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Identity And Chemical Background — Deep Dive

By Editorial Desk · published 2026-04-20 · last reviewed 2026-06-05 · Faq

Everything below concerns melanocortin receptor. We keep the language plain, cite what the science says, and separate well-supported claims from open questions.

Updated 2026-06-05. Numbers and descriptions here follow the published literature rather than marketing material.

Identity and Chemical Background

Melanocortin receptors comprise five subtypes with distinct tissue distributions and functions. Melanotan-2 is described in the literature as a non-selective agonist that engages several of these subtypes, including MC1R, MC3R, MC4R, and MC5R. MC1R is the subtype most directly linked to melanin production in skin cells. Because the compound is not subtype-selective, its observed effects in experimental settings are generally attributed to activity across multiple receptor pathways rather than to a single target.

Melanotan-2 is a synthetic linear peptide built from seven amino acids arranged in a short chain. Its sequence is commonly written as Ac-Nle-Asp-His-D-Phe-Arg-Trp-Lys-NH2, which includes a modified N-terminus and an amidated C-terminus. The molecule belongs to the melanocortin family and acts as a receptor agonist. Structural features such as the D-phenylalanine residue and the Nle substitution are associated with increased stability against enzymatic degradation relative to the natural parent peptide.

Melanotan-2 Identity And Regulatory Status

Activity is attributed to agonism at melanocortin receptors, particularly MC1R and MC4R. Activation of MC1R on melanocytes increases melanin synthesis, which underlies the reported tanning effect. MC4R engagement in the central nervous system is linked to appetite suppression and to effects on sexual arousal reported in early clinical studies. Those studies were small and were not designed to establish efficacy or long-term safety. Receptor selectivity among the melanocortin subtypes is not absolute, which complicates attribution of any effect to a single pathway.

Regulatory treatment varies between countries. Several national medicines agencies have classified the peptide as unapproved, and customs authorities in some jurisdictions seize shipments on that basis. A few jurisdictions channel supply through prescription-only frameworks that do not list the substance by name. Because the material circulates mainly through online vendors, composition and purity are rarely verified before sale. Surveys of unapproved peptide products have reported labels that did not match measured content in a substantial fraction of samples.

Melanotan-2 at a glance

PropertyValueNotes
Molecular formulaC50H69N15O9Free base; salt forms differ
Molecular weightApproximately 1024 g/molCalculated for the free base
AppearanceWhite to off-white powderTypically supplied as a lyophilised solid
SolubilitySoluble in water and polar solventsPoorly soluble in non-polar solvents
Typical storage-20 degrees Celsius, dry, protected from lightRefers to the solid form

Chemistry and Receptor Pharmacology

Published pharmacokinetic information is limited and comes mainly from small studies rather than registrational trials. Plasma half-life is usually described as short, on the order of tens of minutes, followed by rapid tissue distribution and clearance of the intact peptide. Metabolites and low concentrations of parent compound have been reported in urine, a detail relevant to anti-doping and forensic testing. Whether repeated exposure changes receptor sensitivity or clearance over time remains an open question. Values differ noticeably between analytical assays, so published numbers should be read as approximate rather than definitive.

Melanotan II is a synthetic cyclic heptapeptide with the sequence Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-NH2, corresponding to a molecular formula of C50H69N15O9 and a monoisotopic mass near 1024 daltons. It was designed as a structural analogue of alpha-melanocyte-stimulating hormone, a peptide hormone produced by cleavage of proopiomelanocortin. A lactam bridge between the aspartate and lysine side chains closes the ring, and the C-terminal amide removes a free carboxyl group. Both modifications increase resistance to enzymatic degradation compared with the linear parent hormone. Four substitutions distinguish it from afamelanotide, the linear analogue studied under the name melanotan I.

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Background and Chemical Profile

Two structural changes distinguish the synthetic peptide from the natural hormone. A norleucine residue replaces methionine at one position, and a D-configured phenylalanine replaces the natural L-form at another. Both substitutions slow enzymatic breakdown, which extends the molecule's persistence relative to the parent hormone. The lactam bridge further constrains the backbone into a stable conformation. These features are standard design strategies in peptide chemistry and are not unique to this compound; they appear across many research peptides built for improved stability.

The compound was developed in the late 1980s and early 1990s by academic researchers investigating melanocortin signaling and pigmentation. Early work explored whether synthetic analogs could reproduce effects of the natural hormone under controlled conditions. The molecule never advanced through the full regulatory pathway required for approval as a medicine. From the mid-2000s onward it appeared in unregulated consumer markets, often distributed through informal channels. That gap between research origins and commercial availability shapes how the compound is discussed today.

Melanotan-2 Structure and Receptor Pharmacology

No regulatory authority has approved melanotan-2 for human use, and several countries classify it as a prescription-only or controlled substance, which restricts lawful supply. Material sold online is generally labelled as a research chemical and is not required to meet pharmaceutical standards of identity or purity. Published human data consist mainly of small uncontrolled studies, case reports and adverse-event notifications, so the evidence base is descriptive rather than confirmatory. Whether repeated melanocyte stimulation alters long-term naevus behaviour remains an open question that no completed trial has resolved.

