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Background And Regulatory Status — Complete Guide

By Editorial Desk · published 2026-05-12 · last reviewed 2026-05-31 · Info

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

Updated 2026-05-31. Numbers and descriptions here follow the published literature rather than marketing material.

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.

Mechanism and Detection Methods

Detection of GW501516 in biological samples generally relies on liquid chromatography coupled with tandem mass spectrometry. Urine is a common matrix in anti-doping analysis, while blood or plasma may be used in research settings. Sample preparation can involve enzymatic hydrolysis, protein precipitation, or solid-phase extraction before instrumental analysis. Because the compound undergoes metabolism, assays may target the parent molecule, one or more metabolites, or both. Detection windows are not fixed; they depend on factors such as dose, route, individual metabolism, and assay sensitivity. Reference standards are required for accurate identification and quantification.

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.

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

Mechanism and Laboratory Detection

Laboratory handling focuses on identity, purity, and stability. Reference standards are typically stored cold and dry, protected from light, because solutions can degrade over time. Analytical checks may use high-performance liquid chromatography with ultraviolet detection or mass spectrometry. Impurities and related substances can be separated chromatographically and compared with a known standard. Because cardarine is not an approved drug, compendial monographs are absent, and laboratories often rely on in-house methods. Reported purity varies among unregulated products and should not be assumed from a label.

GW501516 binds and activates PPARδ, a nuclear receptor that influences transcription of genes involved in fatty acid oxidation and energy use. Activation shifts some metabolic pathways in preclinical models, which is why the compound has been studied for lipid disorders and exercise-related endpoints. The exact downstream effects in humans are incompletely mapped. PPARδ is expressed in many tissues, including skeletal muscle, liver, and adipose tissue, so broad activation may have varied consequences. Researchers continue to examine how selective or partial activation might alter the balance between benefits and risks.

Published human data are sparse and mostly come from early-phase trials. Those studies examined short-term changes in lipids, glucose, and exercise capacity, but they were not large enough to establish efficacy or long-term safety. Some animal experiments reported increased running endurance, yet such findings do not prove a performance benefit in people. Anti-doping laboratories detect GW501516 and its metabolites in urine or blood using liquid chromatography-tandem mass spectrometry. Detection windows depend on dose, sample type, and individual metabolism. The method is sensitive enough to identify trace residues in tested samples.

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Background and Research Context

PPARδ is a nuclear receptor that regulates gene expression related to fatty acid oxidation, glucose homeostasis, and mitochondrial function. GW501516 binds to this receptor with high affinity and activates downstream signaling in skeletal muscle and other tissues. Animal studies reported increased endurance and altered fuel preference, but human data remain limited and inconsistent. The precise relationship between receptor activation and observed physiological changes is still an area of active investigation. Researchers have also examined whether the compound affects inflammation or cell proliferation. No approved therapeutic indication exists for cardarine.

In laboratory settings, cardarine is studied as a tool compound for probing PPARδ biology. Published experiments often use cell cultures, rodent models, or isolated tissues. Some investigations focus on metabolic effects, while others assess potential risks such as carcinogenicity observed in long-term animal studies. Because human trials are sparse, most knowledge comes from preclinical work and adverse event reports. Scientific literature frequently notes the gap between animal findings and human outcomes. The compound is not a dietary supplement and is not intended for human consumption.

Mechanism and Detection

GW501516 acts as a ligand for PPAR delta, a nuclear receptor that regulates transcription of genes involved in fatty acid oxidation and energy use. Activation of this receptor in skeletal muscle shifts metabolism toward fat burning in animal models. The compound does not burn fat directly; it changes gene expression over hours to days. Researchers study it to understand metabolic flexibility and exercise adaptation. Effects observed in rodents are not automatically expected in humans.

Preclinical research reported that GW501516 increased running endurance in mice and improved lipid profiles in some animal species. Early human trials explored effects on high-density lipoprotein cholesterol, triglycerides, and glucose handling, but the program was discontinued. Published human data are sparse and do not establish efficacy for any condition. Studies also examined PPAR delta in cancer biology, with conflicting findings across models. The relationship between receptor activation, tissue context, and disease risk remains an active area of investigation.

Background from the literature

== History == This cone was described by Sir Geoffrey Ingram Taylor in 1964 before electrospray was "discovered". This work followed on the work of Zeleny who photographed a cone-jet of glycerine in a strong electric field and the work of several others: Wilson and Taylor (1925), Nolan (1926) and Macky (1931). Taylor was primarily interested in the behavior of water droplets in strong electric fields, such as in thunderstorms.

Williams contributed to understanding of the distribution of the chemical elements in living organisms and in collaborationwith João J. R. Fraústo da Silva he wrote three books in this area, as well as a book with Rosalind Rickaby on geological aspects of life. Williams retired in 1991 and devoted much of his retirement to the writing of the books mentioned.

