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Background And Regulatory History — Field Notes

By Editorial Desk · published 2025-12-07 · last reviewed 2025-12-25 · Info

GW501516 comes up often in conversation and rarely with the context attached. Here we lay out the basics in order, then work through the practical considerations.

Updated 2025-12-25. Numbers and descriptions here follow the published literature rather than marketing material.

Background and Regulatory History

GW501516 acts on PPARδ, a nuclear receptor that helps regulate fatty acid oxidation and energy homeostasis. In animal studies, activation of this receptor was associated with increased endurance and changes in lipid metabolism. Human trials examined effects on blood lipids and other metabolic markers, but the compound did not advance to approval. Rodent studies later reported tumors in multiple tissues at doses used in those experiments. Whether those findings translate to human risk remains uncertain, and the clinical relevance of the animal data is still debated.

Regulatory bodies treat GW501516 as a prohibited substance in competitive sport. The World Anti-Doping Agency added it to the prohibited list, and it falls under classes covering metabolic modulators and hormone-related agents. It is not approved by drug regulators for human use, and it is not a lawful dietary supplement. Products sold under the cardarine name may contain unlisted ingredients or different compounds. Because no approved product exists, quality and identity are not guaranteed by pharmaceutical manufacturing standards.

Background and Regulatory Status

Cardarine is a common name for GW501516, a synthetic compound first described in the 1990s as a selective agonist of the peroxisome proliferator-activated receptor delta. It was studied in preclinical models for metabolic and cardiovascular conditions, but it has not been approved as a medicine in the United States, Europe, or other major jurisdictions. Retail products labeled as cardarine are generally research chemicals or supplements, not pharmaceutical formulations. Because human safety and efficacy data remain limited, regulatory agencies treat it as an unapproved substance rather than a therapeutic product.

Sporting authorities added GW501516 to prohibited lists after it appeared in athlete samples and online markets. The World Anti-Doping Agency classifies it as a hormone and metabolic modulator, and its use can lead to an anti-doping rule violation. Some early laboratory work suggested effects on fatty acid oxidation and endurance-related metabolism in animals, but those findings do not establish safe or effective use in people. Reports of adverse events in humans are scarce and often anecdotal, which complicates risk assessment.

Cardarine at a glance

PropertyValueNotes
Common nameCardarineCommon internet and media name.
Research codeGW501516Also written GW-1516.
Drug classPPARδ agonistNot a selective androgen receptor modulator.
Development statusDiscontinuedClinical development halted after rodent cancer findings.
Regulatory statusProhibited in sportListed by WADA; not approved as medicine.

Notes from published material

The digital signal is transmitted using OFDM with the HDC (High-Definition Coding) proprietary audio compression format. HDC is based on, but not compatible with, the MPEG-4 standard HE-AAC. It uses a modified discrete cosine transform (MDCT) audio data compression algorithm. Digital Radio Mondiale (DRM) is a competing digital terrestrial radio standard developed mainly by broadcasters as a higher spectral efficiency replacement for legacy AM and FM broadcasting. Mondiale means "worldwide" in French and Italian; DRM was developed in 2001, and is currently supported by 23 countries, and adopted by some European and Eastern broadcasters beginning in 2003. The DRM30 mode uses the commercial broadcast bands below 30 MHz, and is intended as a replacement for standard AM broadcast on the longwave, mediumwave, and shortwave bands. The DRM+ mode uses VHF frequencies centered around the FM broadcast band, and is intended as a replacement for FM broadcasting. It is incompatible with existing radio receivers, so it requires listeners to purchase a new DRM receiver. The modulation used is a form of OFDM called COFDM in which, up to 4 carriers are transmitted on a channel formerly occupied by a single AM or FM signal, modulated by quadrature amplitude modulation (QAM). The DRM system is designed to be as compatible as possible with existing AM and FM radio transmitters, so that much of the equipment in existing radio stations can continue in use, augmented with DRM modulation equipment.

primary structure The first order of complexity of structural organization exhibited by a polypeptide or protein molecule, or by a polynucleotide or nucleic acid molecule; i.e. the specific linear sequence of amino acid residues, or of nucleotides, without regard to their spatial arrangement or conformation or any higher-order structure (either secondary, tertiary, or quartenary) the molecule might assume. By convention, the primary structure of a polypeptide is reported from the amino (N)-terminus to the carboxyl (C)-terminus, and the primary structure of a nucleic acid is reported from the 5'-end to the 3'-end.

