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Melanotan II

Name: Melanotan II
SKU: 7747
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Description
Additional information

Melanotan II / Melanotan 2 (MT-2) is a cyclic peptide analog of ?-MSH that interacts with multiple melanocortin receptors, including MC3R and MC4R. It is studied in research exploring pigmentation, sexual behavior pathways, and appetite regulation. MT-2 is used in laboratory settings to investigate melanocortin system dynamics.

Weight	.06 kg
Size	10 mg
Shelf Life	24 months
Storage	Lyophilized: freeze at ?20 °C (?4 °F) or below. Reconstituted: refrigerate at 2–8 °C (35.6–46.4 °F); use within 1–2 weeks.
Molecular Formula	C??H??N??O?
PubChem CID	92432 http://www.pubchem.ncbi.nlm.nih.gov/compound/92432
Disclaimer	These statements have not been evaluated by the Food and Drug Administration. This product is not intended to diagnose, treat, cure, or prevent any disease. For research purposes only. Not for human consumption.

Melanotan II

Also known as: MT-II · MT-2 · Melanotan 2 Category: Pigmentation · Sexual Health Clinical Status: Preclinical / Research Discontinued FDA Status: Not Approved · Investigational

A synthetic cyclic peptide analog of alpha-melanocyte stimulating hormone (α-MSH), originally developed at the University of Arizona for skin cancer prevention research. Studied for its effects on melanogenesis, sexual function, and appetite regulation. All data presented reflects published research findings only.

Explore the Research ↓

🧬

Peptide Type

Synthetic Cyclic Heptapeptide

📊

Amino Acid Length

7 residues (Ac-Nle-c[Asp-His-D-Phe-Arg-Trp-Lys]-NH₂)

🔬

Primary Research Focus

Melanogenesis & melanocortin signaling

🧪

Current Development Stage

Preclinical · Research discontinued

What Is Melanotan II?

🧠 Simple Explanation

Melanotan II is a lab-made molecule composed of 7 building blocks (amino acids) arranged in a ring shape. It mimics a natural hormone in your body called alpha-MSH, which tells skin cells to produce melanin — the pigment that makes your skin darker. In research studies, it has also shown effects on appetite and sexual arousal.

Scientists originally created it to study whether increasing skin pigmentation could help protect against skin cancer. Development was later discontinued due to side effect concerns, and it has never received regulatory approval.

🔬 Advanced Context

Melanotan II (Ac-Nle-c[Asp-His-D-Phe-Arg-Trp-Lys]-NH₂) is a synthetic cyclic lactam analog of alpha-melanocyte stimulating hormone (α-MSH). It was developed at the University of Arizona in the early 1990s as a potential photoprotective agent. The cyclic structure confers enhanced metabolic stability compared to the linear native hormone.

As a non-selective melanocortin receptor agonist, MT-II exhibits high affinity for both MC1R (mediating pigmentation through cAMP-PKA signaling and eumelanin synthesis) and MC4R (mediating pro-erectile and appetite-suppressive effects through central nervous system pathways). It also demonstrates moderate affinity for MC3R and MC5R.

Clinical trials demonstrated effective UV-independent tanning and pro-erectile activity, but development was discontinued due to side effects including nausea, mole darkening, and cardiovascular concerns. The derivative PT-141 (bremelanotide) was subsequently developed with more selective MC4R targeting, receiving FDA approval in 2019 for hypoactive sexual desire disorder in premenopausal women.

How It Works

Mechanism of action based on clinical and preclinical evidence

STEP 01 →

Melanocortin Receptor Binding

Melanotan II binds with high affinity to MC1R on melanocytes and MC4R in the central nervous system. Its cyclic structure provides enhanced receptor selectivity and metabolic stability compared to native α-MSH.

💡 Simple Translation

The peptide locks onto specific docking sites on skin cells and brain cells — like a key fitting into two different locks, each triggering a different response.

