cyclic heptapeptide is one of those subjects where the details matter more than the headlines. This page pulls together the background, the mechanisms, and the practical points readers ask about most.
Last reviewed on 2026-01-05. Where a claim depends on a specific study, the study is described rather than over-claimed.
Melanotan-2, also written Melanotan II, is a synthetic cyclic heptapeptide designed as an analogue of alpha-melanocyte-stimulating hormone. Its sequence is Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-NH2, and the lactam bridge between the aspartate and lysine side chains constrains the peptide into a ring. This structural change increases receptor affinity and metabolic stability relative to the native hormone. The compound was created in the 1980s as a research tool for studying pigmentation biology.
Melanocytes are the pigment-producing cells of the skin, and they carry melanocortin-1 receptors on their surface. When the receptor is activated, cyclic adenosine monophosphate rises inside the cell and raises the activity of enzymes such as tyrosinase, which increases melanin output. Melanotan-2 binds melanocortin-1 receptors in vitro and in animal models, and this binding is generally described as the basis for the tanning effect. Other receptors account for different effects: melanocortin-4 receptors contribute to appetite and erectile signalling, while melanocortin-3 and melanocortin-5 receptors contribute to energy balance and exocrine function.
Early published reports described melanotan-2 as a tanning agent without sun protection, which means darkening is not the same as protection against ultraviolet radiation. Later studies explored the peptide in erectile dysfunction, hemorrhagic shock, and some skin conditions. No regulator in the United States or Europe has approved it for clinical use. Many products labelled melanotan-2 are sold without approval and their identity and purity are unverified. Its long-term safety in humans remains an open question.
Pharmacologically, melanotan-2 behaves as a non-selective agonist across the melanocortin receptor family. Binding at MC1R on dermal melanocytes promotes eumelanin synthesis, which underlies the tanning response described in early human work. Activity at the centrally expressed MC4R receptor is associated with reported effects on appetite and erectile function. Because the peptide does not discriminate strongly among receptor subtypes, attributing any single observed effect to one receptor pathway is generally not possible without selective antagonists or receptor knockout models.
Research interest has centred on photoprotection and pigmentation, with a smaller body of work on appetite and sexual function. Published human data remain limited to small, frequently uncontrolled studies, and the compound has never received marketing approval from a national medicines regulator. Most laboratory work treats it as a pharmacological tool for probing melanocortin signalling in cell culture or animal models. Whether pigmentation changes observed in people translate into measurable protection against ultraviolet-induced DNA damage remains an open question.
Melanotan-2 is a synthetic cyclic heptapeptide designed as an analogue of alpha-melanocyte-stimulating hormone, the naturally occurring peptide involved in pigmentation signalling. Its sequence is conventionally written as Ac-Nle-cyclo[Asp-His-D-Phe-Arg-Trp-Lys]-NH2, with a lactam bridge joining the aspartate side chain to the lysine side chain. The empirical formula is C50H69N15O9 and the monoisotopic mass lies near 1023.5 daltons. N-terminal acetylation and the D-configured phenylalanine both increase resistance to enzymatic breakdown compared with the parent hormone.
| Property | Value | Notes |
|---|---|---|
| Compound class | Synthetic cyclic heptapeptide | Alpha-MSH analogue containing a D-phenylalanine residue |
| Molecular formula | C50H69N15O9 | Average molecular mass approximately 1024.2 g/mol |
| Appearance | White to off-white lyophilised powder | Normally supplied as a freeze-dried solid in a sealed vial |
| Solubility | Freely soluble in water and polar solvents | Dissolves readily in aqueous buffers and in alcohol-water mixtures |
| Receptor targets | MC1R, MC3R, MC4R, MC5R | Acts as a non-selective melanocortin receptor agonist |
Outside regulated medicine, melanotan II circulates through online vendors as a research chemical, often marketed for tanning. Products sold this way vary widely in purity, concentration, and labeling accuracy, and independent testing has documented discrepancies. Published reports describe both pigment effects and adverse reactions, including nausea, flushing, and darkening of existing moles. Long-term safety data are sparse, and no large controlled trial has established a risk profile. Questions about cumulative effects on melanocytes remain unresolved in the literature.
Melanotan II is a synthetic peptide analog modeled on alpha-melanocyte-stimulating hormone, a naturally occurring signaling peptide involved in pigmentation. Its structure is a cyclic heptapeptide containing two non-natural substitutions, norleucine at position four and D-phenylalanine at position seven. These modifications resist enzymatic breakdown and extend the molecule's activity relative to the native hormone. The compound binds melanocortin receptors and is studied mainly as a pharmacological tool rather than a therapeutic product. It has never received approval as a medicine in any major jurisdiction.
