Everything below concerns PPARδ. We keep the language plain, cite what the science says, and separate well-supported claims from open questions.
Updated 2026-02-26. Numbers and descriptions here follow the published literature rather than marketing material.
Early clinical research explored GW501516 for lipid disorders, obesity, and diabetes. Some short-term human studies reported changes in HDL cholesterol, LDL cholesterol, and triglycerides. The development program was discontinued after rodent studies showed dose-dependent tumor formation in multiple tissues, including liver, bladder, stomach, and skin. These findings raised concerns about long-term cancer risk in humans. Because human exposure data are limited, the clinical significance of the rodent tumors remains uncertain.
Literature on cardarine often separates receptor pharmacology from toxicology. Mechanistic papers describe PPARδ activation and gene expression changes, while safety assessments focus on carcinogenicity and species differences. Questions remain about whether rodent tumors arise through PPARδ-dependent or off-target mechanisms. Another open area is how human metabolism and exposure compare with those in animal studies. Analytical methods such as liquid chromatography–mass spectrometry are used to confirm identity in biological and product samples.
GW501516 acts as an agonist at the peroxisome proliferator-activated receptor delta, a nuclear receptor that regulates gene expression. Activation shifts transcription toward genes involved in fatty acid uptake, oxidation, and energy expenditure. The compound does not bind the androgen receptor and therefore differs from anabolic steroids and SARMs. In rodent models, this metabolic shift has been linked to increased running endurance and reduced fat accumulation. The exact downstream pathways in humans remain incompletely characterized.
Handling and quality assessment of cardarine reference material follow general laboratory practices for poorly characterized compounds. It typically appears as a white to off-white powder and is sparingly soluble in water but soluble in organic solvents such as dimethyl sulfoxide and ethanol. Storage recommendations usually specify a cool, dry, dark place, with long-term storage at low temperature and desiccation. Purity may be checked by high-performance liquid chromatography with ultraviolet detection, while identity is confirmed by mass spectrometry and nuclear magnetic resonance. No pharmacopeial monograph exists, so reported purity and stability depend on the supplier’s methods.
GW501516 acts as a selective agonist at PPARδ, a nuclear receptor that regulates transcription of genes involved in lipid handling and energy metabolism. Activation of PPARδ in preclinical models increases fatty acid oxidation, mitochondrial biogenesis, and exercise endurance in rodents. These effects have made the compound a subject of metabolic research and also a target for sport anti-doping rules. In humans, however, controlled studies are limited, and whether similar endurance or metabolic changes occur at tolerated exposures remains an open question. The receptor’s broad tissue distribution also means downstream effects may vary by organ and condition.
| Property | Value | Notes |
|---|---|---|
| Primary target | PPARδ | Nuclear receptor; not androgen receptor |
| Studied indications | Dyslipidemia; obesity; diabetes | Early clinical research; development discontinued |
| Rodent toxicity | Tumor formation in multiple tissues | Dose-dependent findings in some studies |
| Human approval | None | No approved therapeutic use |
| Typical analytical method | LC-MS/MS | Used for identity and quantification |
Human trials of GW501516 were small and short in duration. They examined lipid levels, glucose handling, and other metabolic markers, but the programs were halted after the animal cancer findings. No approved therapeutic product exists, and published human data are insufficient for establishing long-term safety. Reports of use for athletic performance come mainly from non-clinical settings and cannot be verified through controlled trials. Independent testing of products sold as cardarine has found inconsistent purity and labeling.
Laboratory studies indicate that GW501516 activates PPARδ, a nuclear receptor involved in fatty acid oxidation and energy metabolism. In rodent experiments, treated animals often showed increased endurance and reduced fat mass. These effects were observed under controlled conditions and do not establish safe or effective use in humans. The exact dose-response relationship in humans remains poorly characterized. Species differences in metabolism can affect how results translate across animals and people.
The pharmacological interest in cardarine centers on PPARδ activation and its downstream effects on lipid handling and mitochondrial function. In animal studies, PPARδ agonists have been associated with changes in exercise endurance and fatty acid utilization, though results vary by model and protocol. Human data remain sparse, and the absence of large controlled trials limits conclusions about efficacy. Researchers often describe the compound as a tool for probing PPARδ biology rather than a proven therapeutic agent.