STEP 02 →

Intracellular Signaling Activation

MC1R engagement activates adenylyl cyclase, elevating intracellular cAMP levels and triggering PKA-mediated phosphorylation of CREB. MC4R activation in the hypothalamus and spinal cord initiates pro-erectile signaling independent of NO/cGMP pathways.

💡 Simple Translation

Once attached, each receptor sends a different set of chemical messages inside the cell. Skin cells receive instructions to produce pigment, while brain cells receive signals related to arousal and appetite.

STEP 03 →

Cellular Response

CREB phosphorylation upregulates MITF transcription factor, driving tyrosinase expression and eumelanin biosynthesis in melanocytes. Centrally, MC4R activation modulates hypothalamic energy homeostasis and spinal erectile circuitry.

💡 Simple Translation

Skin cells begin manufacturing more melanin — the natural pigment that darkens your skin. Meanwhile, brain pathways involved in hunger and sexual function are influenced by the same compound through a separate mechanism.

STEP 04

Research Outcome

Clinical studies demonstrated UV-independent skin darkening in 100% of treated subjects, including those with MC1R variant alleles. Pro-erectile responses occurred in 85% of participants (17/20 vs 3/20 placebo). Appetite suppression was commonly observed through MC4R-mediated pathways.

💡 Simple Translation

In controlled studies, treated individuals developed darker skin without needing sun exposure, and the majority of male subjects experienced measurable effects on sexual function.

Molecular Profile

Physicochemical characteristics and storage parameters

Molecular Weight

1,024.18 g/mol

Structure Type

Synthetic Cyclic Heptapeptide

CAS Number

121062-08-6

Molecular Formula

C₅₀H₆₉N₁₅O₉

Amino Acid Sequence

Ac-Nle-c[Asp-His-D-Phe-Arg-Trp-Lys]-NH₂

Structure

Cyclic lactam (α-MSH analog)

Lyophilized Storage

2–8°C refrigerated

Reconstituted Stability

~30 days refrigerated

Reference: PubChem — Melanotan II ↗

Clinical Development Status

Current position in the regulatory pipeline

✓

Preclinical

✓

Phase 1

Phase 2

Phase 3

Phase 4

FDA Approved

Phase 1 trials conducted at the University of Arizona evaluated safety and melanogenic activity. Further clinical development was discontinued due to side effect concerns. The derivative PT-141 (bremelanotide) progressed to FDA approval in 2019 for a separate indication. Melanotan II is not approved by the FDA for any use.

Research Timeline

Key milestones in Melanotan II investigation

1991

Initial Development

Melanotan II synthesized at the University of Arizona as a cyclic analog of α-MSH for skin cancer prevention research

1996

Phase 1 Human Trial

Pilot clinical study evaluated safety and pharmacokinetics; dose-dependent tanning and side effects documented

1998

Erectile Function Study

Double-blind RCT demonstrated 85% erectile response rate in men with psychogenic ED (Wessells et al.)

2004

Female Sexual Function

PT-141 derivative studied in premenopausal women with sexual arousal disorder, showing positive subjective responses

2006

Landmark Tanning RCT

Barnetson et al. confirmed UV-independent eumelanin induction in fair-skinned subjects, including MC1R variant carriers

2019

PT-141 FDA Approval

Bremelanotide (PT-141), derived from MT-II research, received FDA approval for hypoactive sexual desire disorder

2022

WADA Prohibition

Melanotan II added to the World Anti-Doping Agency prohibited substance list

2026

Current Status

Remains a research compound with no regulatory approval; classified as an unapproved drug by the FDA

What Does the Research Show?

