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Background And Regulatory Status — Practical Notes

By Editorial Desk · published 2026-01-20 · last reviewed 2026-02-03 · Topic

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

Reviewed 2026-02-03. Anything still debated is marked as such rather than presented as settled.

Background and Regulatory Status

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.

Mechanism and Safety Research

Early clinical research explored GW501516 for lipid disorders, obesity, and diabetes. Some short-term human studies reported changes in HDL cholesterol, LDL cholesterol, and triglycerides. The development program was discontinued after rodent studies showed dose-dependent tumor formation in multiple tissues, including liver, bladder, stomach, and skin. These findings raised concerns about long-term cancer risk in humans. Because human exposure data are limited, the clinical significance of the rodent tumors remains uncertain.

Literature on cardarine often separates receptor pharmacology from toxicology. Mechanistic papers describe PPARδ activation and gene expression changes, while safety assessments focus on carcinogenicity and species differences. Questions remain about whether rodent tumors arise through PPARδ-dependent or off-target mechanisms. Another open area is how human metabolism and exposure compare with those in animal studies. Analytical methods such as liquid chromatography–mass spectrometry are used to confirm identity in biological and product samples.

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

Regulation and Detection

Cardarine is frequently described as a fat-burning or endurance-enhancing supplement, but these claims exceed the available evidence. The compound is not a hormone, steroid, or selective androgen receptor modulator. Research articles discuss it as a tool compound for studying PPARδ biology, while anti-doping literature focuses on its abuse and detection. Quality of unapproved products is uncertain, and independent analyses have found impurities or incorrect labeling. Open questions include whether human cancer risk resembles that seen in rodents and how often non-athletes use the substance.

Cardarine has no approved therapeutic indication and is not marketed as a medicine. The World Anti-Doping Agency lists GW501516 as a prohibited substance at all times, covering both in-competition and out-of-competition periods. National laws vary: some countries treat it as an unapproved drug subject to import controls, while others have specific restrictions on sale for human consumption. It is often sold as a research chemical, a label that does not imply safety or legality. Enforcement actions have targeted online vendors and shipments.

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Identity and Regulatory Status

Regulatory treatment varies, but cardarine is not approved as a medicine. Sports authorities list GW501516 as a prohibited substance, and it is banned at all times under the World Anti-Doping Agency code. Many countries restrict sales for human consumption, while online vendors market it as a research chemical. Such products may lack purity data, and their actual contents can differ from the label. Purchasing or possessing cardarine may carry legal consequences depending on jurisdiction. The compound is not a dietary supplement ingredient in regulated markets.

Clinical development stopped after rodent studies showed tumors at multiple sites. Whether those findings predict human cancer risk remains an open question, but they led sponsors to discontinue programs. Human safety data are limited to small, short-term studies that were not designed to assess cancer risk. Reported effects in those studies included changes in blood lipids, but the evidence is insufficient for medical use. Long-term consequences of nonmedical use are not well characterized. Questions about dose, duration, and individual susceptibility remain unresolved.

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.

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.

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

The renin enzyme circulates in the bloodstream and hydrolyzes (breaks down) angiotensinogen secreted from the liver into the peptide angiotensin I. Angiotensin I is further cleaved in the lungs by endothelial-bound angiotensin-converting enzyme (ACE) into angiotensin II, the most vasoactive peptide. Angiotensin II is a potent constrictor of all blood vessels. It acts on the smooth muscle and, therefore, raises the resistance posed by these arteries to the heart, and so for the same cardiac output, the blood pressure will rise. Angiotensin II also acts on the adrenal glands and releases aldosterone, which stimulates the epithelial cells in the distal tubule and collecting ducts of the kidneys to increase re-absorption of sodium, exchanging with potassium to maintain electrochemical neutrality, and water, leading to raised blood volume and raised blood pressure. The RAS also acts on the CNS to increase water intake by stimulating thirst, as well as conserving blood volume, by reducing urinary loss through the secretion of vasopressin from the posterior pituitary gland. The normal concentration of renin in adult human plasma is 1.98–24.6 ng/L in the upright position.

UK-414,495 is a drug developed by Pfizer for the treatment of female sexual arousal disorder. UK-414,495 acts as a potent, selective inhibitor of the enzyme neutral endopeptidase, which normally serves to break down the neuropeptide VIP. The consequent increase in VIP activity alters blood flow to the genital region leading to increased lubrication and muscle relaxation.

nonilfenossipolietilenossietanolo (33 letters – chemical) pentagonododecaedrotetraedrico (30 letters – 3D geometric figure) esofagodermatodigiunoplastica (29 letters – surgery) elettroencefalograficamente (27 letters – medical adverb: electroencephalographically) diclorodifeniltricloroetano (27 letters – chemical: DDT)

Silent narration This style of narration uses title screens to visually narrate the documentary. The screens are held for about 5–10 seconds to allow adequate time for the viewer to read them. They are similar to the ones shown at the end of movies based on true stories, but they are shown throughout, typically between scenes.

Sources: en.wikipedia.org

Supporting material

=== Religious organizations === Celtic Reconstructionism, a form of Polytheism Congregation of Clerics Regular of the Divine Providence (Theatines), a Roman Catholic religious order Community of the Resurrection, an Anglican religious order Congregation of the Resurrection, a Catholic religious order

Matlock is an American legal drama television series that premiered with a sneak peek on September 22, 2024, before its timeslot premiere on October 17 on CBS. The show was developed by Jennie Snyder Urman, and while it shares a name with the Matlock TV series which starred Andy Griffith, it features a vastly different premise overall. In October 2024, the series was renewed for a second season which premiered on October 12, 2025. In January 2026, the series was renewed for a third season.