=== Immigration === Pritzker supports Syrian refugees, and criticized the first Trump administration and Rauner for "turning a blind eye on them". He also supports enhancing funding for immigrant and refugee services, increasing health care options for undocumented immigrants, improving the U-Visa certification process for victims of violent crimes, and providing access to financial aid for undocumented students such as DACA recipients. He has said he would sign the "Illinois Trust Act", a pro-immigration bill. In January 2025, when asked about the mass deportation of illegal immigrants in the second presidency of Donald Trump, Pritzker spoke in favor of deporting convicted criminals who are undocumented, but criticized the targeting of "law-abiding residents" who are integrated into communities.

== See also == List of commanders of 82nd Airborne Division (United States) 82nd Airborne Division War Memorial Museum United States military beret flash Geneviève Duboscq Medal of Honor: Airborne Monica Lin Brown World War II combat jump airfields: RAF Balderton RAF Barkston Heath RAF Chalgrove RAF Cottesmore RAF Folkingham RAF Merryfield RAF Membury RAF North Witham RAF Ramsbury RAF Saltby RAF Spanhoe International:

Sources: en.wikipedia.org

Further detail

THC is widely used as a recreational drug, both by itself or with other cannabinoids like cannabidiol (CBD) or in the form of cannabis. It is the main psychoactive constituent in cannabis. The effects of THC include euphoria, appetite stimulation, sedation, cognitive and memory impairment, pain relief, anxiety, and reduced body temperature. THC can produce strong hallucinogenic effects, mystical experiences, and psychosis-like reactions at high doses in a subset of individuals. These hallucinogenic effects are distinct from but potentially just as strong as or even stronger than those of other hallucinogens like serotonergic psychedelics, dissociatives, and salvia. Besides the hallucinogenic effects, high doses of THC can also produce effects including anxiety, panic, paranoia, delusions, heavy sedation, and catalepsy. Strong THC exposures and associated hallucinogenic and aversive effects have been especially associated with cannabis edibles.

The mammalian cell production process, as used for most biopharmaceuticals, is divided into the four main steps: (1) Cultivation, or the reproduction of the cells; (2) Fermentation, or the actual production of the protein, typically in 10,000 Liter bioreactors; (3) Purification, or the separation of the cells from the culture medium and purification, mostly by chromatography; (4) Formulation, or the conversion of the sensitive proteins to a stable form. All steps are fully automated. The low productivity of the animal culture makes the technology expensive and vulnerable to contamination, as a small amount of bacteria would soon outgrow a larger population of animal cells. Its main disadvantages are low volume productivity and the animal provenance. It is conceivable that other technologies, particularly plant cell production, will gain importance in future. Given the fundamental differences between the two process technologies, plants for mammalian cell culture technologies have to be built ex novo. The pros and cons of an involvement of a fine chemical company in cell culture technology are listed below: Pros:

== History == Clomipramine was developed by Geigy as a chlorinated derivative of imipramine. It was first referenced in the literature in 1961 and was patented in 1963. The drug was first approved for medical use in Europe in the treatment of depression in 1970, and was the last of the major TCAs to be marketed. In fact, clomipramine was initially considered to be a "me-too drug" by the FDA, and in relation to this, was declined licensing for depression in the United States. As such, to this day, clomipramine remains the only TCA that is available in the United States that is not approved for the treatment of depression, in spite of the fact that it is a highly effective antidepressant. Clomipramine was eventually approved in the United States for the treatment of OCD in 1989 and became available in 1990. It was the first drug to be investigated and found effective in the treatment of OCD. The benefits in OCD were first reported by Juan José López-Ibor in 1967, and the first double-blind, placebo-controlled clinical trial of clomipramine for OCD was conducted in 1976, with more rigorous clinical studies that solidified its effectiveness conducted in the 1980s. It remained the "gold standard" for the treatment of OCD for many years until the introduction of the SSRIs, which have since largely superseded it due to greatly improved tolerability and safety (although notably not effectiveness).

When SCLC is found with one or more differentiated forms of lung cancer, such as squamous cell carcinoma or adenocarcinoma, the malignant tumor is then diagnosed and classified as a combined small cell lung carcinoma (c-SCLC). Small-cell lung carcinoma can occur in combination with a wide variety of other histological variants of lung cancer, including extremely complex malignant tissue admixtures.

== Nutrition and health == Koya-dofu is high in nutritional value. The way it is produced lets soy protein mature naturally, which helps in the development of new textures, preserving maximum nutritious value. Phytonutrients become more concentrated in it. Freeze-dried tofu serves as a source of protein, iron, and calcium. Consumption of this type of tofu lowers the risk of heart disease, diabetes, and obesity.

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.

What receptor does cardarine target?

Cardarine targets PPARδ, a nuclear receptor involved in lipid and energy metabolism. It does not bind the androgen receptor in the way SARMs do.

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