Summary of investigational findings from published studies

📊

Key Findings

UV-independent skin darkening observed in 100% of treated subjects

Effective tanning in individuals with MC1R genetic variants who typically cannot tan

Pro-erectile response in 85% of participants (17/20 vs 3/20 placebo)

Appetite suppression commonly reported through MC4R-mediated pathways

📈

Research Milestones

Developed at the University of Arizona in the early 1990s

Phase 1 trials evaluated safety and melanogenic activity

Derivative PT-141 received FDA approval for HSDD in 2019

Research discontinued for MT-II due to side effect profile

🔬

Observed Biological Effects

Eumelanin synthesis stimulation via MC1R-cAMP-PKA signaling

Central pro-erectile signaling through hypothalamic and spinal MC4R

Energy homeostasis modulation and appetite reduction via MC3R/MC4R

Mean tip rigidity duration of ~40 minutes at >80% in study subjects

🧪

Safety Profile in Studies

Nausea reported in ~40% of subjects (dose-dependent, typically transient)

Facial flushing observed in ~35% of participants

Darkening of existing moles requiring dermatological monitoring

Risk of priapism (prolonged erection) noted as a serious adverse event

Published Findings

Peer-reviewed studies with linked sources

Study	Model	Key Finding	Year	Source
Eumelanin induction in fair-skinned subjects	Human (RCT, n=65)	100% of treated subjects showed melanin increase; effective even in MC1R variant carriers who typically cannot tan	2006	Br J Dermatology ↗
Erectile response in psychogenic ED	Human (RCT, n=20)	85% erectile response rate (17/20) vs 15% placebo (3/20); mean tip rigidity >80% for ~40 min	1998	Urology ↗
Phase I safety and pharmacokinetics	Human (Phase 1)	Dose-dependent tanning and side effects; nausea most common AE; established initial safety parameters	1996	Life Sciences ↗
Discovery and development review	Review	Comprehensive review of MT-I and MT-II development history, receptor pharmacology, and clinical progression	2006	Peptides ↗
Bremelanotide in female sexual arousal	Human (n=18)	PT-141 (MT-II derivative) showed positive subjective sexual response in premenopausal women with arousal disorder	2004	Int J Impotence Res ↗
Melanocortin receptor pharmacology	Animal (Multiple)	Characterized MC1R-MC5R binding profiles; confirmed non-selective agonism with highest affinity at MC1R and MC4R	2001	Research Literature ↗
MT-II tanning and UV protection analysis	Animal / Human (Mixed)	Increased eumelanin provides some UV protection, though not equivalent to a natural gradual tan	2006	Research Literature ↗

⚠️ Model type is clearly indicated for each entry. Research on Melanotan II was discontinued due to side effect concerns. The derivative PT-141 progressed to FDA approval.

Research Applications

Areas of active investigation in peer-reviewed literature

Investigated in MC1R-mediated melanogenesis and UV-independent skin pigmentation

Studied in MC4R-mediated pro-erectile signaling pathways in the central nervous system

Explored in hypothalamic energy homeostasis and appetite regulation through MC3R/MC4R

Examined as a photoprotective agent for potential skin cancer prevention

Evaluated in sexual arousal and desire pathways in both male and female subjects

Assessed in melanocortin receptor pharmacology and non-selective agonist profiling

Investigated as a precursor compound in the development of PT-141 (bremelanotide)

Studied in exocrine gland function through MC5R interaction pathways

Delivery Methods Studied in Research

Investigational administration routes evaluated in published studies

Subcutaneous Injection

Primary administration route evaluated in clinical trials; localized delivery beneath the skin

Intranasal Administration

Investigated in select studies as an alternative non-injection delivery method

Oral Administration

Not a primary route studied for MT-II; peptide susceptible to enzymatic degradation in the GI tract

Dosing Ranges Studied in Research

In published clinical research, investigational dosing has ranged between 0.010 mg/kg and 0.025 mg/kg body weight administered via subcutaneous injection. The 1996 Phase 1 study evaluated escalating doses to establish initial safety parameters. Community reports describe loading protocols of 250–500 mcg daily with maintenance of 500–1,000 mcg weekly.

⚠️ These figures are presented for scientific reference only and do not constitute usage recommendations. No standardized human dosing protocol has been established through completed regulatory trials.

Why It Arrives as a Powder

Understanding lyophilized formulation in research peptides

❄️

Stability Preservation

Lyophilization removes water content, significantly reducing the rate of chemical degradation. This preserves the peptide's structural integrity during storage and transport.