=== Production of chlorocarbons === Mercury-based catalysis is woven throughout the history of chlorinated ethanes and ethylenes. Vinyl chloride is produced by the addition of HCl to acetylene using a mercury-carbon catalyst. Considerable effort is required to limit the contamination of the product with mercury.

Sources: en.wikipedia.org

Related pages on this site

Background from the literature

Hemoglobin-based oxygen carriers (HBOCs) Palmer's lab identifies new ways to build HBOCs. Their design strategy focus on increasing the molecular diameter of HBOCs so they're unable to traverse across blood vessel walls into the tissue space and limit negative side-effects. Supporting Publications:

The lack of oral activity of DMT is due to rapid metabolism by the enzyme monoamine oxidase A (MAO-A). However, when taken in combination with an irreversible monoamine oxidase inhibitor (MAOI) or a reversible inhibitor of MAO-A (RIMA) such as a harmala alkaloid like harmine or harmaline or a pharmaceutical RIMA like moclobemide, DMT becomes orally active with an extended duration relative to parenteral use of DMT alone. Certain plants like Peganum harmala and the Banisteriopsis caapi used in ayahuasca contain harmala alkaloids which allow DMT to become orally active. When oral DMT is used with an MAOI and the materials are not naturally sourced, the combination is known as pharmahuasca. Changa is a plant-derived form of DMT that is smoked. Smoking and intravenous injection of DMT have extremely intense but very-short-lived effects, whereas intramuscular injection and particularly oral administration with an MAOI have less intense but longer-lasting effects.