Safety discussions about cardarine frequently cite rodent carcinogenicity findings reported in the 2000s. In those studies, treated animals developed tumors at multiple sites, leading sponsors to discontinue clinical development. The relevance of these findings to humans has not been resolved, but they are a major reason the compound is not approved. Current literature emphasizes uncertainty about long-term effects and the risks of unregulated use. Regulators and health agencies have not established a safe human exposure level.
Cardarine is a synthetic compound also known as GW501516, GW-501516, and sometimes endurobol. It was developed as a selective agonist of peroxisome proliferator-activated receptor delta, a nuclear receptor involved in fatty acid oxidation and energy metabolism. The compound was studied in preclinical models for metabolic and cardiovascular conditions, but it did not become a marketed human medicine. In regulatory and anti-doping contexts, it is treated as a prohibited substance rather than a licensed medicine.
== Uses == It is used as a wood product and in folk medicine. This valuable wood was used in Chinese furniture from the late Ming and early Qing dynasties, and new furniture in the same styles are sought after as luxury and prestige items.
In biology, sulfation is typically effected by sulfotransferases, which catalyze the transfer of the equivalent of sulfur trioxide to substrate alcohols and phenols, converting the latter to sulfate esters. The source of the SO3 group is usually 3'-phosphoadenosine-5'-phosphosulfate (PAPS). When the substrate is an amine, the result is a sulfamate. Sulfation is one of the principal routes for post-translational modification of proteins. Sulfation is involved in a variety of biological processes, including detoxification, hormone regulation, molecular recognition, cell signaling, and viral entry into cells. It is among the reactions in phase II drug metabolism, frequently effective in rendering a xenobiotic less active from a pharmacological and toxicological standpoint, but sometimes playing a role in the activation of xenobiotics (e.g. aromatic amines, methyl-substituted polycyclic aromatic hydrocarbons). Sulfate is part of sulfolipids, such as sulfatides, which constitute 20% of the galactolipids in myelin. Another example of biological sulfation is in the synthesis of sulfonated glycosaminoglycans, such as heparin, heparan sulfate, chondroitin sulfate, and dermatan sulfate. Sulfation is also a possible posttranslational modification of proteins.
==== United Kingdom ==== During the 1980s, 7-Eleven convenience stores were based in London and the South East of England. The first shop opened in Hendon, north London in 1985. In October 1997 all 57 UK 7-Eleven stores were sold to Budgens. The company announced in 2014 they had planned to return to the UK market, but this did not progress beyond its announcement. In 2019, the company announced again it had planned to return, but as of October 2022 no stores had been opened.
Due to its success in livestock operations cryobranding has attracted the attention of humans in pursuit of novel body modifications. It remains a rare practice, with many instances carried out in an amateur setting. Most report pain, edema and sloughing of skin. Branding times vary but most are strongly overbranded, perhaps due a naive assumption that human skin requires the same brand durations as those of cattle and horses. Branding times up to 30 seconds have been recorded, although even 10 seconds have proved sufficient to produce a third degree cryoburn. This instance of a 10-second freeze brand formed the basis of the first medical report on a case of human cryobranding. The case involved a 33-year-old woman who received a large runic cryobrand to her inner forearm. The brand was cooled in a dry ice isopropanol bath for 5 minutes and then applied to her hairless skin for 10 seconds. The woman developed a third degree burn at the center of the imprint and sought medical attention 18 days after being branded. Her wound was treated with the same protocol for thermal burns and closed approximately 8 weeks after branding and 5 weeks after treatment began. At six months the final brand was somewhat hyperpigmented, with a central scar from the open wound. The mild steel branding iron used in this case bore a combination of two vowels from the Elder Futhark alphabet, an ᛁ superimposed on a ᛟ (equivalent to the English vowels i and o). Ranchers strongly advise that a gap be left in a brand face where the pattern has crossing lines.
=== Analogues === Analogues of 4-HO-MET include psilocin (4-HO-DMT), 4-HO-DET (ethocin), 4-HO-MiPT (miprocin), 4-HO-DPT (deprocin), 4-HO-MPT (meprocin), 4-HO-DALT (dalocin), and 4-HO-MALT (malocin), among others. 4-AcO-MET (metacetin) and 4-PrO-MET are ester prodrugs of 4-HO-MET. Other analogues of 4-HO-MET include methylethyltryptamine (MET), 5-HO-MET, and 5-MeO-MET.