The compound was developed in the late 1980s and 1990s by academic researchers investigating photoprotection. The rationale held that stimulating melanin production might reduce ultraviolet damage to skin and lower skin cancer risk. Early work examined receptor binding, pigment response, and short-term tolerability in small studies. That program did not produce an approved drug, and formal development stalled after early-phase trials. Whether induced pigmentation confers meaningful photoprotection remains an open question.
The compound emerged from research programs in the 1980s that examined analogues of alpha-melanocyte-stimulating hormone for pigmentation and photoprotection. Investigators modified the native sequence to extend activity duration and potency. A related analogue, afamelanotide, was developed within the same broad line of inquiry and eventually gained approval in certain jurisdictions for a rare light-sensitivity condition. Melanotan-2 itself did not progress through the same regulatory route and has no approved therapeutic indication.
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.
=== Traditional Chinese medicine === Within traditional Chinese medicine E. sinensis was historically used to treat a variety of ailments, such as bruises, fractures, amenorrhea, postpartum blood stasis, and used as a pain reliever. Tubiechong could be prepared in different ways depending on what was being treated, preparation methods include, grinding, frying, water extraction, and rice wine extraction. The most common method being water or rice wine extraction. Only the females are used in medicine. There are claims by TCM physicians that Tubiechong can reduce and treat tumors, via actions on blood vessels. The apparent effect on the blood vessels is why it was prescribed for the ailments it was (and still is).
By 1928, he had reached a new height of power, controlling lands from Xikang to Chengdu. Liu declared ambitious plans to his subordinates: "First, we must unify Sichuan; then we must seize the Central Plains." He had begun establishing a political-military school in Chengdu to train the 24th Army for this task. The Sichuanese warlord Yang Sen had attempted a similar campaign by attacking the Wuhan government the prior year, suffering major defeat. Liu Wenhui had benefited from this, seizing many of Yang Sen's territories in the wake of his failed campaign. As part of his broader strategy, Liu had also supported Tang Shengzhi, Feng Yuxiang, and Yan Xishan, but they had been subdued by Chiang's forces for the time being, straining relations with the Nanjing government. Still, this did not stop Chiang from appointing him to high positions.Liu's nephew Liu Xiang was still the most powerful warlord in Sichuan, ruling Chongqing and the eastern portion of the province, but a new coalition of warlords had formed to oppose him. On 10 December 1928, Yang Sen, Li Jiayu, and Luo Zezhou sent a telegram denouncing Liu Xiang and organized a joint army to overthrow him. Facing defeat, Liu Xiang reached out to Liu Wenhui for aid, promising several territories in exchange for his support. Liu Wenhui did intervene, defeating the warlord coalition; in return, Liu Xiang ceded the Zigong, Neijiang, and Longchang areas to him. Having taken refuge with the Guangxi clique, Yang Sen reportedly vowed revenge against Liu Wenhui for his defeat.
Most of the rest of the world excluded prisoners as potential research subjects following formulation of the Nuremberg Code, based on its assertion that acceptable experimental subjects must be "so situated as to be able to exercise free power of choice". Despite regulations that limit circumstances where inclusion of vulnerable populations in clinical trials is permitted, such groups, such the economically disadvantaged, continue to be made part of research through coercive means as recently as 2015. International clinical trials day is celebrated on 20 May. The acronyms used in the titling of clinical trials are often contrived, and have been the subject of derision.
=== DMPK, ADME, and bioanalysis === BioDuro conducts in vitro ADME assays, in vivo PK/TK studies, metabolic stability studies, and bioanalytical method development using LC–MS/MS platforms. These services are used to characterize compound absorption, distribution, metabolism, and excretion profiles during preclinical development.
Sources: en.wikipedia.org
=== February === 3 February – Prime Minister Keir Starmer rejects an allegation that he broke COVID-19 regulations by having a voice coach present at a press conference where he responded to a Brexit deal negotiated by Boris Johnson. For the first time, Reform UK have led an opinion poll, after coming top with 25% in a YouGov poll for Sky News. Labour are second on 24%, with the Conservatives on 21%. Northern Ireland's Economy Minister, Conor Murphy steps down from the post and announces he will leave Stormont after being elected to the Irish Seanad. Caoimhe Archibald is appointed to replace him as Economy Minister. 4 February – BBC News reports that Jack Lopresti, the former Conservative MP for Filton and Bradley Stoke who lost the seat at the last general election has joined the Ukrainian military. Welsh Conservatives leader Darren Millar and his colleague Russell George miss a Senedd vote on the Eluned Morgan government's budget for 2025–26 because they have travelled to the United States for the annual National Prayer Breakfast. 5 February – Deputy Prime Minister Angela Rayner confirms that local elections in East Sussex, West Sussex, Essex, Thurrock, Hampshire, the Isle of Wight, Norfolk, Suffolk and Surrey will be delayed for a year to allow major local government reorganisations to take place. Four of the seven MPs suspended from the Labour Party for voting against the child benefit cap are readmitted to the party; they are Richard Burgon, Ian Byrne, Imran Hussain and Rebecca Long-Bailey.