=== Pharmacokinetics === A small amount of rimexolone is absorbed into the systemic circulation. On hourly treatment with the eye drops for a week, blood serum concentrations peaked at 150 pg/ml on average, with many patients remaining below the detection threshold of 80 pg/ml. The elimination half-life from the circulation is estimated at one to two hours; the substance is mainly (over 80%) excreted via the faeces.

== Research == Pseudoephedrine has been studied in the treatment of snoring. However, data are inadequate to support this use. A study has found that pseudoephedrine can reduce milk production in breastfeeding women. This might have been due to suppression of prolactin secretion. Pseudoephedrine might be useful for lactation suppression.

== Bibliography == Audi, G.; Kondev, F. G.; Wang, M.; et al. (2017). "The NUBASE2016 evaluation of nuclear properties". Chinese Physics C. 41 (3) 030001. Bibcode:2017ChPhC..41c0001A. doi:10.1088/1674-1137/41/3/030001. Beiser, A. (2003). Concepts of modern physics (6th ed.). McGraw-Hill. ISBN 978-0-07-244848-1. OCLC 48965418. Hoffman, D. C.; Ghiorso, A.; Seaborg, G. T. (2000). The Transuranium People: The Inside Story. World Scientific. ISBN 978-1-78-326244-1. Kragh, H. (2018). From Transuranic to Superheavy Elements: A Story of Dispute and Creation. Springer. ISBN 978-3-319-75813-8. Zagrebaev, V.; Karpov, A.; Greiner, W. (2013). "Future of superheavy element research: Which nuclei could be synthesized within the next few years?". Journal of Physics: Conference Series. 420 (1) 012001. arXiv:1207.5700. Bibcode:2013JPhCS.420a2001Z. doi:10.1088/1742-6596/420/1/012001. ISSN 1742-6588. S2CID 55434734.

Sources: en.wikipedia.org

Notes from published material

=== Pharmacodynamics === Phenelzine is a non-selective and irreversible inhibitor of monoamine oxidase. It inhibits both MAO-A and MAO-B, with only slight preference for MAO-A. By inhibiting monoamine oxidase, phenelzine reduces the metabolic breakdown of serotonin, norepinephrine, dopamine, and related trace amines. Classic MAOIs increase the absolute amount of these neurotransmitters within as well as outside neurons, unlike reuptake inhibitors, which mainly produce relative extracellular increases by blocking transporter-mediated reuptake. This mechanism, together with phenelzine's additional effects on GABA metabolism, is thought to contribute to its antidepressant and anxiolytic effects. Phenelzine and its metabolites also inhibit other enzymes to a lesser extent, two of which are alanine transaminase (ALA-T), and γ-aminobutyric acid transaminase (GABA-T), the latter of which is not caused by phenelzine itself, but by phenylethylidenehydrazine (PEH), which is a phenelzine metabolite. By inhibiting GABA-T and ALA-T, phenelzine causes an increase in the alanine and GABA levels in the brain and body. GABA is the major inhibitory neurotransmitter in the central nervous system of mammals, and is very important for the normal suppression of anxiety, stress, and depression. Phenelzine's action in increasing GABA concentrations may significantly contribute to its antidepressant, and especially, anxiolytic/antipanic properties, the latter of which have been considered superior to those of other antidepressants.

=== Original format === The original FASTA/Pearson format is described in the documentation for the FASTA suite of programs. It can be downloaded with any free distribution of FASTA (see fasta20.doc, fastaVN.doc, or fastaVN.me—where VN is the Version Number). In the original format, a sequence was represented as a series of lines, each of which was no longer than 120 characters and usually did not exceed 80 characters. This probably was to allow for the preallocation of fixed line sizes in software: at the time most users relied on Digital Equipment Corporation (DEC) VT220 (or compatible) terminals which could display 80 or 132 characters per line. Most people preferred the bigger font in 80-character modes and so it became the recommended fashion to use 80 characters or less (often 70) in FASTA lines. Also, the width of a standard printed page is 70 to 80 characters (depending on the font). Hence, 80 characters became the norm. The first line in a FASTA file started either with a ">" (greater-than) symbol or, less frequently, a ";" (semicolon) was taken as a comment. Subsequent lines starting with a semicolon would be ignored by software. Since the only comment used was the first, it quickly became used to hold a summary description of the sequence, often starting with a unique library accession number, and with time it has become commonplace to always use ">" for the first line and to not use ";" comments (which would otherwise be ignored).

Anglo Boer War - Home The Boer War, A 2 part documentary series shown on British television (1999). Scrapbook of Boer War, MSS P 456 at L. Tom Perry Special Collections, Harold B. Lee Library, Brigham Young University The Concentration Camps 1899–1902 by Hennie Barnard Archived 23 March 2020 at the Wayback Machine British Commanders of the Boer War, Link

== Function == It is known that it participates in some specific immune responses. It plays a part in tissue inflammation as well as the engulfing of pathogens by phagocytes. In addition it is known to help to neutralize some viruses. The properdin promotes the association of C3b with Factor B and provides a focal point for the assembly of C3bBb on a surface. It binds to preformed alternative pathway C3-convertases. Properdin also inhibits the Factor H – mediated cleavage of C3b by Factor I. Properdin, in addition to Factor H, can bind to glycosaminoglycan (GAG) epitopes by renal tubular heparin sulfates. Additionally, the binding of properdin to Salmonella typhosa lipopolysaccharide (LPS) and Neisseria meningitidis lipopolysaccharide result in activation of the complementary alternative pathway. Furthermore, it binds to various microbial surfaces, resulting in the assembly of the alternative pathway C3 convertase.

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 is the main molecular target of cardarine?

It targets PPARδ, a nuclear receptor involved in lipid and energy metabolism. It does not act primarily on androgen receptors. This distinction separates it from SARMs.

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