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Background And Regulatory Status — Quick Reference

By Editorial Desk · published 2025-12-20 · last reviewed 2026-01-08 · News

Everything below concerns Prohibited substance. We keep the language plain, cite what the science says, and separate well-supported claims from open questions.

Last reviewed on 2026-01-08. Where a claim depends on a specific study, the study is described rather than over-claimed.

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.

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.

Regulatory Status and Detection Context

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.

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 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 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.

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Identity and Pharmacological Mechanism

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.

The compound is typically described as a laboratory compound rather than a therapeutic product. Published reports have explored its role in lipid disorders, insulin sensitivity, and exercise metabolism, yet no major drug regulator has approved it for medical use. Commercial samples sold under the cardarine name may vary in purity and identity. Analytical confirmation is therefore necessary when the material is discussed in scientific or regulatory contexts. Its classification as a prohibited substance in sport further shapes how it is studied and reported.

Supporting material

== Further reading == Valera, Maria José; Torija, Maria Jesús; Mas, Albert; Mateo, Estibaliz (2013). "Acetobacter malorum and Acetobacter cerevisiae identification and quantification by Real-Time PCR with TaqMan-MGB probes". Food Microbiology. 36 (1): 30–39. doi:10.1016/j.fm.2013.03.008. ISSN 0740-0020. PMID 23764217. Sagarzazu, Noelia Isabel, et al. "Optimization of denaturing high performance liquid chromatography technique for rapid detection and identification of acetic acid bacteria of interest in vinegar production." Acetic Acid Bacteria 2.1s (2013): e5. Ogawa S, Tachimoto H, Kaga T (January 2010). "Elevation of ceramide in Acetobacter malorum S24 by low pH stress and high temperature stress". Journal of Bioscience and Bioengineering. 109 (1): 32–6. doi:10.1016/j.jbiosc.2009.07.007. PMID 20129078.

== Botany == The genus is composed of mostly vigorous, woody, climbing vines / lianas. The woody stems are quite fragile until several years old. Leaves are opposite and divided into leaflets and leafstalks that twist and curl around supporting structures to anchor the plant as it climbs. Some species are shrubby, while others, like C. recta, are herbaceous perennial plants. The cool temperate species are deciduous, but many of the warmer climate species are evergreen. They grow best in cool, moist, well-drained soil in full sun. Clematis species are mainly found throughout the temperate regions of the Northern Hemisphere, rarely in the tropics. Clematis leaves are food for the caterpillars of some Lepidoptera species, including the willow beauty (Peribatodes rhomboidaria). The timing and location of flowers varies; spring-blooming clematis flower on side shoots of the previous year's stems, summer/fall blooming clematis bloom only on the ends of new stems, and twice-flowering clematis do both.

== Use == While originally invented as a tool to help university librarians to decide which journals to purchase, the impact factor soon became used as a measure for judging academic success. This use of impact factors was summarised by Hoeffel in 1998:

=== Sublingual administration === Estradiol tablets can be taken sublingually instead of orally. Non-micronized estradiol tablets in doses of 0.125, 0.25, and 1 mg were previously marketed for use by sublingual administration under brand names such as Diogynets, Estradiol Membrettes, and Dimenformon in the 1950s. Non-micronized estradiol has poor water solubility, but micronized estradiol is rapidly absorbed by the sublingual route. All oral estradiol tablets are micronized, as this improves the efficiency of estradiol absorption in the gastrointestinal tract. Likewise, all oral estradiol valerate tablets seem to be micronized. The sublingual route is, in actuality, probably a combination of sublingual and oral delivery of estradiol due to incidental swallowing of some of the estradiol. The absorption of sublingual estradiol can be attributed to the rich vascularization under the tongue. With administration of an oral estradiol tablet sublingually, complete dissolution of the tablet occurs within a few minutes and circulating levels of estradiol begin to rise within 5 minutes. Maximal levels of estradiol occur after 30 to 60 minutes of administration. After this, estradiol levels drop steeply within 4 hours, and this is followed by a more gradual decline in levels of estradiol and a return to baseline concentrations by 24 hours. The rapid rise and steep fall of estradiol levels with sublingual administration of estradiol is analogous to the case of intravenous injection and intranasal administration of the hormone.

