, et al. · Journal of pineal research · 2024

ReviewInfluence2.0
39
Researchers reviewed the structure and signaling of melatonin receptors, which are important for how melatonin interacts with cells in the body. They noted that different species have various receptor subtypes, particularly in mammals, which play a role in melatonin's effects.

Key findings

  1. 01Researchers found that melatonin binds specifically to its receptors, influencing various biological processes.
  2. 02The study observed different subtypes of melatonin receptors across species, highlighting their diversity.
  3. 03Researchers noted the significance of these receptors in understanding melatonin's role in health and biology.
PubMed
#08

Etiopathogenesis and Emerging Methods for Treatment of Vitiligo.

Iwanowski Tomasz, et al. · International journal of molecular sciences · 2023

ReviewInfluence1.0
35
Researchers reviewed the causes and treatment options for vitiligo, a skin condition affecting 0.5% to 2% of people worldwide. They found that genetic factors and immune responses may play a role in its development and highlighted new treatment methods, including topical and oral medications currently being studied.

Key findings

  1. 01Researchers observed that the exact causes of vitiligo remain unclear, with several theories suggesting genetic predisposition and immune system involvement.
  2. 02The study highlighted new treatment options, including topical ruxolitinib, which has been approved, and other agents like oral ritlecitinib and afamelanotide that are in clinical trials.
  3. 03Advancements in molecular and genetic research may lead to the development of more effective therapies for vitiligo.
PubMed
#09

Melanotan II injection resulting in systemic toxicity and rhabdomyolysis.

Case Report
30
The case report highlighted systemic toxicity, including rhabdomyolysis, following the excessive subcutaneous injection of melanotan-II in a human subject.
0.16 mgkg-1intravenously (IV) and orally (PO)(human)2 weeks0.08 to 0.21 mg kg-1subcutaneously (SC)(human)2 weeks0.16 mg/kg/daysubcutaneous(human)two weeks0.03 nmol/hintracerebroventricular(sheep)days4 mgsubcutaneous(guinea pigs)one month
PubMed
#10

Risks of unregulated use of alpha-melanocyte-stimulating hormone analogues: a review.

ReviewInfluence2.0
24
Researchers observed that the unregulated use of melanotan-I and II is associated with significant risks, including cutaneous complications and potential melanoma development.
0.16 mgkg-1intravenously (IV) and orally (PO)(human)2 weeks0.08 to 0.21 mg kg-1subcutaneously (SC)(human)2 weeks0.16 mg/kg/daysubcutaneous(human)two weeks0.03 nmol/hintracerebroventricular(sheep)days4 mgsubcutaneous(guinea pigs)one month
PubMed
Safety

Safety & Handling

Research Gaps

No long-term human trials have been conducted to assess the chronic effects of melanotan I on skin health and potential carcinogenic risks. Additionally, the precise mechanisms by which melanotan I influences melanogenesis and its interaction with existing skin conditions remain unclear.

Solubility

Melanotan I is soluble in water and DMSO, but poorly soluble in organic solvents like acetonitrile.

Storage & Handling

Lyophilized

Stable for 2+ years at -20°C, 12 months at 4°C

Reconstituted

Use within 14 days when refrigerated at 4°C

Avoid

Avoid repeated freeze-thaw cycles, direct light

Solvent

Bacteriostatic water or sterile saline recommended

Safety information is derived from published research and may not reflect all known risks. This is not medical advice.

Legal Status

Legal Status

🇩🇪DE

Not approved as a medicinal product. Not a controlled substance. Sale as research chemical is a legal grey area.

🇺🇸US

Not approved by the FDA for any indication. Not scheduled by the DEA.

🇦🇺AU

Approved by the TGA for the treatment of erythropoietic protoporphyria under specific conditions.

🇬🇧UK

Not approved by the MHRA for general use. Available under special circumstances for specific conditions.

Legal status information is provided for general reference only and may not reflect the most current regulatory changes. Always verify with official government sources before making any decisions.

Community Insights

Community Insights

Publications per Year

10 total
1
96
1
97
2
00
1
06
1
10
1
12
1
17
1
18
1
23
Pricing

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Mechanism

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Mechanism

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Legal Disclaimer

This page is for informational and research purposes only. All information is based on published scientific literature and does not constitute medical advice, diagnosis, or treatment recommendations. Many substances listed may not be approved for human use and may be subject to drug regulation laws (e.g., AMG in Germany, FDA in the US). PepStack does not encourage the use of any substance on humans. Always consult a qualified healthcare professional before making any health-related decisions. Use of this information is entirely at your own risk. PepStack assumes no liability for the accuracy, completeness, or timeliness of the content provided. Full disclaimer