Melanotan 1 and 2 are synthetic analogues of α-MSH, designed to bind melanocortin receptors with high affinity. This page summarises the biochemistry, mechanism of action, and published research underpinning their use in in vitro studies.
Alpha-melanocyte-stimulating hormone (α-MSH) is a tridecapeptide derived from pro-opiomelanocortin (POMC). It acts as a natural agonist at melanocortin receptors MC1R–MC5R, regulating pigmentation, inflammation, and energy homeostasis.
Melanotan 1 and Melanotan 2 are synthetic cyclic α-MSH analogues with structural modifications that increase receptor affinity and resistance to enzymatic degradation compared with endogenous α-MSH. These properties make them useful compounds for investigating melanocortin receptor biology in laboratory research.
MT-1 and MT-2 bind selectively to melanocortin receptors — primarily MC1R (pigmentation) and MC3R/MC4R (metabolic regulation). Their cyclic structure confers greater receptor affinity than endogenous α-MSH.
Upon binding, adenylyl cyclase is activated via Gs proteins, elevating intracellular cyclic AMP. This downstream cascade drives melanogenesis in melanocyte cultures and modulates inflammatory cytokine expression.
Elevated cAMP activates CREB transcription factor, upregulating MITF and tyrosinase expression. In vitro, this produces measurable dose-dependent increases in melanin synthesis in B16 melanoma and primary melanocyte lines.
MC1R and MC3R activation suppresses NF-κB and downstream pro-inflammatory mediators including TNF-α and IL-6. Research models utilise this to study melanocortin involvement in neuroinflammation and dermal inflammation.
MC4R agonism by MT-2 has been investigated in experimental models of energy homeostasis. In vitro hypothalamic studies demonstrate modulation of orexigenic neuropeptide signalling, making these compounds useful research tools for studying melanocortin pathways.
Both analogues incorporate D-amino acid substitutions and cyclisation that resist peptidase cleavage. This extended half-life in cell culture conditions makes them reproducible tools for multi-day in vitro assay formats.
Research Use Only. All information on this page is provided for educational and scientific reference purposes only. MelanoMax products are supplied exclusively for in vitro laboratory research. They are not approved for human or veterinary use, and nothing on this page constitutes medical advice. Researchers must ensure compliance with all applicable local regulations.