Melanotan 1 (Afamelanotide) | Linear MC1R Agonist | ā„99% HPLC Verified
PRODUCT SPECIFICATIONS
- Chemical Name : [Nleā“, D-Pheā·]-$alpha$-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)
High-resolution 2D molecular structure of Melanotan 1, illustrated as a peptide backbone with repeating amide bonds, side chains, aromatic rings, and labeled heteroatoms (O and N) on a clean white background.” data-image-caption=”2D chemical structure of Melanotan 1 (a peptide) with highlighted oxygen and nitrogen atoms.
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- 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-Pheā· 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
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Disclaimer: For Research Use Only (RUO). Not for human or veterinary use. Not for cosmetic application.
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DESCRIPTION
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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.
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In the research context, Melanotan 1 serves as a critical selective probe for mapping peripheral melanocortin signaling. It is extensively utilized to study:
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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).
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Unlike Melanotan IIās non-selective, broad-spectrum activation across MC1R, MC3R, MC4R, and MC5R, Melanotan 1ās MC1R-specific targeting eliminates confounding variables from peripheral CNS activity, energy homeostasis disruption, or immune activationāmaking it the gold standard for investigating pure pigmentation and photoprotection biology.
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EXPERIMENTAL & ANALYTICAL USE
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Melanotan 1 is utilized in laboratory research for:
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Receptor Selectivity Profiling : Determining binding constants ($K_i$) and signal transduction efficacy specifically at MC1R interfaces to establish baseline pharmacodynamics without confounding MC4R signaling.
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Melanogenesis & Photoprotection : Investigating eumelanin synthesis pathways, MITF upregulation, and tyrosinase kinetics.
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Photosensitivity Disorder Modeling : Studying molecular mechanisms of light-induced phototoxicity in Erythropoietic Protoporphyria (EPP) and Solar Urticaria (SU).
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DNA Damage & Repair Pathways : Exploring potential links between MC1R activation and Nucleotide Excision Repair (NER) pathway enhancement in UV-exposed skin.
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Toxicology & Safety Profiling : Dissecting which melanocortin-mediated adverse effects stem from peripheral MC1R activation versus central MC4R activity.
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Analytical Calibration : Serving as a peptide reference standard for LC-MS/MS detection, impurity quantification, and metabolite profiling.
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TOXICOLOGY AND DETECTION METHODS
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For forensic and anti-doping research, Melanotan 1 is identified in biological matrices using Liquid Chromatography-Tandem Mass Spectrometry (LC-MS/MS).
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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).
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Metabolite Profile: Unlike the cyclic Melanotan 2, MT-1ās linear structure undergoes predictable enzymatic cleavage:
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- N-terminal degradation: Loss of acetyl-modified norleucine residue.
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- ā C-terminal cleavage: Sequential removal of lysine-amide.
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Adverse Event Mechanisms: Unlike Melanotan 2ās association with renal infarction and systemic hypertension (via non-selective MC4R activation), Melanotan 1ās 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)
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HANDLING AND STABILITY
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Melanotan 1 is supplied as a lyophilized white powder (acetate salt).
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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.
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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.
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Storage : Lyophilized vials must be stored at $-20^{circ}C$. Reconstituted aliquots should be used immediately or stored at $-80^{circ}C$.
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RESEARCH USE ONLY
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Melanotan 1
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- RESEARCH USE ONLY
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- Not for therapeutic use.
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- MC1R Selective Agonist
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- Minimizes CNS Side Effects
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RUO COMPLIANCE
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All experimental applications of Melanotan 1 are conducted under Research Use Only (RUO) protocols.
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FDA Status : While a pharmaceutical form (ScenesseĀ®) is approved for EPP, this bulk lyophilized powder is not approved for human use or compounding.
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WADA Status : Explicitly prohibited under Section S2 (Peptide Hormones).
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Intended Use : Not for diagnostic, therapeutic, cosmetic, or veterinary purposes.
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FEATURES / HIGHLIGHTS
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- MC1R-selective agonist with minimal off-target MCR activity.
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- Linear 13-amino acid structure optimized for pure skin pigmentation research.
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- Verified $ge99%$ purity via HPLC to ensure D-Pheā· integrity.
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- Extended in vivo half-life (vs. natural $alpha$-MSH) due to N-acetyl/C-amide termini.
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- Superior safety profile vs. Melanotan II (no sympathomimetic toxicity).
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- Strictly designed and labeled for Research Use Only (RUO).
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WHY PROFOUND AMINOS?
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Profound Aminos supplies high-purity Melanotan 1 (Acetate) for controlled pharmacological, toxicological, and receptor-binding research programs.
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Researchers value:
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- Stereochemical Validation : RUO-grade Melanotan 1 with verified D-Phenylalanine integrity to ensure accurate receptor binding data ($K_i$).
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- Impurity Transparency : Rigorous removal of synthesis byproducts (aspartimides) that can skew immunogenicity assays.
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- Mass Spec Verification : Identity confirmation matching the specific linear mass ion (m/z 823.9) to detect degradation.
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- Regulatory Awareness : Clear documentation aligning with FDA 503A safety advisories and WADA classifications.
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Profound Aminos is selected by research organizations studying melanocortin signaling, renal hemodynamics, and peptide toxicology.
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References
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- 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.
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- Biolcati G, Marchesini E, Sorge F, et al. Long-term observational study of afamelanotide in erythropoietic protoporphyria. Br J Dermatol. 2015.
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- World Anti-Doping Agency (WADA). The 2025 Prohibited List: International Standard. Section S2. Effective January 1, 2025.
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- 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.
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STORAGE INSTRUCTIONS
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- Store lyophilized vial at $-20^{circ}C$ in a sealed container.
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- Protect from UV light and moisture.
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- Avoid repeated freeze-thaw cycles of the reconstituted solution.
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- Maintained in a RUO-standard laboratory environment.
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FAQS
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Q1: What is the primary research application of Melanotan 1?
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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.
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Q2: How does Melanotan 1 differ from Melanotan 2?
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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.
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Q3: Is Melanotan 1 suitable for human use?
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No. Research-grade Melanotan 1 is strictly for Research Use Only (RUO) and is not approved for human consumption, cosmetic tanning, or therapeutic use.
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Q4: How should Melanotan 1 be stored for stability?
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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.
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Q5: Is Melanotan 1 detected in sports drug testing?
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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.
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RUO DISCLAIMER
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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.
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