Narrated by Jonathan Cullen, produced by Andy Paterson, directed by Patrick Forbes 22 September Fighting the G-Force, it looked at the Brooks Air Force Base in Texas; F-16 aircraft of the United States Air Force Thunderbirds; a G-force simulator on 30 May 1997, where a pilot experiences G-LOC; Major Mark Arlinghaus of the Thunderbirds; Captain Rick Forster, an F-16 instructor; Luke Air Force Base in Arizona, where F-16 pilots were trained; Major Rob Kesterson, an instructor with the 62nd Fighter Squadron; Lt Toby Brallier of the 62nd Fighter Squadron, who blacked out, but he was in a two-seat F-16 trainer; Holloman Air Force Base in New Mexico, where all USAF pilots learn about G-LOC, and are medically tested; Captain John Condojani and G-suits; a G-force centrifuge, rotating once every two seconds; pilots referred to G-LOC as 'doing the funky chicken'; to fly in an A-10, a pilot had to cope with 7.5G, and there were no exceptions; F-16 pilots had to cope with 9G; Captain Rick Fofi, a physical training officer with the USAF; women had been allowed to fly USAF fighter aircraft since 1993; Dr William Albery, chief of USAF aerospace medical research; Colonel James Dooley of flight motion effects at Brooks AFB in Texas, in the Armstrong Laboratory, named after Harry George Armstrong, known for the Armstrong limit; taller pilots were more susceptible to G-LOC; when the German Air Force inherited East German pilots, it discovered that the East German air force believed that G-LOC could be prevented by ruthless selection of pilots and better fitness preparation; Wing Commander Andreas Valentiner of the Luftwaffe Institute of Aviation Medicine; the German Air Force decided to ruthlessly select pilots by G-LOC in a centrifuge as well, before any training commenced - it was the only NATO air force to do this; Dr Brendan Godfrey, director of the Armstrong Laboratory; Captain Kelly Greene of Wright-Patterson Air Force Base in Ohio; Colonel Ron Hill, head of the Crew Systems Directorate; Finley Barfield, chief engineer of the F-16, and what became the Automatic Ground Collision Avoidance System, to avoid controlled flight into terrain (CFIT); Dr Paul Werchan of Brooks AFB; Dr Gene McCall of the United States Air Force Scientific Advisory Board; the Northrop Grumman RQ-4 Global Hawk, planned to first fly in late 1997. Narrated by Piers Gibbon, produced by Simon Berthon, directed by Mark Rubens, made by 3BM Television with The Learning Channel (TLC) 29 September The Iceberg Cometh, about the dangers of icebergs in the Atlantic Ocean; for every metre above surface, four metres are below; the icebergs are made of snow that fell half a million years ago; Greenland is as large as western Europe; icebergs can travel thirty miles a day; the International Ice Patrol was formed in 1914, and now checks half a million square miles; patrols take place three times a week from March to July in the Atlantic Marine Ecozone; glaciologist Peter Wadhams of the University of Cambridge; the North Greenland Ice Core Project (NGRIP) began in 1995. Produced by David Frank, directed by Cathy Rogers, made by RDF Television with the Discovery Channel 13 October Coma, on 4 June 1996 a 32-year-old woman was beaten unconscious in New York Central Park; she was one of four women beaten by 22-year-old John Royster, with the last, 62-year-old Evelyn Alvarez on Park Avenue, not surviving, and Royster was caught from a fingerprint, and was sentenced to life without parole in 1998; neurosurgeon Jamshid Ghajar; the Jamaica Hospital Medical Center, where a nine year old boy, Alex, had been hit by a car, and had severe head trauma, and had a head CT scan; the 'second accident' in the first week in hospital, where the brain swelled, and blocked the flow of blood; a tube was inserted into the brain, to release fluid from swelling, known as a ventriculostomy; the New York Hospital Pediatric ICU, now the Weill Cornell Medical Center; on day two, the eye pupils began to dilate, which can indicate brain swelling, and the intracranial pressure increased, until day three: by day twenty, Alex began to show greater responses, and by day 39, he was walking, and will make a good recovery; neurosurgeon Randall Chesnut, of Oregon, now at the University of Washington School of Medicine; Nicole Ward had a car accident, with a brain injury, but makes a good recovery, thanks to the ventriculostomy procedure; the International Conference on Recent Advances in Neurotraumatology (ICRAN) in early September 1996 at the University of Bologna in Rimini in north-east Italy, where new guidelines of the American Academy of Neurology would be disseminated, from work by the Colorado Medical Society in 1991. A US production, narrated by Piers Gibbon, produced by Paula Apsell, directed by Linda Garmon, made by Nova and WGBH. Shown on Nova on 7 October 1997 20 October Superhighway Robbery, an updated repeat 27 October Sun Storm, about geomagnetic storms, with Nicola Fox of the Heliophysics Science Division; Mike Lockwood (physicist); the March 1989 geomagnetic storm and Hydro-Québec's electricity transmission system; Telesat of Ottawa, and the High Altitude Observatory; a warning system for geomagnetic storms, the Cluster satellite network, was to be launched on 4 June 1996 on board Ariane flight V88, but the launch was a disaster; historical solar records at the Armagh Observatory showed how weather fluctuated with solar activity over the years, John Butler found a connection with Earth temperature; Brian Tinsley looked at electrical charge in clouds causing