Melanotan I (afamelanotide) is a synthetic analog of alpha-melanocyte-stimulating hormone (α-MSH) that binds MC1R on melanocytes with higher affinity and far greater resistance to enzymatic breakdown than the endogenous hormone. MC1R activation triggers cAMP and protein kinase A signaling, activates MITF, and increases tyrosinase—the key melanogenesis enzyme. Melanocytes then produce more eumelanin, the dark photoprotective pigment that absorbs UV and quenches free radicals, unlike pheomelanin, which offers little protection and is associated with higher risk in fair skin.
Beyond pigmentation, MT1 enhances DNA repair via nucleotide excision repair—the pathway that removes UV-induced pyrimidine dimers underlying photocarcinogenesis. That dual profile—pigmentation plus repair—underpins regulatory approval: afamelanotide as an implant (Scenesse) is approved by the EMA and FDA for erythropoietic protoporphyria (EPP), a rare condition with severe photosensitizing pain on minimal sun exposure. Trials showed significantly longer pain-free sun exposure. An anti-inflammatory profile is also described via cytokine modulation and reduced neuroinflammation through MC1R on microglia.
Key distinction from MT2: MT1 has negligible MC4R affinity, avoiding central effects on appetite, sexual arousal, and autonomic tone typical of MT2. That makes MT1 more predictable and safer when the goal is melanogenesis and photoprotection alone. Tan develops more slowly than with MT2 but without the accompanying CNS side effects.
🌞 Photoprotection and melanogenesis (MC1R): ★★★★★
🔧 DNA repair (nucleotide excision repair): ★★★★☆
🔥 Anti-inflammatory profile: ★★★☆☆
✅ Safety: ★★★★☆ (regulator-approved for EPP; no significant MC4R activity)
⚠️ Possible sensations and side effects: early nausea, pigment spots with overdose; generally well tolerated
🤝 Combinations (goal → stack)
🌞 Skin photoprotection + matrix → MT1 + GHK-Cu
💇 Hair pigmentation → MT1 + PTP-20
🛡️ Skin + immune background → MT1 + Thymosin Alpha 1
| CAS number | 75921-69-6 |
| Batch purity | 99.72 % |
Full details in our guide
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