Sources: en.wikipedia.org
USA Defence Secretary Donald Rumsfeld told an armed services committee of the Senate on 2004-05-07 that "There are a lot more photographs and videos that exist [...] I looked at them last night and they're hard to believe [...] The pictures I've seen depict conduct, behaviour that is so brutal and so cruel and so inhumane that anyone engaged in it or involved in it would have to be brought to justice." He also said that the abused detainees may be offered compensation. In a scene described as "surreal" by AFP, it was found in mid May, 2004 that US troops were handing out cash to freed prisoners along with a note stating "You have not been mistreated.". A reporter visiting the prison Camp War Horse described the tour:
=== Pharmacokinetics === PSGAG reaches peak blood concentration in 20–40 minutes when injected intramuscularly; 30–40% of it binds to blood proteins. It enters all tissues, reaching cartilage within two hours. When PSGAG reaches the synovial fluid, it is then taken up by the cartilage matrices, with osteoarthritic cartilage showing a stronger preference for taking it up. It reaches its peak levels in the joints at 48 hours, and lasts up to 96 hours, before leaving and being excreted by the kidneys.
== Distinctions and honours == On 8 June 1961, Player was the guest on NBC's The Ford Show, Starring Tennessee Ernie Ford. In a comedy skit, he gives Tennessee Ernie Ford a golf lesson. Received the 1965 BBC Overseas Sports Personality of the Year Award. Received the 1966 Bob Jones Award from the United States Golf Association. Named Honorary Member of the Royal and Ancient Golf Club of St Andrews in 1994. Received Honorary Doctor of Laws Degree from University of St Andrews in 1995. Received Honorary Doctor of Science from the University of Ulster, Northern Ireland in 1997 The WGC-Bridgestone Invitational trophy is named the Gary Player Cup. Named Honorary Member of Carnoustie in 1999 Received Honorary Doctorate in Law, University of Dundee, Scotland in 1999 South African Sportsman of the Century award in 2000 Received the 2003 Laureus Lifetime Achievement Award at the Laureus World Sports Awards in Monte Carlo. Awarded the Order of Ikhamanga (in gold for exceptional achievement) in 2003 by President Mbeki of South Africa for excellence in golf and contribution to non-racial sport in South Africa. He was the world's first golfer to be featured on any country's postal stamp in South Africa. Has designed over 400 golf courses on six continents around the world. He received the 2006 Payne Stewart Award from the PGA Tour.
The hepatocyte is a complex and multifunctional differentiated cell whose cell response will be influenced by the zone in hepatic lobule, because concentrations of oxygen and toxic substances present in the hepatic sinusoids change from periportal zone to centrilobular zone10. The hepatocytes of the intermediate zone have the appropriate morphological and functional features since they have the environment with average concentrations of oxygen and other substances. This specialized cell is capable of:
In genetics, DNase I hypersensitive sites (DHSs) are regions of chromatin that are sensitive to cleavage by the DNase I enzyme. In these specific regions of the genome, chromatin has lost its condensed structure, exposing the DNA and making it accessible. This raises the availability of DNA to degradation by enzymes, such as DNase I. These accessible chromatin zones are functionally related to transcriptional activity, since this remodeled state is necessary for the binding of proteins such as transcription factors. Since the discovery of DHSs 30 years ago, they have been used as markers of regulatory DNA regions. These regions have been shown to map many types of cis-regulatory elements including promoters, enhancers, insulators, silencers and locus control regions. A high-throughput measure of these regions is available through DNase-Seq.
Sources: en.wikipedia.org
It targets PPARδ, a nuclear receptor involved in lipid and energy metabolism. It does not act primarily on androgen receptors. This distinction separates it from SARMs.
Rodent studies found dose-dependent tumors in several organs. The sponsor discontinued the program over cancer concerns. Human risk from long-term use remains unknown.
Controlled human endurance trials are lacking. Animal studies show increased exercise capacity under some conditions. Anecdotal reports are not equivalent to clinical evidence.
Cardarine targets PPARδ, a nuclear receptor involved in lipid and energy metabolism. It does not bind the androgen receptor in the way SARMs do.