Also known as: 121062-08-6, Melanotan-II, UPF5CJ93X7, DTXSID90153135, L-Lysinamide, N-acetyl-L-norleucyl-L-alpha-aspartyl-L-histidyl-D-phenylalanyl-L-arginyl-L-tryptophyl-, cyclic (2-7)-peptide, RefChem:925444, DTXCID3075626, MT-II
Melanotan II (121062-08-6, Melanotan-II, UPF5CJ93X7) is classified under melanocortin agonists, sold for research use only and not approved for human consumption.
Aggregated from the cited literature below. We summarize sources — we don't author claims.
Melanotan-II (MT-II) is described in the provided literature as a lactam-bridged cyclic heptapeptide analog of alpha-melanocyte-stimulating hormone (alpha-MSH). It has been evaluated in vitro as a “superpotent” melanotropic peptide, studied in a pilot phase-I clinical setting, investigated for diet-induced neurobehavioral changes in zebrafish, used as a starting point for peptide engineering to obtain different melanocortin receptor agonist profiles, and discussed in relation to renal infarction reports and preformulation properties.
Mechanism (as reported)
A study characterizing MT-II in terms of receptor targeting describes MT-II as a melanotropin (melanocortin) receptor-targeting agent (PMID 37478579). Another paper describes MT-II as an unselective agonist of human melanocortin receptors (hMCRs) and discusses replacing its lactam cyclization to tune binding/functional selectivity (PMID 35188390).
Key findings (each cites a source)
Melanotan-II (MT-II) is described as a lactam-bridged cyclic heptapeptide analog of alpha-melanocyte-stimulating hormone (alpha-MSH) with a structure reported as Ac-Nle4-Asp5-His6-D-Phe7-Arg8-Trp9-Lys10 alpha-MSH4-10-NH2. [PMID 8637402]
In vitro characterization in the clinical pilot report describes MT-II as having “superpotent melanotropic activity.” [PMID 8637402]
In a zebrafish model, zebrafish fed a short-term high-fat diet showed recognition memory impairment, elevated anxiety levels, and reduced exploratory propensity after three weeks, and these high-fat diet-induced abnormalities were reported to be reversed by MT-II treatment. [PMID 37478579]
A pilot phase-I study in 3 normal male volunteers reported that MT-II produced tanning activity in humans, with increased pigmentation observed 1 week after dosing ended. [PMID 8637402]
In that phase-I pilot study, Grade II somnolence and fatigue were reported for one subject at a higher dose level, along with mild nausea at most MT-II dose levels; a stretching/yawning complex correlated with intermittent spontaneous penile erections, as described in the report. [PMID 8637402]
Research using MT-II as a parent compound described an approach (“Chemical Linkage of Peptide onto Scaffolds”) that replaced MT-II’s lactam cyclization with xylene-derived thioethers and reported binding affinities spanning low nanomolar to sub-micromolar ranges; the paper further reported functional selectivity toward hMC1R for a specific designed compound relative to MT-II. [PMID 35188390]
A peptide chemistry study reported efficient condensation of a 5-hydroxypyrroloindoline with cysteine-thiol or tryptophan-indole to form tryptathionine or 2,2'-bis-indole “staple” constructs applicable to α-MSH/MT-II-related targeting using α-MSH for investigating chemoselectivity and affinity; it reported nanomolar Ki values and one sub-nanomolar Ki value. [PMID 38285527]
A review and case report discuss Melanotan II as a non-selective melanocortin-receptor agonist and describe the literature context in which thrombotic pharmacological influence and possible direct toxic effect on renal parenchyma were considered in a proposed mechanism for renal injury. [PMID 31953620]
A preformulation study measured dissociation constants (via potentiometric titration and UV spectrophotometry), pKa values (histidine and arginine), and apparent partition coefficient parameters at multiple pH values; it reported an observed bioavailability of 4.6% in the rat and suggested that the compound may be a suitable candidate for oral delivery based on these data. [PMID 7983590]
Vendor test rankings (20)
Vendors ranked by their independent third-party test grade for Melanotan II, attributed to Finnrick. The grade is their verdict, not ours.
Real third-party HPLC results aggregated from Peptigrity, each attributed to the lab that ran it — average purity 99.6% across 260 tests. Not our verdict.
Lan EL, Ugwu SO, Blanchard J, Fang X, Hruby VJ, Sharma S · Journal of pharmaceutical sciences · 1994 · PMID 7983590
FAQ
What is Melanotan II?
Melanotan II (121062-08-6, Melanotan-II, UPF5CJ93X7) is classified under melanocortin agonists, sold for research use only and not approved for human consumption. Research goals associated with it include skin, hair & pigmentation, sexual & reproductive.
Is Melanotan II FDA-approved?
No. Melanotan II is sold for research use only and is not approved for human consumption.
What does the research on Melanotan II say?
peptideone aggregates 12 references from PubMed for Melanotan II. The summary on this page digests them with citations; we summarize sources and make no efficacy claims.