📅

Extended Shelf Life

Dry powder form can maintain potency at -20°C for extended periods, far exceeding the approximately 30-day window for reconstituted liquid preparations.

🛡️

Degradation Prevention

Peptide bonds are susceptible to hydrolysis in aqueous environments. Removing the solvent eliminates this primary degradation pathway.

🔬

Laboratory Preparation Standards

Reconstitution in research settings follows established protocols using bacteriostatic water or sterile saline, allowing precise concentration control.

✅

Sterile Research Conditions

Lyophilized preparations are processed under controlled, low-bioburden environments. Aseptic reconstitution maintains the sterility required for reliable research outcomes.

Transparency & Quality Verification

Analytical standards applied to research-grade peptide materials

🧪

Third-Party Analytical Testing

Independent laboratories perform comprehensive analysis on each production batch, ensuring unbiased verification of compound identity and purity.

📊

Purity Verification (HPLC)

High-Performance Liquid Chromatography confirms peptide purity levels, typically targeting ≥98% for research-grade material.

🔬

Identity Confirmation (Mass Spectrometry)

Mass spectrometry validates molecular weight and structural identity, confirming the compound matches its expected profile.

📋

Batch-Specific Certificates of Analysis

Each lot is accompanied by a unique COA detailing purity percentage, lot number, test date, labeled vs. actual content, and testing laboratory.

📁

Documentation Transparency

All analytical results, testing methodologies, and laboratory credentials are made available for researcher review and institutional compliance.

🌡️

Storage Verification Standards

Cold-chain integrity monitoring ensures proper temperature maintenance from production through delivery, preserving compound stability.

Related Peptides

Other compounds under active investigation

Frequently Asked Questions

Investigational context for common inquiries

Melanotan II is a synthetic cyclic heptapeptide composed of 7 amino acids arranged in a lactam ring structure. It was designed at the University of Arizona in the early 1990s as an analog of alpha-melanocyte stimulating hormone (α-MSH), the natural hormone responsible for stimulating melanin production in skin cells. The compound was originally developed to investigate whether enhanced pigmentation could offer protection against skin cancer.

Melanotan II reached Phase 1 clinical trials, which evaluated safety and pharmacokinetics. However, further clinical development was discontinued due to side effect concerns including nausea, mole changes, and cardiovascular risks. The compound remains a research tool with no regulatory approval from any agency. Its derivative, PT-141 (bremelanotide), was developed with improved selectivity and received FDA approval in 2019 for a different indication.

Randomized controlled trials demonstrated that Melanotan II effectively induces UV-independent skin darkening, including in individuals with MC1R genetic variants who are typically unable to tan. In a double-blind study, 85% of treated men experienced erectile responses compared to 15% on placebo. Appetite suppression has been consistently observed. However, these effects are accompanied by a notable side effect profile that led to discontinuation of clinical development.

The primary administration route studied in clinical trials is subcutaneous injection. Intranasal delivery has also been investigated in select studies as a non-injection alternative. Unlike some peptides, Melanotan II is not well-suited for oral administration due to enzymatic degradation in the gastrointestinal tract.

Yes, significant safety concerns have been documented. Nausea occurs in approximately 40% of subjects and is the most common initial side effect. Facial flushing affects ~35% of participants. Darkening of existing moles and formation of new nevi have been reported, requiring dermatological monitoring. Priapism (prolonged erection lasting >4 hours) is a serious adverse event requiring medical attention. Potential cardiovascular effects at higher doses and unregulated product quality are additional concerns.

Melanotan II is most directly compared to Melanotan I (afamelanotide) and PT-141 (bremelanotide). Melanotan I is a linear 13-amino acid peptide that selectively targets MC1R for pigmentation with minimal sexual side effects — it received regulatory approval as Scenesse for erythropoietic protoporphyria. PT-141 was derived from MT-II with modifications to reduce pigmentation while preserving MC4R-mediated sexual effects — it received FDA approval in 2019 for HSDD in premenopausal women. MT-II is unique in its non-selective activation of multiple melanocortin receptors.

