Description
Setmelanotide is a potent cyclic peptide analog of ?-melanocyte stimulating hormone (?-MSH) and selectively activates MC4R in the hypothalamus to suppress appetite and increase energy expenditure. It is the first approved pharmacological agent for obesity driven by rare genetic deficiencies in POMC, PCSK1, LEPR, or Bardet-Biedl syndrome. Engineered for high specificity, Setmelanotide avoids cardiovascular side effects typical of earlier MC4R agonists. With GMP-grade manufacturing and ?99.93% purity, it’s a reliable tool for advanced metabolic and genetic obesity research.
Product Specifications
| Parameter | Details |
|---|---|
| Product Name | Setmelanotide |
| Synonyms | RM-493, BIM-22493, IRC-022493 |
| CAS Number | 920014-72-8 |
| Purity | ?99.93% (HPLC) |
| Classification | MC4R agonist peptide |
| EC?? (MC4R) | ~0.27 nM |
| Molecular Formula | C??H??N??O?S? |
| Molecular Weight | ~1,117 Da |
| Appearance | White to off-white powder |
| Solubility | Soluble in aqueous buffers and DMSO |
| Storage | –20 °C, light and moisture protected |
| GMP Compliance | Yes |
| Intended Use | Laboratory research use only |
Mechanism of Action & Research Applications
Setmelanotide binds MC4R in the hypothalamus, enhancing cAMP signaling to suppress hunger and boost energy use. It’s used in research on:
Genetic obesity due to POMC, PCSK1, or LEPR deficiencies
Bardet-Biedl syndrome obesity models
Appetite regulation and metabolic thermogenesis studies
Energy expenditure and weight control mechanisms
Unlike earlier MC4R agonists, Setmelanotide does not raise heart rate or blood pressure in tested models.
Side Effects (For Research Context Only)
Commonly observed in clinical and experimental contexts:
Injection site reactions
Skin hyperpigmentation or darkening of existing nevi
Gastrointestinal symptoms: nausea, vomiting, abdominal discomfort
Headache and fatigue
Rare behavioral effects: spontaneous erections, mood changes
Mild hypotensive effects have been reported under specific conditions
These findings help guide dosage and monitoring strategies in preclinical research.
Disclaimer
Setmelanotide is strictly for laboratory research use only. Not approved for clinical, diagnostic, or therapeutic use.


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