Melanotan 1 (Afamelanotide) | Linear MC1R Agonist | ≥99% HPLC Verified

PRODUCT SPECIFICATIONS

• Chemical Name : [Nle⁴, D-Phe⁷]-$alpha$-MSH
• Systematic Name : Ac-Ser-Tyr-Ser-Nle-Glu-His-D-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH2
• Peptide Classification : Synthetic linear analogue of alpha-melanocyte-stimulating hormone ($alpha$-MSH)
• Peptide Type : MC1R-selective melanocortin receptor agonist
• Molecular Formula : $C_{78}H_{111}N_{21}O_{19}$
• Molecular Weight : 1646.85 g/mol
• CAS Registry Number : 75921-69-6
• Purity : $ge99%$ (HPLC verified; specifically tested for D-Phe⁷ racemization)
• Solubility : Soluble in sterile water and dilute acetic acid; pH-dependent stability
• Storage : Lyophilized powder at $-20^{circ}C$, protected from light and moisture
• Molecular Structure : Linear 13-amino acid peptide with critical D-Phe substitution and N-acetyl/C-amide termini

Disclaimer: For Research Use Only (RUO). Not for human or veterinary use. Not for cosmetic application.

Melanotan 1 is a superpotent melanocortin analog engineered to overcome the rapid enzymatic degradation of natural $alpha$-MSH while maintaining exceptional selectivity for MC1R. Through rational drug design, the strategic inclusion of D-Phenylalanine (D-Phe) at position 7 and L-Norleucine (Nle) at position 4 confers enhanced enzymatic stability and prolonged receptor occupancy. The addition of N-acetyl and C-amide terminal modifications provides resistance to exopeptidase degradation, enabling extended half-lives compared to the natural hormone.

In the research context, Melanotan 1 serves as a critical selective probe for mapping peripheral melanocortin signaling. It is extensively utilized to study:

Melanocyte Biology : Tyrosinase activation and eumelanin synthesis in human and murine models.
Photoprotection Mechanisms : UV absorption capacity, ROS scavenging, and DNA repair pathway activation (Nucleotide Excision Repair).
Receptor Pharmacology : Binding kinetics and signal transduction specificity at MC1R vs. off-target MCR subtypes (MC3R/MC4R).

Unlike Melanotan II’s non-selective, broad-spectrum activation across MC1R, MC3R, MC4R, and MC5R, Melanotan 1’s MC1R-specific targeting eliminates confounding variables from peripheral CNS activity, energy homeostasis disruption, or immune activation—making it the gold standard for investigating pure pigmentation and photoprotection biology.

EXPERIMENTAL & ANALYTICAL USE

Melanotan 1 is utilized in laboratory research for:

Receptor Selectivity Profiling : Determining binding constants ($K_i$) and signal transduction efficacy specifically at MC1R interfaces to establish baseline pharmacodynamics without confounding MC4R signaling.

Melanogenesis & Photoprotection : Investigating eumelanin synthesis pathways, MITF upregulation, and tyrosinase kinetics.

Photosensitivity Disorder Modeling : Studying molecular mechanisms of light-induced phototoxicity in Erythropoietic Protoporphyria (EPP) and Solar Urticaria (SU).

DNA Damage & Repair Pathways : Exploring potential links between MC1R activation and Nucleotide Excision Repair (NER) pathway enhancement in UV-exposed skin.

Toxicology & Safety Profiling : Dissecting which melanocortin-mediated adverse effects stem from peripheral MC1R activation versus central MC4R activity.

Analytical Calibration : Serving as a peptide reference standard for LC-MS/MS detection, impurity quantification, and metabolite profiling.

TOXICOLOGY AND DETECTION METHODS

For forensic and anti-doping research, Melanotan 1 is identified in biological matrices using Liquid Chromatography-Tandem Mass Spectrometry (LC-MS/MS).

Primary Analyte: The intact parent peptide is monitored using the doubly charged precursor ion $[M+2H]^{2+}$ at m/z 823.9 (reflecting the linear 13-amino acid structure at 1646.8 Da).

Metabolite Profile: Unlike the cyclic Melanotan 2, MT-1’s linear structure undergoes predictable enzymatic cleavage:

• N-terminal degradation: Loss of acetyl-modified norleucine residue.
• ○ C-terminal cleavage: Sequential removal of lysine-amide.

Adverse Event Mechanisms: Unlike Melanotan 2’s association with renal infarction and systemic hypertension (via non-selective MC4R activation), Melanotan 1’s MC1R-selective mechanism is not implicated in thrombotic microangiopathy or sympathomimetic toxicity. Research confirms that MT-1-related adverse effects are primarily local (injection site reactions) or melanocyte-specific (naevus darkening)

HANDLING AND STABILITY

Melanotan 1 is supplied as a lyophilized white powder (acetate salt).

Reconstitution : Soluble in sterile bacteriostatic water or normal saline. For extended stability during multi-day assays, reconstitution in 0.1% acetic acid is often preferred to prevent base-catalyzed deamidation.

Linear Structure Sensitivity : While the N-acetyl/C-amide termini confer serum stability, the peptide is sensitive to exopeptidases. Avoid repeated freeze-thaw cycles which can disrupt the conformational integrity.

