Melanotan-1 (Afamelanotide)¶
Melanotan-1 (afamelanotide, CAS 75921-69-6) is a synthetic 13-amino acid cyclic peptide analog of α-melanocyte-stimulating hormone (α-MSH) with a molecular weight of approximately 1,646.8 Da. As the first synthetic melanocortin peptide developed for human research, Melanotan-1 is a selective MC1R (melanocortin-1 receptor) agonist that potently stimulates eumelanin synthesis in melanocytes. It is a primary research tool in melanocortin receptor pharmacology, melanogenesis, and photoprotection biology.
Technical Specifications¶
| Property | Value |
|---|---|
| CAS Number | 75921-69-6 |
| Molecular Formula | C₇₈H₁₁₁N₂₁O₁₉ |
| Molecular Weight | ~1,646.8 Da |
| Purity | ≥98% (HPLC-verified) |
| Appearance | Lyophilized white powder |
| Solubility | Soluble in sterile water and aqueous buffers |
| Storage | -20°C (lyophilized), 2–8°C (reconstituted) |
Mechanism of Action¶
Melanotan-1 binds with high affinity and selectivity to the melanocortin-1 receptor (MC1R), a Gαs-coupled GPCR expressed primarily on epidermal melanocytes. MC1R activation stimulates adenylyl cyclase, increasing intracellular cAMP and activating PKA, which phosphorylates the cAMP response element-binding protein (CREB). CREB then drives transcription of the microphthalmia-associated transcription factor (MITF), the master regulator of melanocyte differentiation and function. MITF upregulates the expression of key melanogenic enzymes — tyrosinase (TYR), tyrosinase-related protein 1 (TYRP1), and dopachrome tautomerase (DCT) — leading to increased synthesis of eumelanin (brown/black photoprotective pigment) over pheomelanin (red/yellow pigment). The resulting eumelanin deposition in keratinocytes provides enhanced photoprotection through UV absorption and free radical scavenging. Unlike Melanotan-2, Melanotan-1 exhibits high MC1R selectivity with minimal MC3R/MC4R engagement, producing melanogenesis without significant central nervous system or appetite effects.
Research Applications¶
- Primary: Melanocortin-1 receptor pharmacology — eumelanin synthesis, MITF signaling, melanocyte biology
- Secondary: UV photoprotection and DNA damage research, erythropoietic protoporphyria (EPP) models, skin pigmentation genetics
- Model Systems: In vitro (primary human melanocytes, B16-F10 melanoma cells, MC1R-transfected HEK293), in vivo (skin pigmentation and UV challenge models in rodents)
Quality Control & Analytical Methods¶
- HPLC: ≥98% purity verification at 214/220 nm (C18 reversed-phase column)
- Mass Spectrometry: ESI-MS for molecular weight confirmation (~1,646.8 Da)
- Peptide Content: Amino acid analysis (AAA) for net peptide content determination
- Endotoxin: <1 EU/mg (LAL assay)
- TFA Content: <1% (ion chromatography)
Stability & Storage¶
| Condition | Stability |
|---|---|
| -20°C (lyophilized) | 24 months |
| 4°C (lyophilized) | 6 months |
| 25°C (lyophilized) | 1 month |
| Reconstituted (4°C) | 7 days |
| Reconstituted (-20°C) | 30 days |
Key Research References¶
- Hadley & Dorr (2006) — Melanocortin peptides: from the bench to the bedside. Peptides. PMID: 16558908
- Minder et al. (2009) — Afamelanotide for erythropoietic protoporphyria. N Engl J Med. PMID: 19164166
- Abdel-Malek et al. (2006) — The melanocortin-1 receptor and human pigmentation. Pigment Cell Res. PMID: 16979598
Source & Purchase¶
For researchers requiring research-grade MELANOTAN 1 with full analytical documentation including HPLC, LC-MS, and Certificate of Analysis, visit the HK Peptides product page for specifications, bulk pricing, and ordering.
Related Molecules¶
- Melanotan-2 — Broad-spectrum melanocortin receptor agonist
- PT-141 — Bremelanotide, MC3R/MC4R selective
- KPV — α-MSH C-terminal fragment, anti-inflammatory
- All Product Specifications
FAQ¶
Q: What purity level is standard for Melanotan-1? A: HK Peptides supplies Melanotan-1 at ≥98% purity by HPLC with full COA documentation.
Q: How should Melanotan-1 be stored for research use? A: Lyophilized Melanotan-1 should be stored at -20°C, protected from light. Reconstituted solutions at 4°C for short-term use (up to 7 days).