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Background And Regulatory Status — Deep Dive

By Editorial Desk · published 2025-08-15 · last reviewed 2025-09-01 · Faq

This is a working overview of Investigational drug, written for readers who want more than a one-paragraph summary but less than a textbook.

This page was last updated on 2025-09-01 and is reviewed periodically as new material appears.

Background and Regulatory Status

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.

Legal status varies by country. In some places, cardarine is controlled under medicines or psychoactive substances laws; in others, it may be sold with minimal oversight as a research chemical. Customs agencies have intercepted shipments, and several national health agencies have issued warnings about products marketed for bodybuilding or performance enhancement. The lack of a standardized pharmaceutical supply means identity, purity, and contamination levels can differ widely between samples. These factors make cardarine a regulatory and public health concern rather than a conventional prescription drug.

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.

Background and Regulatory History

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.

Cardarine is a common name for the investigational chemical GW501516, also written GW-1516. It was developed as a peroxisome proliferator-activated receptor delta agonist for metabolic conditions such as dyslipidemia. Early research focused on lipid handling and energy use in skeletal muscle and other tissues. The compound was never approved as a medicine. In public discussion, it is often grouped with performance-enhancing substances, although its receptor target differs from that of anabolic steroids or selective androgen receptor modulators. Regulatory and health authorities have issued warnings about its use.

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.

Cardarine at a glance

PropertyValueNotes
IUPAC name{4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]phenoxy}acetic acidSystematic name for GW501516
CAS Registry Number317318-70-0Unique identifier for the parent compound
Molecular formulaC21H18F3NO3S2Includes carbon, hydrogen, fluorine, nitrogen, oxygen, and sulfur
Molecular weight453.5 g/molApproximate value for the neutral form
AppearanceWhite to off-white powderTypical description for purified laboratory material

Background from the literature

=== Climate === Located in northwestern Italy at the foot of the Alps, Turin features a mid-latitude, four seasons humid subtropical climate (Köppen: Cfa), similar to that of Grenoble, located not far away in the French Alps. Winters are moderately cold and dry; summers are mild in the hills and quite hot in the plains. Rain falls mostly during spring and autumn; during the hottest months, otherwise, rains are less frequent but heavier (thunderstorms are frequent). During the winter and autumn months banks of fog, which are sometimes very thick, form in the plains but rarely on the city because of its location at the end of the Susa Valley. Snowfalls are not uncommon during the winter months, though substantial accumulation is quite uncommon. Its position on the east side of the Alps makes the weather drier than on the west side because of the föhn wind effect. The highest temperature ever recorded was 37.1 °C (98.8 °F) on 11 August 2003, and the lowest was −21.8 °C (−7.2 °F) on 12 February 1956.

A point mutation is a genetic mutation where a single nucleotide base is changed, inserted or deleted from a DNA or RNA sequence of an organism's genome. Point mutations have a variety of effects on the downstream protein product—consequences that are moderately predictable based upon the specifics of the mutation. These consequences can range from no effect (e.g. synonymous mutations) to deleterious effects (e.g. frameshift mutations), with regard to protein production, composition, and function.

The United Nations Security Council responded swiftly to the killing by later imposing an arms embargo against South Africa. After a period of routine harassment against his family by the authorities, as well as fearing for his life, Woods fled the country after being placed under house arrest by the South African Government. Woods later wrote a book in 1978 entitled Biko, exposing police complicity in his death. That book, along with Woods's autobiography Asking For Trouble, both being published in the United Kingdom, became the basis for the film.

=== Temperature === Two issues are involved when considering the temperature of a ligation reaction. First, the optimum temperature for DNA ligase activity which is 37°C, and second, the melting temperature (Tm) of the DNA ends to be ligated. The melting temperature is dependent on length and base composition of the DNA overhang—the greater the number of G and C, the higher the Tm since there are three hydrogen bonds formed between G-C base pair compared to two for A-T base pair—with some contribution from the stacking of the bases between fragments. For the ligation reaction to proceed efficiently, the ends should be stably annealed, and in ligation experiments, the Tm of the DNA ends is generally much lower than 37°C. The optimal temperature for ligating cohesive ends is therefore a compromise between the best temperature for DNA ligase activity and the Tm where the ends can associate. However, different restriction enzymes generates different ends, and the base composition of the ends produced by these enzymes may also differ, the melting temperature and therefore the optimal temperature can vary widely depending on the restriction enzymes used, and the optimum temperature for ligation may be between 4-15°C depending on the ends. Ligations also often involve ligating ends generated from different restriction enzymes in the same reaction mixture, therefore it may not be practical to select optimal temperature for a particular ligation reaction and most protocols simply choose 12-16°C, room temperature, or 4°C.

