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Regulatory Status And Detection Context — Reference Sheet

By Editorial Desk · published 2025-11-04 · last reviewed 2025-11-21 · Data

The short version of research chemical fits in a sentence. The long version — which is the one that helps — is below.

This page was last updated on 2025-11-21 and is reviewed periodically as new material appears.

Regulatory Status and Detection Context

A persistent misconception is that cardarine is a fat-burning drug or a safe alternative to anabolic steroids. No approved therapeutic product exists, and human safety data are limited. The tumor findings in rodents remain a central concern in scientific reviews. Products sold online may contain inaccurate labels, impurities, or different compounds entirely, which complicates any assessment of effects. Independent testing of such products has reported frequent mislabeling. For these reasons, discussions in the literature emphasize risks and unknowns rather than benefits.

Cardarine is not approved for human therapeutic use in any major jurisdiction. It appears on the World Anti-Doping Agency Prohibited List as a PPARδ agonist within the hormone and metabolic modulators category. Sports organizations test for it because it has been detected in athlete samples and seized products. Regulatory actions against marketed research chemical versions have occurred in several countries, though enforcement varies. Availability through unregulated channels complicates oversight.

Analytical laboratories typically identify cardarine and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is a common matrix in anti-doping testing, while blood and tissue may be used in research settings. Detection windows depend on the assay, the sample matrix, and the compound's metabolism. Because cardarine is extensively metabolized, laboratories often target specific metabolites to improve sensitivity and confirmation. Reference standards are required for reliable quantification. Method validation includes checks for selectivity, linearity, and carryover.

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.

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.

Cardarine at a glance

PropertyValueNotes
Regulatory statusNot approved for human therapeutic useNo marketing authorization identified in major jurisdictions.
Anti-doping classPPARδ agonist; hormone and metabolic modulatorsListed on the WADA Prohibited List.
Common test matrixUrineAlso blood and tissue in research settings.
Typical analytical methodLC-MS/MSTargets parent compound and metabolites.
Major safety signalTumor findings in rodentsHuman relevance not established; limited human data.

Identity and Pharmacological Mechanism

Cardarine is a common name for GW501516, a synthetic compound studied for its effects on lipid and glucose metabolism. It functions as an agonist at peroxisome proliferator-activated receptor delta, or PPARδ, a nuclear receptor that influences gene expression. The molecule is not a steroid, nor is it a selective androgen receptor modulator. It is also known in research and sports literature as GW-501516 and endurobol. Early laboratory work examined its metabolic activity in cell cultures and animal models.

Activation of PPARδ changes transcription of genes involved in fatty acid transport, mitochondrial function, and skeletal muscle fuel preference. In rodent studies, pharmacological PPARδ activation was associated with increased endurance and altered body composition. These findings generated interest in performance enhancement, but species differences and study designs limit direct extrapolation to humans. Small human trials were conducted in the 2000s and later discontinued. The extent to which cardarine produces similar metabolic or performance effects in people remains an open question.

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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.

Supporting material

In 2016, Burger King signed a build-to-suit lease agreement on a new 150,000 square feet (14,000 m2) five-story headquarters building to be built at 5707 Blue Lagoon Drive, just down the street from its existing nine-story headquarters at 5505 Blue Lagoon Drive. This was slightly smaller than the 200,000 square feet (19,000 m2) it was leasing in its current headquarters building at the time. In 2018, Burger King moved into its new headquarters at 5707 Blue Lagoon Drive. As of August 2024, the Burger King system operates more than 18,700 locations in more than 100 countries and U.S. territories.

A leiomyosarcoma (LMS) is a rare malignant (cancerous) smooth muscle tumor. The word is from leio- 'smooth', myo- 'muscle' and sarcoma 'tumor of connective tissue'. The stomach, bladder, uterus, blood vessels, and intestines are examples of hollow organs made up of smooth muscles where LMS can be located; however, the uterus and abdomen are the most common sites. Although leiomyosarcomas are rare, they belong to the more common types of soft-tissue sarcoma, representing 10–20% of new cases. This type of cancer is more frequently diagnosed in adults as compared to children. When considering LMS specifically in the context of the uterus, it affects approximately 6 individuals per 1 million people in the United States each year. LMSs are resistant cancers, meaning they are generally not very responsive to chemotherapy or radiation. The best outcomes occur when the tumor tissue can be removed surgically at an early stage, while it is small and has not yet spread from the original site (it remains in situ).

