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Background And Regulatory Status — What the Evidence Shows

By Editorial Desk · published 2025-07-02 · last reviewed 2025-07-16 · Blog

A practical reference on GW501516: what it is, how it behaves, what the literature reports, and where the honest uncertainties sit.

Reviewed 2025-07-16. Anything still debated is marked as such rather than presented as settled.

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.

Background and Regulatory History

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

Reference notes

== Abstracting and indexing == Matrix Biology is abstracted and indexed in BIOBASE, Biochemistry and Biophysics Citation Index, Biological & Agricultural Index, Biological Abstracts, BIOSIS Previews, Chemical Abstracts Service, Current Advances in Ecological and Environmental Sciences, Current Awareness in Biological Sciences, Current Contents, EMBASE, EMBiology, Genetics Abstracts, MEDLINE, Science Citation Index, and Scopus. According to the Journal Citation Reports, the journal has a 2024 impact factor of 4.6.

==== Production ==== Animal hides are soaked in water to produce "stock". The stock is then treated with lime to break down the hides. The hides are then rinsed to remove the lime, any residue being neutralized with a weak acid solution. The hides are heated, in water, to a carefully controlled temperature around 70 °C (158 °F). The "glue liquor" is then drawn off, more water added, and the process repeated at increasing temperatures. The glue liquor is then dried and chipped into pellets.

Long bones are characterized by a shaft, the diaphysis, that is much longer than its width; and by an epiphysis, a rounded head at each end of the shaft. They are made up mostly of compact bone, with lesser amounts of marrow, located within the medullary cavity, and areas of spongy, cancellous bone at the ends of the bones. Most bones of the limbs, including those of the fingers and toes, are long bones. The exceptions are the eight carpal bones of the wrist, the seven articulating tarsal bones of the ankle and the sesamoid bone of the kneecap. Long bones such as the clavicle, that have a differently shaped shaft or ends are also called modified long bones. Short bones are roughly cube-shaped, and have only a thin layer of compact bone surrounding a spongy interior. Short bones provide stability and support as well as some limited motion. The bones of the wrist and ankle are short bones. Flat bones are thin and generally curved, with two parallel layers of compact bone sandwiching a layer of spongy bone. Most of the bones of the skull are flat bones, as is the sternum. Sesamoid bones are bones embedded in tendons. Since they act to hold the tendon further away from the joint, the angle of the tendon is increased and thus the leverage of the muscle is increased. Examples of sesamoid bones are the patella and the pisiform. Irregular bones do not fit into the above categories. They consist of thin layers of compact bone surrounding a spongy interior. As implied by the name, their shapes are irregular and complicated.

Sources: en.wikipedia.org

Related pages on this site

Notes from published material

== Side effects == Potential side effects of 5-HTP include heartburn, abdominal pain, nausea, vomiting, diarrhea, drowsiness, sexual problems, vivid dreams or nightmares, and muscle problems. Serotonin syndrome can occur. Because 5-HTP has not been thoroughly studied in a clinical setting, possible side effects and interactions with other drugs are not well known. According to the US National Library of Medicine, 5-HTP has not been associated with serotonin syndrome or any serious adverse events in humans. Across multiple studies, 5-HTP has also been reported to not cause any noticeable hematological or cardiovascular changes. 5-HTP had also been associated with eosinophilia, but later studies have not found any causal connection.

== Colleges and schools == Up until 2007, the university was divided into seven faculties (Arts, Celtic Studies, Commerce, Law, Medicine and Health Sciences, and Science), which were further subdivided into some 69 departments. In 2007–2008, the university transitioned from the faculties and departments structure to a structure of five colleges divided into various schools.

Cholestasis can be suspected when there is an elevation of both 5'-nucleotidase and ALP enzymes. With a few exceptions, the optimal test for cholestasis would be elevations of serum bile acid levels. However, this is not normally available in most clinical settings necessitating the use of other biomarkers. If 5' nucleosidase and ALP enzymes are elevated, imaging studies such as computed tomography (CT) scan, ultrasound, and magnetic resonance imaging (MRI) are used to differentiate intrahepatic cholestasis from extrahepatic cholestasis. Additional imaging, laboratory testing, and biopsies might be conducted to identify the cause and extent of cholestasis.

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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