What Is Melanotan 2?
Melanotan 2 (MT-2; sequence: Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-NH2) is a cyclic lactam analog of α-melanocyte stimulating hormone (α-MSH) developed at the University of Arizona in the 1980s as part of a program aimed at creating a safe tanning agent to reduce skin cancer incidence. Unlike its parent compound melanotan I (afamelanotide, which selectively targets MC1R), MT-2 is a nonselective melanocortin agonist activating MC1R, MC3R, MC4R, and MC5R — producing a broader set of physiological effects that have driven its extensive use as a research tool for the melanocortin system.
MT-2 served as the structural template from which PT-141 (bremelanotide) was derived — with PT-141 retaining the MC4R and MC3R activity while losing the cyclic structure’s MC1R potency. This lineage makes MT-2 uniquely valuable for comparative melanocortin receptor research.
Mechanism of Action
- MC1R Agonism: Stimulates melanocytes to produce eumelanin (dark brown-black pigment), increasing skin pigmentation — the originally intended pharmacological application
- MC3R Agonism: Influences energy balance, feeding behavior, and immune modulation through hypothalamic MC3R
- MC4R Agonism: Primary mediator of MT-2’s effects on sexual arousal, energy expenditure, and appetite suppression — the same receptor targeted by PT-141
- MC5R Agonism: Implicated in exocrine gland function and immune responses
- Nitric Oxide Release: MC4R activation increases hypothalamic NO, contributing to erectile/genital effects
Research Applications and Data
Pigmentation Research
- Demonstrated reliable tanning effect in Phase 1/2 human trials (Hadley et al., University of Arizona)
- Increased Melanin Index scores vs. placebo in fair-skinned participants
- Established as the primary research tool for MC1R biology and eumelanin synthesis pathways
Sexual Function Research
- Phase 1/2 studies demonstrated erection facilitation in men with psychogenic and organic ED
- Mechanistic studies established MC4R as the primary receptor mediating sexual arousal effects
- Served as proof-of-concept for the melanocortin-sexual function axis, leading to PT-141 development
Metabolic and Feeding Research
- MC4R-mediated appetite suppression documented in rodent feeding behavior studies
- Used extensively as a pharmacological probe for MC3R/MC4R function in energy balance research
- Nausea via area postrema MC3R activation — a key adverse effect that informed PT-141’s design to reduce emetic potential
Immune Research
- Documented anti-inflammatory effects via MC3R/MC5R in models of joint inflammation and sepsis
- MC1R activation on immune cells modulates macrophage and dendritic cell inflammatory cytokine production
MT-2 vs. PT-141 vs. Afamelanotide — Research Comparison
| Parameter | Melanotan 2 (MT-2) | PT-141 (Bremelanotide) | Afamelanotide (MT-1) |
|---|---|---|---|
| Structure | Cyclic heptapeptide | Cyclic heptapeptide (linear analog) | Linear tridecapeptide |
| MC1R potency | High | Low | High (selective) |
| MC4R potency | High | High (primary target) | Low |
| FDA approval | None | Yes (Vyleesi — HSDD) | Yes (Scenesse — EPP) |
| Primary research use | Pan-MC receptor pharmacology | MC4R-mediated sexual function | MC1R, photoprotection |

HPLC Verified
Melanotan 2 Acetate (MT-2) 10mg
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