Sources: en.wikipedia.org

Notes from published material

The lowering of the blood cholesterol level can reduce the risk of coronary heart disease." β-glucan lowers cholesterol in part by increasing the viscosity of digesta in the small intestine, although cholesterol reduction is greater in those with higher total cholesterol and LDL cholesterol in their blood. Additionally, studies suggest that it increases the activity of CYP7A1, a key enzyme in the synthesis of bile acids, thus increasing the excretion of cholesterol, and that it may have additional anti-atherogenic mechanisms. The degree of cholesterol reduction depends upon the particular strain of β-glucan in a range between a molecular weights of 26.8 and 3000 kD. Although more viscous β-glucans result in a more viscous solution of intestinal digesta, and thus more cholesterol uptake, after a certain molecular weight, β-glucans become less soluble and thus contribute less to solution viscosity. The intake of β-glucan in liquid form generally results in greater solubilization and oat β-glucan is more effective at lowering cholesterol in juices than in hard foods like bread and cookies. Despite the recognized impact of viscosity on serum cholesterol levels, no current data exists comparing internal solution viscosity and serum cholesterol. Intake of oat β-glucan at daily amounts of at least 3 grams lowers total and low-density lipoprotein cholesterol levels by 5–10% in people with normal or elevated blood cholesterol levels.

=== Observed markers of dedifferentiation === For dedifferentiation, genes in the extracellular matrix play an important role. For example, MMP, the matrix metalloproteinase, has shown up-regulated activity during early stages of limb regeneration. Matrix Metalloproteinases are responsible for degradation of both non-matrix and matrix proteins. MMP degrades proteins in the extracellular matrix of a cell, resulting in the destabilization of the differentiated cell identity. However, the markers selected to represent dedifferentiation can differ according to the tissue and cell types that are being studied. For example, in mice myotubes, dedifferentiation is marked by a decreased expression of Myogenin, a protein present in differentiated myotubes.

Crystallized honey occurs when some of the glucose content has spontaneously crystallized from solution as the monohydrate. It is also called "granulated honey" or "candied honey". Honey that has crystallized (or is commercially purchased crystallized) can be returned to a liquid state by warming. Despite a common misconception, honey crystallizing does not mean it has expired. Pasteurized honey has been heated in a pasteurization process which requires temperatures of 72 °C (161 °F) or higher. Pasteurization destroys yeast cells. It also liquefies any microcrystals in the honey, which delays the onset of visible crystallization. However, excessive heat exposure also results in product deterioration, as it increases the level of hydroxymethylfurfural (HMF) and reduces enzyme (e.g. diastase) activity. Heat also darkens the honey, and affects taste and fragrance. Raw honey is as it exists in the beehive or as obtained by extraction, settling, or straining, without adding heat (although some honey that has been "minimally processed" is often labeled as raw honey). Raw honey contains some pollen and may contain small particles of wax. Strained honey has been passed through a mesh material to remove particulate material (pieces of wax, propolis, other defects) without removing pollen, minerals, or enzymes. Filtered honey of any type has been filtered to the extent that all or most of the fine particles, pollen grains, air bubbles, or other materials normally found in suspension, have been removed.

=== Qigong === Qigong and Chinese medicine place huge emphasis on a form of energy called 精 (pinyin: jīng, also a morpheme denoting "essence" or "spirit") – which one attempts to develop and accumulate. "Jing" is sexual energy and is considered to dissipate with ejaculation, so masturbation is considered "energy suicide" amongst those who practice this art. According to Qigong theory, energy from many pathways/meridians becomes diverted and transfers itself to the sexual organs during sexual excitement. The ensuing orgasm and ejaculation will then finally expel the energy from the system completely. The Chinese proverb 一滴精,十滴血 (pinyin: yì dī jīng, shí dī xuè, literally: a drop of semen is equal to ten drops of blood) illustrates this point. The scientific term for semen in Chinese is 精液 (pinyin: jīng yè, literally: fluid of essence/jing) and the term for sperm is 精子 (pinyin: jīng zǐ, literally: basic element of essence/jing), two modern terms with classical referents.

Acoustic and seismic metamaterials are also research areas. Metamaterial research is interdisciplinary and involves such fields as electrical engineering, electromagnetics, classical optics, solid state physics, microwave and antenna engineering, optoelectronics, material sciences, nanoscience and semiconductor engineering. Recent developments also suggest potential applications of metamaterials in optical computing, with metamaterial-based systems theoretically being able to perform certain tasks more efficiently than conventional computing.

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 approved for any medical use?

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

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