=== Spectroscopy === In chemistry, spectroscopy is used to analyze products of reactions. To understand if dexamethasone is synthesized from a reaction, spectroscopy must be taken and compared to the literature spectrum. There are multiple spectroscopy analyses that can be taken including 1H NMR, 13C NMR, IR, Mass spectrometry, and UV/vis spectroscopy. Using IR spectroscopy, the peaks show the functional groups found in the molecule. Peaks at 3472, 1662, and 1618 represent alcohol, aldehyde, and alkene functional groups. UV-vis spectroscopy is another way to analyze a product to figure out what it is. Finally, mass spectroscopy showed peaks at: 393.1, 355.2 147.1 m/z. The peak at 393.1 m/z is the peak for dexamethasone as its molecular weight is 392.46 m/z.

Charles Miller Metzner (1931), judge on the United States District Court for the Southern District of New York and the Temporary Emergency Court of Appeals Lawrence E. Walsh (1932), independent counsel in the Iran-Contra affair; 4th United States Deputy Attorney General William Golub (1934), lawyer and advisor to Governor Nelson Rockefeller Harold Leventhal (1934), judge on the United States Court of Appeals for the District of Columbia Circuit John Slate (1935), lawyer and name partner of Skadden Arps Slate Meagher & Flom Daniel Mortimer Friedman (1937), judge of the United States Court of Appeals for the Federal Circuit, last chief judge of the United States Court of Claims, and acting solicitor general of the United States Wilfred Feinberg (1940), judge of the United States Court of Appeals for the Second Circuit Hugh H. Bownes (1941), judge of the United States Court of Appeals for the First Circuit Richard Kuh (1941), New York County district attorney and prosecutor of Lenny Bruce for obscenity Leonard I. Garth (1942), senior judge on the United States Court of Appeals for the Third Circuit Charles L. Brieant (1944), judge of the United States District Court for the Southern District of New York Jack Greenberg (1945), civil rights lawyer who argued the Brown v. Board of Education case before the United States Supreme Court Roy Cohn (1946), attorney and counsel to Sen. Joseph McCarthy Arthur Lazarus Jr. (1947), American Indian rights lawyer, argued United States v.

Sources: en.wikipedia.org

Supporting material

Fluorescent techniques have been used to assess a number of protein dynamics including protein tracking, conformational changes, protein–protein interactions, protein synthesis and turnover, and enzyme activity, among others. Three general approaches for measuring protein net redistribution and diffusion are single-particle tracking, correlation spectroscopy and photomarking methods. In single-particle tracking, the individual molecule must be both bright and sparse enough to be tracked from one video to the other. Correlation spectroscopy analyzes the intensity fluctuations resulting from migration of fluorescent objects into and out of a small volume at the focus of a laser. In photomarking, a fluorescent protein can be dequenched in a subcellular area with the use of intense local illumination and the fate of the marked molecule can be imaged directly. Michalet and coworkers used quantum dots for single-particle tracking using biotin-quantum dots in HeLa cells. One of the best ways to detect conformational changes in proteins is to label the protein of interest with two fluorophores within close proximity. FRET will respond to internal conformational changes result from reorientation of one fluorophore with respect to the other. One can also use fluorescence to visualize enzyme activity, typically by using a quenched activity-based proteomics (qABP). Covalent binding of a qABP to the active site of the targeted enzyme will provide direct evidence concerning if the enzyme is responsible for the signal upon release of the quencher and regain of fluorescence.

=== Europe === Following discussions on the safety of certain pharmaceutical products derived from kava and sold in Germany, the EU imposed a temporary ban on imports of kava-based pharmaceutical products in 2002. The sale of kava plant became regulated in Switzerland, France, and in prepared form in the Netherlands. Some Pacific island states, which had been benefiting from the export of kava to the pharmaceutical companies, have attempted to overturn the EU ban on kava-based pharmaceutical products by invoking international trade agreements: Fiji, Samoa, Tonga, and Vanuatu argued at the WTO that the ban was imposed with insufficient evidence. The pressure prompted Germany to reconsider the evidence base for banning kava-based pharmaceutical products. On 10 June 2014, the German Administrative Court overturned the 2002 ban, making selling kava as a medicine legal, albeit strictly regulated; personal possession of kava has never been illegal. In Germany, kava-based pharmaceutical preparations are currently prescription drugs. Furthermore, patient and professional information brochures have been redesigned to warn about potential side effects. These strict measures have been opposed by some of the leading kava scientists. In early 2016, a court case was filed against the Bundesinstitut für Arzneimittel und Medizinprodukte (BfArM/German Federal Institute for Drugs and Medical Devices), arguing that the new regulatory regime is too strict and not justified.