Storage : Lyophilized vials must be stored at $-20^{circ}C$. Reconstituted aliquots should be used immediately or stored at $-80^{circ}C$.

RESEARCH USE ONLY

Melanotan 1

• RESEARCH USE ONLY
• Not for therapeutic use.
• MC1R Selective Agonist
• Minimizes CNS Side Effects

RUO COMPLIANCE

All experimental applications of Melanotan 1 are conducted under Research Use Only (RUO) protocols.

FDA Status : While a pharmaceutical form (Scenesse®) is approved for EPP, this bulk lyophilized powder is not approved for human use or compounding.

WADA Status : Explicitly prohibited under Section S2 (Peptide Hormones).

Intended Use : Not for diagnostic, therapeutic, cosmetic, or veterinary purposes.

FEATURES / HIGHLIGHTS

• MC1R-selective agonist with minimal off-target MCR activity.
• Linear 13-amino acid structure optimized for pure skin pigmentation research.
• Verified $ge99%$ purity via HPLC to ensure D-Phe⁷ integrity.
• Extended in vivo half-life (vs. natural $alpha$-MSH) due to N-acetyl/C-amide termini.
• Superior safety profile vs. Melanotan II (no sympathomimetic toxicity).
• Strictly designed and labeled for Research Use Only (RUO).

WHY PROFOUND AMINOS?

Profound Aminos supplies high-purity Melanotan 1 (Acetate) for controlled pharmacological, toxicological, and receptor-binding research programs.

Researchers value:

1. Stereochemical Validation : RUO-grade Melanotan 1 with verified D-Phenylalanine integrity to ensure accurate receptor binding data ($K_i$).
2. Impurity Transparency : Rigorous removal of synthesis byproducts (aspartimides) that can skew immunogenicity assays.
3. Mass Spec Verification : Identity confirmation matching the specific linear mass ion (m/z 823.9) to detect degradation.
4. Regulatory Awareness : Clear documentation aligning with FDA 503A safety advisories and WADA classifications.

Profound Aminos is selected by research organizations studying melanocortin signaling, renal hemodynamics, and peptide toxicology.

References

1. Hadley ME, Hruby VJ, Blanchard J, et al. Discovery and development of novel melanogenic drugs. Melanotan I and II. Pharm Biotechnol. 1998;11:575-595.
2. Biolcati G, Marchesini E, Sorge F, et al. Long-term observational study of afamelanotide in erythropoietic protoporphyria. Br J Dermatol. 2015.
3. World Anti-Doping Agency (WADA). The 2025 Prohibited List: International Standard. Section S2. Effective January 1, 2025.
4. Breindahl T, Evans-Brown M, Hindersson P, et al. Identification and characterization by LC-UV-MS/MS of melanotan II… Drug Test Anal. 2015;7(2):164-172.

STORAGE INSTRUCTIONS

• Store lyophilized vial at $-20^{circ}C$ in a sealed container.
• Protect from UV light and moisture.
• Avoid repeated freeze-thaw cycles of the reconstituted solution.
• Maintained in a RUO-standard laboratory environment.

FAQS

Q1: What is the primary research application of Melanotan 1?

Melanotan 1 is used to investigate the signaling pathways of the Melanocortin 1 Receptor (MC1R), specifically studying effects on melanogenesis and photoprotection without the confounding CNS effects seen in MC4R agonists.

Q2: How does Melanotan 1 differ from Melanotan 2?

Melanotan 1 is a linear peptide with high selectivity for MC1R (skin), whereas Melanotan 2 is a cyclic peptide with non-selective binding (MC1R/MC3R/MC4R) that triggers appetite suppression and sexual arousal.

Q3: Is Melanotan 1 suitable for human use?

No. Research-grade Melanotan 1 is strictly for Research Use Only (RUO) and is not approved for human consumption, cosmetic tanning, or therapeutic use.

Q4: How should Melanotan 1 be stored for stability?

It should be stored lyophilized at $-20^{circ}C$. Once reconstituted, the linear peptide is sensitive to enzymatic degradation; therefore, immediate use or storage at $-80^{circ}C$ is recommended.

Q5: Is Melanotan 1 detected in sports drug testing?

Yes. Melanotan 1 is explicitly prohibited by WADA under Section S2 (Peptide Hormones) and can be detected via LC-MS/MS in urine and blood.

RUO DISCLAIMER

This compound is for Research Use Only (RUO). It is not intended for human, veterinary, or cosmetic applications. All information provided is based on peer-reviewed scientific literature and intended solely for laboratory and academic research purposes. This product is not a dietary supplement or drug.

DISCLAIMER:

• Products sold on our website are meant for scientific research purposes only, designed for in vitro testing and lab experimentation exclusively. These products are not intended to be used as foods, drugs or cosmetics, any sort of bodily introduction of the products into humans or animals is strictly prohibited. They must also not be misbranded, misused, or mislabeled, or used for anything other than research and scientific investigation.
• All the products you see on the website are being sold in a lyophilized powder state (freeze-dried), in a sealed sterile vial; and should be reconstituted.
  The product’s label clearly states the amount of product a vial contains; some products are offered in different variations.
• The products we are selling come in a sealed vial but require additional lab equipment for proper testing. 
• Though we make sure packaging, label, seals and writing does not differ from the product photos you see on our website, there is a chance for a minimal deviation.

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