No. Melanotan II is not approved by the FDA or any regulatory agency for human use. The FDA has issued warnings about MT-II products sold online and classifies it as an unapproved drug. It is also prohibited by the World Anti-Doping Agency (WADA). Its derivative PT-141 (bremelanotide) is the only melanocortin-based peptide to receive FDA approval for sexual dysfunction.

Because Melanotan II did not complete the full clinical trial process required for regulatory approval — and its clinical development was actively discontinued due to safety concerns — it cannot legally be marketed, sold, or represented as a treatment for any medical condition. The 'research use only' designation indicates that the compound is intended exclusively for scientific investigation in controlled laboratory settings.

Research-grade Melanotan II is typically analyzed using High-Performance Liquid Chromatography (HPLC) for purity assessment and mass spectrometry for molecular identity confirmation. Each production batch should be accompanied by a Certificate of Analysis (COA) from an independent, third-party laboratory detailing the purity percentage, lot number, and testing date.

In lyophilized (powder) form, Melanotan II should be stored at 2–8°C (refrigerated). Once reconstituted in solution, it should remain refrigerated and used within approximately 30 days. The compound appears as a white lyophilized powder and is soluble in water and saline. It should be protected from light and kept in its sealed container until preparation.

Sources & References

Peer-reviewed publications cited on this page

A randomized controlled trial of melanotan II in the induction of eumelanin synthesis in fair-skinned subjects ↗

Barnetson RS, Ooi TK, Zhuang L, et al. · British Journal of Dermatology (2006) · PMID: 16293341

Synthetic melanotropic peptide initiates erections in men with psychogenic erectile dysfunction: double-blind, placebo controlled crossover study ↗

Wessells H, Fuciarelli K, Hansen J, et al. · Urology (1998) · PMID: 9679884

Evaluation of melanotan-II, a superpotent cyclic melanotropic peptide in a pilot phase-I clinical study ↗

Dorr RT, Lines R, Levine N, et al. · Life Sciences (1996) · PMID: 8831529

Discovery and development of novel melanogenic drugs. Melanotan-I and -II ↗

Hadley ME, Dorr RT · Peptides (2006) · PMID: 16289566

An effect on the subjective sexual response in premenopausal women with sexual arousal disorder by bremelanotide (PT-141) ↗

Diamond LE, Earle DC, Heiman JR, et al. · International Journal of Impotence Research (2004) · PMID: 15073503

⚠️ Important Notice

For laboratory research use only. Not approved for human consumption. Not intended to diagnose, treat, cure, or prevent any disease.

All information presented on this page is derived from peer-reviewed literature and is provided exclusively for educational and scientific reference purposes. Nothing on this page constitutes medical advice, personal recommendations, or encouragement of any kind.

Melanotan II

10 mg

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Melanotan II

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Melanotan II

What Is Melanotan II?

How It Works

Melanocortin Receptor Binding

Intracellular Signaling Activation

Cellular Response

Research Outcome

Molecular Profile

Clinical Development Status

Research Timeline

Initial Development

Phase 1 Human Trial

Erectile Function Study

Female Sexual Function

Landmark Tanning RCT

PT-141 FDA Approval

WADA Prohibition

Current Status

What Does the Research Show?

Key Findings

Research Milestones

Observed Biological Effects

Safety Profile in Studies

Published Findings

Research Applications

Delivery Methods Studied in Research

Subcutaneous Injection

Intranasal Administration

Oral Administration

Dosing Ranges Studied in Research

Why It Arrives as a Powder

Stability Preservation

Extended Shelf Life

Degradation Prevention

Laboratory Preparation Standards

Sterile Research Conditions

Transparency & Quality Verification

Third-Party Analytical Testing

Purity Verification (HPLC)

Identity Confirmation (Mass Spectrometry)

Batch-Specific Certificates of Analysis

Documentation Transparency

Storage Verification Standards

Related Peptides

Frequently Asked Questions

Sources & References