MT-II Melanotan II 10mg
Melanotan II
Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-NH2
Overview
Melanotan II is a synthetic cyclic heptapeptide analogue of alpha-melanocyte-stimulating hormone (alpha-MSH). It was developed at the University of Arizona by Victor Hruby and Mac Hadley in the 1990s. As a non-selective melanocortin receptor agonist, MT-II binds and activates MC1R, MC3R, MC4R, and MC5R subtypes, producing a broad range of physiological effects. Activation of MC1R on melanocytes stimulates melanogenesis — the production and distribution of melanin pigment. This involves upregulation of tyrosinase and other melanogenic enzymes through the cAMP/PKA/CREB signaling cascade. The result is increased eumelanin synthesis, which produces skin darkening (tanning) without UV exposure. MC4R activation in the hypothalamus mediates two additional effects: appetite suppression and sexual arousal. The sexual function effects of MT-II led to the development of the more selective MC4R agonist bremelanotide (PT-141), which was subsequently approved by the FDA for hypoactive sexual desire disorder. MC3R and MC4R activation also influences energy homeostasis and body composition, with preclinical research showing reduced food intake and fat mass in animal models.
Mechanism of Action
Melanotan II is a synthetic cyclic heptapeptide analogue of alpha-melanocyte-stimulating hormone (alpha-MSH). It was developed at the University of Arizona by Victor Hruby and Mac Hadley in the 1990s. As a non-selective melanocortin receptor agonist, MT-II binds and activates MC1R, MC3R, MC4R, and MC5R subtypes, producing a broad range of physiological effects. Activation of MC1R on melanocytes stimulates melanogenesis — the production and distribution of melanin pigment. This involves upregulation of tyrosinase and other melanogenic enzymes through the cAMP/PKA/CREB signaling cascade. The result is increased eumelanin synthesis, which produces skin darkening (tanning) without UV exposure. MC4R activation in the hypothalamus mediates two additional effects: appetite suppression and sexual arousal. The sexual function effects of MT-II led to the development of the more selective MC4R agonist bremelanotide (PT-141), which was subsequently approved by the FDA for hypoactive sexual desire disorder. MC3R and MC4R activation also influences energy homeostasis and body composition, with preclinical research showing reduced food intake and fat mass in animal models.
Key Research Findings
- Dorr et al. (1996) conducted the first human study of melanotan II, demonstrating significant skin darkening and penile erections as side effects at doses of 0.010-0.025 mg/kg subcutaneously.
- Hruby et al. (1995) characterized the structure-activity relationships of MT-II, showing the cyclic lactam bridge confers enhanced receptor binding and metabolic stability compared to linear alpha-MSH.
- Wessells et al. (2000) demonstrated MT-II initiated penile erections in men with erectile dysfunction, establishing the melanocortin system as a target for sexual function research.
- Fan et al. (1997) showed MC4R activation by MT-II and alpha-MSH suppresses food intake in rodent models, establishing the melanocortin system's role in appetite regulation.
Citations & References
Evaluation of melanotan-II, a superpotent cyclic melanotropic peptide in a pilot phase-I clinical study
Dorr RT, Lines R, Levine N, et al. — Life Sci (1996)
Cyclic lactam alpha-melanotropin analogues of Ac-Nle4-cyclo[Asp5, D-Phe7, Lys10] alpha-melanocyte-stimulating hormone-(4-10)-NH2 with bulky aromatic amino acids at position 7 show high antagonist potency and selectivity at specific melanocortin receptors
Hruby VJ, Lu D, Sharma SD, et al. — J Med Chem (1995)
Synthetic melanotropic peptide initiates erections in men with psychogenic erectile dysfunction: double-blind, placebo controlled crossover study
Wessells H, Fuciarelli K, Hansen J, et al. — J Urol (1998)
Role of melanocortinergic neurons in feeding and the agouti obesity syndrome
Fan W, Boston BA, Kesterson RA, et al. — Nature (1997)
Dosage in Research
Initial human studies used subcutaneous doses of 0.010-0.025 mg/kg. Skin darkening studies used cumulative protocols with multiple low-dose administrations. Most research has used subcutaneous injection.
Dosage information is derived from published research literature and is presented for educational purposes only. This is not medical advice. All products are for laboratory research use only.
Storage & Handling
Store lyophilized (freeze-dried) powder at -20°C to 4°C in a dry environment protected from light. Unreconstituted peptide is stable for extended periods when stored properly.
Once reconstituted with bacteriostatic water or an appropriate solvent, store at 2-8°C and use within the timeframe specified on the Certificate of Analysis. Avoid repeated freeze-thaw cycles.
A Certificate of Analysis documenting purity, identity, and recommended storage conditions is included with every order.
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Research Use Only
All products are intended for laboratory research and educational purposes only. Products have not been evaluated by the FDA and are not intended for human consumption, diagnosis, treatment, or prevention of any disease. Purchasers must be 21+ and confirm research use intent.