== Definition == The term secretome was coined by Tjalsma and colleagues in 2004 to denote all the factors secreted by a cell, along with the secretory pathway constituents. In 2010, this definition of secretome was revised to include only proteins secreted into the extracellular space. Related concepts include the matrisome, which is the subset of the secretome that includes extracellular matrix proteins and their associated proteins; the receptome, which includes all membrane receptors, and the adhesome, which includes all proteins involved in cell adhesion.

Sources: en.wikipedia.org

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Reference notes

=== Awards === Half-Life: Alyx won "Game of the Year" at the 2020 VR Awards. At the Game Awards 2020, it was nominated for "Best Game Direction", "Best Audio Design" and "Best Action", and won for "Best VR/AR". At the 17th British Academy Games Awards, it was nominated for "Best Game", "Game Direction", "Audio Achievement" and "Artistic Achievement". At the 24th Annual D.I.C.E. Awards, it was nominated for "Action Game of the Year", "Outstanding Achievement in Game Direction", and "Outstanding Achievement in Game Design", and won for "Immersive Reality Technical Achievement" and "Immersive Reality Game of the Year".

==== Bile ==== Bile produced by the liver is made up of water (97%), bile salts, mucus and pigments, 1% fats and inorganic salts. Bilirubin is its major pigment. Bile acts partly as a surfactant which lowers the surface tension between either two liquids or a solid and a liquid and helps to emulsify the fats in the chyme. Food fat is dispersed by the action of bile into smaller units called micelles. The breaking down into micelles creates a much larger surface area for the pancreatic enzyme, lipase to work on. Lipase digests the triglycerides which are broken down into two fatty acids and a monoglyceride. These are then absorbed by villi on the intestinal wall. If fats are not absorbed in this way in the small intestine problems can arise later in the large intestine which is not equipped to absorb fats. Bile also helps in the absorption of vitamin K from the diet. Bile is collected and delivered through the common hepatic duct. This duct joins with the cystic duct to connect in a common bile duct with the gallbladder. Bile is stored in the gallbladder for release when food is discharged into the duodenum and also after a few hours.

At 11:07, radar detected another, larger attack. This second wave consisted of 107 aircraft. They were met while still 60 miles (97 km) out, and at least 70 of these aircraft were shot down before reaching the ships. Six attacked Rear Admiral Alfred E. Montgomery's group, nearly hitting two of the carriers and causing casualties on each. Four of the six were shot down. A small group of torpedo aircraft attacked Enterprise, with one torpedo exploding in the wake of the ship. Three other torpedo aircraft attacked the light carrier Princeton and were shot down. In all, 97 of the 107 attacking aircraft were destroyed. A third raid, consisting of 47 aircraft, came in from the north. It was intercepted by 40 fighters at 13:00, while 50 miles (80 km) out from the task force. Seven Japanese aircraft were shot down. A few broke through and made an ineffective attack on Task Group 58.4. Many others did not press home their attacks. This raid therefore suffered less than the others, and 40 of its aircraft managed to return to their carriers. A fourth Japanese raid was launched between 11:00 and 11:30, but pilots had been given an incorrect position for the U.S. fleet and could not locate it. They broke into two loose groups and turned for Guam and Rota to refuel. One group flying toward Rota stumbled upon Montgomery's task group. Eighteen aircraft joined battle with American fighters and lost half their number. A smaller group of nine Japanese dive bombers of this force evaded U.S. aircraft and attacked Wasp and Bunker Hill but scored no hits; eight were shot down.

The hypothesis assumed that functional OR genes can be correlated to the olfactory capability of a given animal. In this view, a decrease in the fraction of functional OR genes would cause a reduction in the sense of smell; species with higher pseudogene count would also have a decreased olfactory ability. This assumption is flawed. Dogs, which are reputed to have good sense of smell, do not have the largest number of functional OR genes. Additionally, pseudogenes may be functional; 67% of human OR pseudogenes are expressed in the main olfactory epithelium, where they possibly have regulatory roles in gene expression. More importantly, the vision priority hypothesis assumed a drastic loss of functional OR genes at the branch of the OWMs, but this conclusion was based by low-resolution data from only 100 OR genes. High-resolution studies instead agree that primates have lost OR genes in every branch from the MRCA to humans, indicating that the degeneration of OR gene repertories in primates cannot simply be explained by the changing capabilities in vision. It has been shown that negative selection is still relaxed in modern human olfactory receptors, suggesting that no plateau of minimal function has yet been reached in modern humans and therefore the olfactory capability might still be decreasing. This is considered to provide a first clue to the future human genetic evolution.

Sources: en.wikipedia.org

Frequently asked questions

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.

Why is cardarine banned in sport?

It is prohibited by the World Anti-Doping Agency as a hormone and metabolic modulator. Athletes who test positive for GW501516 can face sanctions, including suspensions and loss of results.

What is the difference between cardarine and GW501516?

Cardarine is a common or trade-style name, while GW501516 is the research code for the same chemical entity. Some sources also use Endurobol or GSK-516. The names refer to the same compound, not distinct drugs.

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.

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