Singapore has a tropical rainforest climate (Köppen: Af) with no distinctive seasons, uniform temperature and pressure, high humidity, and abundant rainfall. Temperatures usually range from 23 to 32 °C (73 to 90 °F). While temperature does not vary greatly throughout the year, there is a wetter monsoon season from November to February. From July to October, there is often haze caused by bush fires in neighbouring Indonesia, usually from the island of Sumatra. Singapore follows the GMT+8 time zone, one hour ahead of the typical zone for its geographical location. This causes the sun to rise and set particularly late during February, where the sun rises at 7:15 am and sets around 7:20 pm. During July, the sun sets at around 7:15 pm. The earliest the sun rises and sets is in late October and early November when the sun rises at 6:46 am and sets at 6:50 pm. Singapore recognises that climate change and rising sea levels in the decades ahead will have major implications for its low-lying coastline. It estimates that the nation will need to spend $100 billion over the course of the next century to address the issue. In its 2020 budget, the government set aside an initial $5 billion towards a Coastline and Flood Protection Fund. Singapore is the first country in Southeast Asia to levy a carbon tax on its largest carbon-emitting corporations producing more than 25,000 tons of carbon dioxide per year, at $5 per ton.
== Pharmacokinetics == With the once-monthly formulation of paliperidone palmitate, the time to peak is 13 days and the elimination half-life is 25 to 49 days; for the 3-month formulation, the time to peak is 30 to 33 days and the half-life is 84 to 95 days (deltoid muscle) or 118 to 139 days (gluteal). These data come from a 2021 review whose authors included employees of Janssen Research & Development, the manufacturer of paliperidone palmitate. The peak-to-trough ratio of paliperidone palmitate at steady state ranges from 1.56 to 1.70 with the 1- and 3-month formulations. No pharmacokinetic data for the 6-month formulation has been released as of January 2021. However, a 2025 case report described a patient who still had measurable plasma paliperidone concentrations in the low therapeutic range 886 days (2.5 years) after her last injection, indicating that in some individuals the drug may be released from the depot far longer than the predicted half‑life. The pharmacokinetic profile was originally derived from a 2009 pooled analysis of 18,530 paliperidone concentration samples from 1,795 subjects across six Phase I trials and five Phase II and III trials funded by Johnson & Johnson Pharmaceutical Research and Development, LLC. Invega Sustenna, Invega Trinza, and Invega Hafyera all utilize nanoparticle technology. The NanoCrystal® technology used in all three long-acting paliperidone products is manufactured by Alkermes plc.
==== Corporate developments and acquisitions ==== In September 2020, the company acquired a 9.9% stake in CStone Pharmaceuticals for $200 million (HK$1.55 billion), helping to commercialise its anti-PD-L1 monoclonal antibody, CS1001. In October 2020, the company acquired Arixa Pharmaceuticals. In November 2020, using a Reverse Morris Trust structure, Pfizer merged its off-patent branded and generic drug business, known as Upjohn, with Mylan to form Viatris, owned 57% by Pfizer shareholders. On January 5, 2021, Pfizer introduced a new logo. In April 2021, Pfizer acquired Amplyx Pharmaceuticals and its anti-fungal compound fosmanogepix (APX001). In August, the company announced it would acquire Trillium Therapeutics Inc and its immuno-oncology portfolio for $2.3 billion. In November 2021, gene therapy research was delayed by trial changes. In March 2022, the company acquired Arena Pharmaceuticals for $6.7 billion in cash. In June 2022, the company acquired ReViral Ltd, for up to $525 million, gaining access to experimental drugs used to combat respiratory syncytial virus infections. In October 2022, the company acquired Biohaven Pharma and its calcitonin gene-related peptide programs for $11.6 billion. It also acquired Global Blood Therapeutics for $5.4 billion, boosting Pfizer's rare disease business. In April 2023, Pfizer moved its world headquarters from 42nd Street in Midtown Manhattan to the Spiral at Hudson Yards. In September 2023, CDC Endorsed Pfizer's Maternal RSV Vaccine to Shield Newborns.