rain, found by aircraft of the National Center for Atmospheric Research (NCAR); Ernest Hildner of the Space Weather Prediction Center; North American Aerospace Defense Command (NORAD); Daniel N. Baker of the Laboratory for Atmospheric and Space Physics; the Advanced Composition Explorer, launched in August 1997, would detect the magnetic polarity of any solar winds. Narrated by Robin Ellis, directed by Dan Chambers, produced by Robert Eagle, made by Eagle & Eagle 3 November Natural Born Genius?, about inherited intelligence; the population geneticist Robert Plomin, who came to London in 1994; bioethicist Jonathan Glover; psychologist Camilla Benbow of Iowa State University, and the Study of Mathematically Precocious Youth; statistician Charles Spearman was the first to conduct research into general intelligence in 1904, and found that schoolchildren who were good at one academic subject were also good at other subjects and vice versa, and invented the term g factor (psychometrics), although Francis Galton had briefly looked at the subject; psychologist Ian Deary of the University of Edinburgh, where much research on intelligence has been conducted; Alfred Binet of France invented the intelligence test, so that low-scoring children could be given extra help; cognitive psychologist Michael Howe of the University of Exeter believed that the 11-plus exams in England, for grammar school entrance, could possibly label children; much educational testing took place in the US, as the government believed in it, by the Educational Testing Service (ETS); psychologist Stephen J. Ceci disputed reading cast-iron outcomes of individual intelligence tests, but nonetheless believed that general intelligence could be predicted across a population as a whole; Chris Allander of the Army School of Recruiting; Michael Howe conducted environmental education research of parental support, and if that was as much a factor as genetic or innate ability - environmental educational research largely ignored any genetic component, which Robert Plomin dismissed; psychologist Sandra Scarr had conducted much research on adopted children, which largely and conclusively proved the case for genetically inherited intelligence and abilities - and she believed that you could only teach subjects to children of whom had enough capability; Robert Plomin's wife, psychologist Judith Dunn, and varying intelligence of children within individual families; identical twins raised apart had identical IQ scores; psychologist Thalia C. Eley of the Institute of Psychiatry, Psychology and Neuroscience; from Robert Plomin's exhaustive adoption genetic studies, he finds a genetic link. Narrated by Barbara Flynn, produced by Rosalind Arden, directed by David Cresswell, made by John Gau Productions. John Gau had made Triumph of the Nerds the year before 10 November Losing It, about the persistence of sportspeople in the face of adversity; Steve Backley, javelin thrower gained three world records and was European champion in 1990 at the age of 21, but at the 1991 World Championships in Athletics in Tokyo, he didn't get past the qualifying round, where he had to throw 82m but he could only manage 78m; a fortnight later he threw 91m, gaining the British and Commonwealth records; mental strength is often the difference between success and failure; Doug Sanders, the American golfer, missed a straightforward put at the 1970 British Open; Sally Gunnell at the 1992 Olympics; sports psychologist Dave Collins (a former Royal Marine); footballer Lee Chapman who suffered a loss of confidence in 1982; Sally Gunnell, despite feeling intensely nervous before the final on 19 August of the 1993 World Championships in Athletics in Stuttgart, came first and broke the world record; Scottish golfer Sam Torrance and mental preparation for the zone; cricketer Michael Atherton; tennis player Mark Cox; neuroscientist Susan Greenfield, Baroness Greenfield, and alpha waves or alpha rhythm; banishing negative thoughts; Paul Holmes, sports psychologist of the Great Britain Pistol Squad (run by British Shooting since 2007); total mental absorption, denoted by alpha wave brain activity on an ECG, appeared to strongly help success; psychologist David Milner. Narrated by sports commentator Brian Moore, produced by Geoff Deehan, made by Union Pictures 17 November The Day the Earth Was Hit, the Tunguska event on 30 June 1908; David Morrison (astrophysicist) of NASA Ames; Duncan Steel of The Spaceguard Foundation; physicist Edward Teller; Russian mineralogist Leonid Kulik lead the investigation in 1927; the Tunguska explosion had the strength of a 15 megatonne nuclear explosion; astrophysicist Victor Clube and Bill Napier of Armagh Observatory; scientists from Tomsk State University visit Vanavara (rural locality) in the Siberian summer; the 1945 nuclear explosions had similarities in explosive effect to the Tunguska event; Benny Peiser; the Beta Taurids meteor shower; geochemist Evgeny Kolesnikov of Moscow University; tests at Sandia National Laboratories by Mark Boslough; astronomer Eleanor F. Helin of JPL, who worked on the Near-Earth Asteroid Tracking programme. Narrated by Anthony Hyde, produced by Simon Welfare, directed by Stephen White, made by Granite Productions 24 November When Pigs Ruled the World, about the species that survived the extinction event 250 million years ago, to give rise to mammals; Roger Smith of the South African Museum in the Karroo desert; Scottish paleontologist Mike Benton of the University of Bristol; Peter Ward (paleontologist) of