== January 14, 1982 (Thursday) == An Ethiopian Air Force Antonov An-26 crashed near Addis Ababa, Ethiopia while transporting a group of Ethiopian, Libyan and Cuban soldiers to a fight in Eritrea. All 73 occupants on board were killed. It the state of Hidalgo in Mexico, near the town of Atotonilco de Tula, the bodies of 13 men were found by a drainage canal. The dead men would be found to have been from Colombia, who had been arrested, as well as a Mexican taxicab driver who had helped transport them to the scene of the deaths. Mexico City Police Chief Arturo Durazo Moreno, accused by a subordinate of having planned the killings, would end up fleeing Mexico after the inauguration of a new president. Robert Dale Henderson began a spree of mostly random murders that would kill 12 people across five U.S. states, in a little more than three weeks until his arrest on February 6, starting with a beautician in Cincinnati. One week later, on January 21, he murdered a family of three in Cherry Fork, Ohio, followed by the January 24 killing of a receptionist in Charleston, South Carolina, the January 25 homicides of a doctor and a clerk in Palatka, Florida and a mother and daughter later in the day in Valdosta, Georgia. He killed a nightclub owner in Port Allen, Louisiana on January 29, and three hitchhikers in Hernando County, Florida on February 4, before approaching a deputy sheriff at a shopping center in Punta Gorda, Florida, making a confession, and surrendering.

Sources: en.wikipedia.org

Supporting material

=== Notes === "Inglorious Bastards" features uncredited vocals from DJ Clue. "M.T.B.T.T.F." stands for "Mike Tyson Blow to the Face". Due to sample clearance issues with "So Be It", a "Pt. II" remix with a different instrumental was uploaded onto streaming platforms in its place upon the album's release. A few hours later, the issue would be resolved, with the original track being reinstated. The initial Kaws and Verdy physical versions of the album did not include either version of "So Be It" or Tyler, the Creator's appearance on "P.O.V.".

Seven genes encode seven distinct 14-3-3 proteins in most mammals (See Human genes below) and 13–15 genes in many higher plants, though typically in fungi they are present only in pairs. Protists have at least one. Eukaryotes can tolerate the loss of a single 14-3-3 gene if multiple genes are expressed, but deletion of all 14-3-3s (as experimentally determined in yeast) results in death. 14-3-3 proteins are structurally similar to the Tetratrico Peptide Repeat (TPR) superfamily, which generally have 9 or 10 alpha helices, and usually form homo- and/or hetero-dimer interactions along their amino-termini helices. These proteins contain a number of known common modification domains, including regions for divalent cation interaction, phosphorylation & acetylation, and proteolytic cleavage, among others established and predicted. 14-3-3 binds to peptides. There are common recognition motifs for 14-3-3 proteins that contain a phosphorylated serine or threonine residue, although binding to non-phosphorylated ligands has also been reported. This interaction occurs along a so-called binding groove or cleft that is amphipathic in nature. To date, the crystal structures of six classes of these proteins have been resolved and deposited in the public domain.

In evolutionary biology, sequence space is a way of representing all possible sequences (for a protein, gene or genome). The sequence space has one dimension per amino acid or nucleotide in the sequence leading to highly dimensional spaces. Most sequences in sequence space have no function, leaving relatively small regions that are populated by naturally occurring genes. Each protein sequence is adjacent to all other sequences that can be reached through a single mutation. It has been estimated that the whole functional protein sequence space has been explored by life on the Earth. Evolution by natural selection can be visualised as the process of sampling nearby sequences in sequence space and moving to any with improved fitness over the current one.

=== Early misidentifications === Many early researchers, both before and after the periodic table was published, were eager to be the first to discover and name the missing element. Its location in the table suggested that it should be easier to find than other undiscovered elements. This turned out not to be the case, due to technetium's radioactivity.

Sources: en.wikipedia.org

Frequently asked questions

Is cardarine approved for any medical use?

No. Cardarine has not received approval for human therapeutic use in major jurisdictions. It remains an investigational compound.

Why is cardarine prohibited in sport?

It is classified as a PPARδ agonist on the WADA Prohibited List. Anti-doping laboratories can detect it and its metabolites in urine. Its use is banned in competition and usually out of competition.

What is known about cardarine and cancer?

Rodent studies reported increased tumor incidence at multiple sites. The human relevance remains uncertain, but the findings contributed to discontinuation of development. No long-term human cancer data are available.

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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