MC1R Agonism & Melanogenesis Stimulation
Afamelanotide (Melanotan-I)
Melanotan I (MT1), clinically known as afamelanotide, is a synthetic analog of alpha-melanocyte-stimulating hormone (α-MSH), a naturally occurring neuropeptide derived from proopiomelanocortin (POMC). Developed initially at the University of Arizona, MT1 was engineered to be a more potent and metabolically stable version of α-MSH, with a half-life of approximately 1.5 hours compared to the native hormone's minutes-long duration.
MT1 is the only melanocortin receptor agonist to have received regulatory approval — it is approved in the European Union under the brand name Scenesse® for the prevention of phototoxicity in adults with erythropoietic protoporphyria (EPP), a rare genetic disorder causing extreme light sensitivity. This clinical validation distinguishes MT1 from most research peptides and provides a robust human safety and efficacy dataset.
Afamelanotide is a 13-amino-acid linear peptide with the sequence Ac-Ser-Tyr-Ser-Nle-Glu-His-D-Phe-Arg-Trp-Gly-Lys-Pro-Val-NH2. Key structural modifications compared to native α-MSH include: substitution of Met⁴ with norleucine (Nle) to prevent oxidative degradation, replacement of Phe⁷ with D-Phe to increase receptor binding affinity and metabolic stability, and N-terminal acetylation with C-terminal amidation to further resist enzymatic degradation.
These modifications collectively extend the biological half-life from approximately 2–3 minutes (native α-MSH) to approximately 1.5 hours, while also increasing potency at the melanocortin-1 receptor (MC1R) by approximately 100-fold compared to the native sequence.
MT1 functions as a potent agonist of the melanocortin-1 receptor (MC1R), a G-protein coupled receptor expressed predominantly on melanocytes in the skin. Upon binding to MC1R, MT1 activates the Gαs protein, stimulating adenylyl cyclase and increasing intracellular cyclic AMP (cAMP) levels. Elevated cAMP activates protein kinase A (PKA), which phosphorylates the transcription factor CREB (cAMP response element-binding protein).
Phosphorylated CREB activates the microphthalmia-associated transcription factor (MITF), the master regulator of melanocyte biology. MITF drives expression of tyrosinase, tyrosinase-related protein-1 (TRP-1), and TRP-2 — the key enzymes of the melanogenesis pathway — resulting in increased eumelanin production and enhanced photoprotection.
MT1 (Melanotan I, clinically known as afamelanotide) is a synthetic version of a hormone your body naturally produces called alpha-MSH. This hormone is part of your skin's built-in sun protection system — it's what triggers your skin to tan in response to UV exposure.
MT1 works by activating a receptor on melanocytes (the cells that produce skin pigment) called MC1R. When this receptor is activated, it triggers a chain reaction that increases production of eumelanin — the dark, protective form of melanin. Crucially, MT1 can do this without requiring UV exposure first. It's essentially activating the tanning pathway directly.
MT1 is the only peptide in this guide that has received full regulatory approval — it's sold in the EU as Scenesse® for a rare genetic condition called erythropoietic protoporphyria (EPP), where patients experience extreme pain from even brief sun exposure. This means MT1 has completed Phase III clinical trials and has a well-characterized human safety profile, which is rare in the peptide research space.
MT1 stands apart from most research peptides because it has genuine clinical validation behind it. The EU-approved formulation is a subcutaneous implant; Purgo Labs supplies the lyophilized powder format strictly for laboratory research use. The clinical data provides a strong mechanistic foundation for researchers studying melanocortin biology.
Binds MC1R on melanocytes, activating adenylyl cyclase → cAMP → PKA cascade that drives melanogenesis transcription factors.
PKA phosphorylates CREB, which activates MITF — the master regulator of melanocyte biology and eumelanin synthesis.
MITF drives expression of tyrosinase, TRP-1, and TRP-2, the enzymatic machinery of eumelanin production.
MC1R activation suppresses NF-κB-mediated inflammatory signaling, providing secondary anti-inflammatory effects.
Skin & Anti-Aging Research
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| Peptide Class | α-MSH analog (13 amino acids) |
| Molecular Weight | 1,646.8 Da |
| Receptor Target | Melanocortin-1 receptor (MC1R) |
| Clinical Status | EU-approved (Scenesse®) for EPP |
| Half-life | ~1.5 hours (vs. 2–3 min for native α-MSH) |
| Available Sizes | 10mg vials |
| Form | Lyophilized powder |
| Purity | ≥99% (third-party tested) |
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Purchase MT1 at Purgo LabsMedical Disclaimer: All content on this site is for educational and research purposes only. Research peptides are not FDA-approved for human use. Always consult a qualified healthcare professional before considering any peptide or supplement protocol. Nothing on this site constitutes medical advice, diagnosis, or treatment.