the University of Washington; around 1977 a farmer found a strange footprint, made by a therapsid, the ancestor of mammals, in the Guadalupian part of the middle Permian; biologist Colin Tudge, and how large genetic variety was needed for rapid natural selection to occur, to go from sauropsids to synapsids; animatronics technician Neill Gorton would develop a working moving model; the Moschops plant eater, the more dangerous carnivore Anteosaurus, and the slower Lystrosaurus; paleontologists did not know whether therapsids laid eggs, or have birth to live animals; nasal concha bones; the Permian–Triassic extinction event, 252 million years ago, which scientists did not know the direct cause, and had taken place over 100,000 years; Pangaea was formed 350 million years ago; Tony Hallam of the University of Birmingham, and the events in the Triassic; due the extinction event, Lystrosaurus became much greater in number, as its predators had become extinct; small reptiles evolved into the dinosaurs, and Lystrosaurus evolved into rodents; loss of species was being counted on Madagascar; conservationist Joanna Durbin (now of the Climate, Community & Biodiversity Alliance) and the population of Lemur monkeys on Madagascar; Colin Tudge believed that mass extinctions were integral to evolution; Lystrosaurus lasted for ten million years. Narrated by Roger Allam, produced by Joanne Reay, directed by Howard Reay, made by The Mission, with the Discovery Channel 1 December Mindreaders, about autistic traits; Simon Baron Cohen at Cambridge; Temple Grandin in east Colorado; experimental psychologist Alison Gopnik of the University of California, Berkeley; the Sally–Anne test; Helen Tager-Flusberg, and Williams syndrome; Nancy Etcoff of Harvard Medical School; Phineas Gage; neurologist Robert T. Knight of UC Berkeley; Turner syndrome, where females miss the other X chromosome, and have autistic characteristics; David Skuse of the UCL Great Ormond Street Institute of Child Health found that if this X chromosome originated from the mother, the chances of autistic characteristics were much higher; female brains were typically more attuned to faces than male brains; the book An Anthropologist on Mars. Narrated by British actor Bernard Hill, produced by John Wyver, directed by Jeremy Taylor, made by Illuminations Productions. The female actress was Zoe Margolis, later known for Girl with a One-Track Mind 15 December The Conspiracy of Science, about biotechnology companies in Boston (US); David Kent of Genzyme; the Economic Espionage Act of 1996; the murder of Tsunao Saitoh, and his daughter, in May 1996; Steven Rosenberg of the National Cancer Institute; David Blumenthal of Massachusetts General Hospital; a study by Sandoz (now Novartis) into calcium channel blockers, such as felodipine, by Curt Furberg; full disclosure, or lack of any, of known adverse effects remains a greatly controversial subject. Narrated by Neil Pearson, produced by Geoff Deehan, directed by Tim Shawcross, made by Union Pictures with The Learning Channel (TLC) 22 December Moscow, We Have a Problem, about the Mir EO-23 collision in 1997; Mir had a fire on 24 February 1997; Michael Foale travelled to Mir in May 1997 on Atlantis; the father of Michael Foale was an RAF Meteor pilot; Mir had been in orbit since February 1987, 248 miles above the Earth; the shuttle was docked with Mir for five days; cosmonaut Konstantin Feoktistov, designer of Mir; Mir was only meant to last three years; the oxygen that the cosmonauts breathe originates from the crew's urine; on 24 June 1997, due to saving money on a radar system, a manual docking of the Progress resupply vehicle took place, where the Progress vehicle hit a module, side on; NASA never conducted docking without radar, in such a possibly dangerous way; Vladimir Solovyov (cosmonaut), director of the RKA Mission Control Center; cosmonaut Vasily Tsibliyev accidentally disconnected an important power cable; two more cosmonauts arrived to mend the module on 14 August 1997; the two previous cosmonauts returned to Earth; on 15 September 1997, Mir came close to a NASA satellite; the International Space Station would be launched in June 1998, to cost £20bn; Frank L. Culbertson Jr, director from 1995 of the Shuttle–Mir program; Michael Foale returned to Earth on 27 September 1997 after 142 days, on the Atlantis shuttle; cosmonaut Sergei Krikalev. Narrated by Haydn Gwynne, produced by Julian Ware, directed by Patrick Fleming, made by ITN Factual

Sources: en.wikipedia.org

Frequently asked questions

Is cardarine a selective androgen receptor modulator?

No. Cardarine is a PPARδ agonist, while selective androgen receptor modulators act on androgen receptors. The two classes differ in receptor target and downstream effects.

Why did clinical development stop?

Preclinical rodent studies reported cancers, including liver and bladder tumors, at tested doses. The human relevance of those findings is uncertain, but development was discontinued. No approved human product resulted.

Is cardarine approved for medical use?

No. It remains an investigational compound without approved therapeutic labeling. Sports regulators prohibit its use, and health agencies have warned against consuming it.

Is cardarine approved for human use?

No. Major drug regulators have not approved GW501516 for treating any medical condition. Products sold as cardarine are typically unapproved research chemicals or supplements, so their contents and safety are not assured.

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