=== Bacterial or viral === As bacterial and viral infections can both cause the same kinds of symptoms, it can be difficult to distinguish which is the cause of a specific infection. Distinguishing the two is important, since viral infections cannot be cured by antibiotics whereas bacterial infections can.
Sources: en.wikipedia.org
=== Glycogen storage === During periods of high blood sugar, glucose 6-phosphate from glycolysis is diverted to the glycogen-storing pathway. It is changed to glucose-1-phosphate by phosphoglucomutase and then to UDP-glucose by UTP--glucose-1-phosphate uridylyltransferase. Glycogen synthase adds this UDP-glucose to a glycogen chain.
The 1980 Familia/323 was the first front-engine, front-wheel-drive vehicle from Mazda since the R130. This generation of 323 was Wheels magazine's car of the year for 1980. The existing station wagon version, simply a facelifted version of the previous rear-drive model (fitted with the square headlights and grille from the new model), was sold in parallel with the BD. The wagon was available with either three or five doors and was equipped either with the old 1272 cc TC engine or the 1415 cc UC. The 1.4 was replaced from 1983 with the newly developed 1490 cc E5 engine. The TC 1.3 produces 60 PS (44 kW) while the larger versions offer 70 PS (51 kW). By 1985, the old 1.3 was replaced by the 1296 cc E3 engine with 68 PS (50 kW); it was only available with the three-door station wagon body.
== Business activities == MacKinnon is co-inventor with his friend and scientific collaborator, neurobiologist Bruce Bean of Harvard Medical School, of a dietary supplement for treating and preventing muscle cramps; they tested it in clinical trials and are co-founders a company to commercialize their invention, Flex Pharma. Christoph Westphal and Jennifer Cermak were co-founders as well. The company undertook drug development of a formulation of supplement as a drug candidate for neuromuscular disorders like ALS, and raised a $40 million Series A round. The company had an $86 million initial public offering in 2015. In 2016, the company launched "HotShot" as a dietary supplement for endurance athletes. In June 2018 the company halted clinical development of the drug candidate due to tolerability issues, cut its workforce, and said it was considering its strategy. In July 2018 MacKinnon resigned from the board of directors.
== Randomised controlled trial (RCT) == The AIDA diabetes simulator has been tested out in a pilot randomised controlled trial (RCT). The protocol used for the RCT was described a priori in the medical / diabetes literature. The study sought to assess whether diabetes educational teaching sessions using the AIDA simulator led to better outcomes than similar diabetes educational teaching sessions without a computer. The study was run at the Ospedale di Marino, near Rome, in Italy by an independent diabetologist / endocrinologist – unconnected with the simulator's development. Twenty-four volunteers (12 male and 12 female) with type 1 diabetes of more than 6-years duration, aged 19–48 years, who gave written informed consent, were randomly assigned to one of two study groups, each receiving different teaching interventions. Group A was exposed to the AIDA diabetes simulator, while Group B (the control group) received conventional lessons with slides and transparencies. Six lessons were held for each group (one per week). At the beginning and end of the study all subjects had their glycated hemoglobin (HbA1c) measured. The subjects also carefully documented the incidence of any symptomatic hypoglycaemic episodes ('hypos'), whether mild (sweating, dizziness), moderate (nausea, vomiting), or severe (requiring assistance). The results seem encouraging. HbA1c levels in Group A dropped significantly from 7.2% to 6.4% after lessons with the diabetes simulator (p = 0.01).
Sources: en.wikipedia.org
No. It is a laboratory-made peptide, while the natural hormone is alpha-melanocyte-stimulating hormone, a longer peptide produced by the pituitary gland and by skin cells. Melanotan-2 mimics only a short active region of that hormone and contains non-natural residues such as D-phenylalanine.
No approved regulatory indication exists in major markets. An approval exists for a different peptide, afamelanotide, which is used for a rare photosensitivity disorder called erythropoietic protoporphyria. Melanotan-2 itself remains a research compound with no cleared clinical role.
Melanocortin-1 receptors on melanocytes are the receptor most closely linked to pigment production. The peptide is not selective, however, and also activates melanocortin-3, melanocortin-4, and melanocortin-5 receptors. That lack of selectivity is the usual explanation offered for both its range of observed effects and its off-target effects.
It is a synthetic cyclic heptapeptide analogue of alpha-melanocyte-stimulating hormone, containing seven amino acids with a lactam ring and a D-configured phenylalanine residue. It is supplied as a lyophilised powder for laboratory research.