Melanotan-2 is a synthetic cyclic heptapeptide designed as a structural analogue of alpha-melanocyte-stimulating hormone, the endogenous tridecapeptide that regulates pigment production. Two modifications distinguish it from the natural hormone: norleucine replaces methionine at the N-terminus, which limits oxidation, and a D-phenylalanine substitution raises receptor affinity. The ring is closed through an aspartate-lysine lactam bridge, giving the molecule a constrained conformation. The free base has a molecular mass near 1024 daltons, and commercial material is usually supplied as an acetate salt. It appears in the literature as a research peptide rather than an approved therapeutic agent.

Background and Receptor Mechanism

Published human data come mostly from small, short studies rather than large controlled trials. Reported outcomes include increased skin pigmentation and, in some reports, effects on appetite and libido, but sample sizes are small and follow-up is limited. Whether long-term use produces durable pigment changes or adverse effects is not established. Because products sold outside pharmacies are not standardized, the actual content of any given vial is often unknown. Independent testing of such material is uncommon.

Melanotan II is a synthetic cyclic heptapeptide analog derived from the core sequence of alpha-melanocyte-stimulating hormone. Researchers at the University of Arizona synthesized it during the 1980s while studying pigmentation and appetite signaling. The compound is not an approved medicine in any major jurisdiction and appears mainly in laboratory and research-chemical settings. Its structure incorporates a lactam bridge between side chains, which constrains the ring and slows enzymatic breakdown relative to the natural hormone.

Notes from published material

In 1973, Cold Storage's Pasaraya Malaysia, a joint venture of Cold Storage's subsidiary Supermarkets Malaysia and "Malaysian interests" was responsible for the construction of Jaya Supermarket in Petaling Jaya, set to be completed in April 1974. In 1985, Cold Storage Malaysia opened its first Majik Market store in Bangsar Baru, Kuala Lumpur, It operated under a franchise from Mumford Inc of Atlanta, USA, which complements its existing Jaya Supermarket chain but differ in concept and management. Due to competition from 7-Eleven, whose Malaysian franchise was then operated by the Antah Holdings group, Cold Storage Malaysia phased out Majik Market as part of its streamlining process. Cold Storage Malaysia, along with Peremba, Gaya Timur and Jusco were responsible for the initial version of Jaya Jusco "superstores" in 1985, with three stores in Dayabumi, Taman Tun Dr Ismail and Subang Jaya. In 1987, Cold Storage Malaysia, which had been through a difficult financial phase in the previous three years, had a change in management with some senior executives leaving. In 1992, DFI Retail Group purchased the company, although no major changes were made to the Cold Storage brand. Cold Storage started the Fresh Food Distribution Centre in Singapore in 1999, a composite multi-temperature warehousing for fresh and frozen food distribution. In 2023, DFI Retail Group divested its Malaysian food retailing business (including Cold Storage brand in that country) to Macrovalue Sdn Bhd.

Lonapegsomatropin, sold under the brand name Skytrofa, is a human growth hormone used for the treatment of growth hormone deficiency. Lonapegsomatropin is a prodrug of somatropin. Lonapegsomatropin was approved for medical use in the United States in August 2021, and in the European Union in January 2022.

PDB Molecule of the Month Serpin Merops protease inhibitor claudication (Family I4) Archived 8 December 2016 at the Wayback Machine Serpins at the U.S. National Library of Medicine Medical Subject Headings (MeSH) James Whisstock laboratory at Monash University Jim Huntington laboratory Archived 30 October 2016 at the Wayback Machine at University of Cambridge Frank Church laboratory at University of North Carolina at Chapel Hill Paul Declerck laboratory at Katholieke Universiteit Leuven Tom Roberts laboratory at University of Sydney Robert Fluhr laboratory Archived 19 October 2014 at the Wayback Machine at Weizmann Institute of Science Peter Gettins laboratory at University of Illinois at Chicago Overview of all the structural information available in the PDB for UniProt: P01009 (Human Alpha-1-antitrypsin) at the PDBe-KB.

== Application == GPC is often used to determine the relative molecular weight of polymer samples as well as the distribution of molecular weights. What GPC truly measures is the molecular volume and shape function as defined by the intrinsic viscosity. If comparable standards are used, this relative data can be used to determine molecular weights within ± 5% accuracy. Polystyrene standards with dispersities of less than 1.2 are typically used to calibrate the GPC. Unfortunately, polystyrene tends to be a very linear polymer and therefore as a standard it is only useful to compare it to other polymers that are known to be linear and of relatively the same size.

Sources: en.wikipedia.org

Background from the literature

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Sources: en.wikipedia.org

Frequently asked questions

Is melanotan-2 a naturally occurring substance?

No. Melanotan-2 is manufactured synthetically. The naturally occurring peptide in the same family is alpha-melanocyte-stimulating hormone, which the body produces as part of normal endocrine and neural signalling.

How is melanotan-2 distinguished from afamelanotide?

Both are synthetic analogues derived from the same parent hormone. Reference descriptions usually characterise afamelanotide as more selective for the MC1R subtype, whereas melanotan-2 is reported to interact with a wider range of melanocortin receptors.

Why does the compound appear in tanning-related discussion?

Early studies explored melanocortin signalling and pigmentation, which later led to informal use of the label tanning peptide. That label is not a regulatory category and does not imply approved status for any purpose.

Is melanotan II approved for medical use?

No. No major regulatory agency has granted a marketing authorisation for melanotan II as a medicine. Products sold under this name are generally presented as laboratory reagents and are not subject to the batch-release testing applied to approved drugs.

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