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 (19)
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 219 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 9 references from PubMed for Melanotan II. The summary on this page digests them with citations; we summarize sources and make no efficacy claims.