Source comparison
Melanotan-1 Receptor Pharmacology: Comparison Table
α-MSH (endogenous) 2.0 nM Low 2–5 minutes Physiological melanogenesis and appetite regulation Natural ligand with poor stability. Rapid degradation limits therapeutic utility Melanotan-1 (afamelanotide) 0.23 nM Negligible 33 minutes (IV); days (SC depot) FDA-a
This comparison does not assign a generated winner or score.
- α-MSH (endogenous)
- 2.0 nM
- Low
- 2–5 minutes
- Physiological melanogenesis and appetite regulation
- Natural ligand with poor stability. Rapid degradation limits therapeutic utility
- Melanotan-1 (afamelanotide)
- 0.23 nM
- Negligible
- 33 minutes (IV); days (SC depot)
- FDA-approved for EPP photoprotection; off-label cosmetic tanning
- High MC1R selectivity with minimal off-target effects. Best safety profile for chronic use
- Melanotan-2 (bremelanotide precursor)
- 0.3 nM
- High (0.9 nM at MC4R)
- ~1 hour
- Investigational (not FDA-approved); cosmetic tanning and sexual dysfunction
- Potent melanogenic effect but significant MC4R activation causes sexual side effects and nausea
- Setmelanotide
- 0.5 nM (MC4R-selective)
- Very high (MC4R > MC1R)
- 5–6 hours
- FDA-approved for POMC/LEPR deficiency obesity
- MC4R agonist. Minimal melanogenic effect; used for appetite regulation, not pigmentation