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Background And Regulatory Status — Worked Examples

By Editorial Desk · published 2025-12-13 · last reviewed 2026-01-01 · Topic

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

This page was last updated on 2026-01-01 and is reviewed periodically as new material appears.

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.

Mechanism and Safety Research

GW501516 acts as an agonist at the peroxisome proliferator-activated receptor delta, a nuclear receptor that regulates gene expression. Activation shifts transcription toward genes involved in fatty acid uptake, oxidation, and energy expenditure. The compound does not bind the androgen receptor and therefore differs from anabolic steroids and SARMs. In rodent models, this metabolic shift has been linked to increased running endurance and reduced fat accumulation. The exact downstream pathways in humans remain incompletely characterized.

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.

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 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.

Anti-doping laboratories identify GW501516 and related metabolites using liquid chromatography coupled with tandem mass spectrometry. Urine is the most common matrix, though blood and dried blood spots may also be analyzed. The method targets the parent compound and phase I and phase II metabolites, which extend the detection window. Because the substance is prohibited at all times, athletes can be tested outside competition. Detection limits and windows depend on the assay, sample type, and individual metabolism.

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.

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Identity and Regulatory Status

Cardarine is a common name for GW501516, an investigational compound developed in the 1990s for metabolic conditions. It acts as an agonist at peroxisome proliferator-activated receptor delta, a nuclear receptor involved in lipid and energy metabolism. The compound is frequently mislabeled as a selective androgen receptor modulator, or SARM, but its molecular target is different. GW501516 reached early clinical testing before development was discontinued. It has no approved therapeutic use in any country. The name cardarine is not a formal international nonproprietary name.

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.

Mechanism and Detection

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.

Anti-doping laboratories identify GW501516 and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is the usual matrix, and detection can occur after the parent compound has cleared from blood. The exact detection window depends on dose, formulation, individual metabolism, and assay sensitivity. Because the compound is prohibited at all times, athletes are subject to testing in and out of competition. Analytical methods continue to improve as new metabolites and designer analogs are characterized.

Identity and Pharmacological Mechanism

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.

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.

Notes from published material

=== Muscle Media === In 1997, Phillips was eager to expand his empire beyond the bodybuilding industry. MM2K changed from targeting the hardcore bodybuilder to the more mainstream exercise participant, and the July 1997 issue saw the magazine redubbed simply as Muscle Media. While Muscle Media 2000 had a distribution of 500,000 copies per issue at its peak, the change in direction alienated many traditional readers, and sales numbers reportedly declined sharply afterwards. Publication finally ceased in 2004 after the EAS company was sold a second time.

==== 2600–2699 ==== Greater Manchester Ambulance Service National Health Service Trust (Establishment) Order 1993 (S.I. 1993/2600) Lancashire Ambulance Service National Health Service Trust (Establishment) Order 1993 (S.I. 1993/2601) Tameside and Glossop Acute Services National Health Service Trust (Establishment) Order 1993 (S.I. 1993/2602) Darlington Memorial Hospital National Health Service Trust (Establishment) Order 1993 (S.I. 1993/2603) Bolton Hospitals National Health Service Trust (Establishment) Order 1993 (S.I. 1993/2604) Priority Healthcare Wearside National Health Service Trust (Establishment) Order 1993 (S.I. 1993/2605) Community Health Care Service (North Derbyshire) National Health Service Trust (Establishment) Order 1993 (S.I. 1993/2606) Wirral Community Healthcare National Health Service Trust (Establishment) Order 1993 (S.I. 1993/2607) North Lakeland Healthcare National Health Service Trust (Establishment) Order 1993 (S.I. 1993/2608) North Downs Community Health National Health Service Trust (Establishment) Order 1993 (S.I. 1993/2609) South Durham Health Care National Health Service Trust (Establishment) Order 1993 (S.I. 1993/2610) Salford Community Health Care National Health Service Trust (Establishment) Order 1993 (S.I. 1993/2611) Community Health Care: North Durham National Health Service Trust (Establishment) Order 1993 (S.I. 1993/2612) Kingston and District Community National Health Service Trust (Establishment) Order 1993 (S.I. 1993/2613) North Durham Acute Hospitals National Health Service Trust (Establishment) Order 1993 (S.I.

=== Available forms === Two arsenic-containing stereoisomers exist in a 3:1 molar ratio. Since melarsoprol is insoluble in water, dosage occurs via a 3.6% propylene glycol intravenous injection. To avoid the risk of injection site reactions, melarsoprol must be given slowly. Melarsoprol used for the treatment of African trypanosomiasis with CNS involvement is given under a complicated dosing schedule. The dosing schedule for children and adults is 2–3.6 mg/kg/day intravenously for three days, then repeated every seven days for a total of three series. To monitor for relapse, follow-up is recommended every six months for at least two years.

Sources: en.wikipedia.org

Further detail

== Press freedom == The 2020 World Press Freedom Index published by Reporters without Borders ranked Thailand 140 of 180 (1=best; 180=worst) nations in press freedom. Other ASEAN nations were ranked: Malaysia, 101; Indonesia, 119; Philippines, 136; Myanmar, 139; Cambodia, 144; Brunei, 152; Singapore, 158; Laos, 172; Vietnam, 175. The 2019 World Press Freedom Index published by Reporters without Borders ranked Thailand 136 of 180 (1=best; 180=worst) nations in press freedom. Other ASEAN nations were ranked: Malaysia, 123; Indonesia, 124; Philippines, 134; Myanmar, 138; Cambodia, 143; Singapore, 151; Brunei, 152; Laos, 171; Vietnam, 176. The 2018 World Press Freedom Index published by Reporters without Borders ranked Thailand 140 of 180 (1=best; 180=worst) nations in press freedom. Other ASEAN nations were ranked: Indonesia, 124; Philippines, 133; Myanmar, 137; Cambodia, 142; Malaysia, 145; Singapore, 151; Brunei, 153; Laos, 170; Vietnam, 175. The World Press Freedom Index 2016: Reporters Without Borders ranked Thailand 136 of 180 (1=best, 180=worst) countries. ASEAN as a whole ranked poorly, with Cambodia the best at 128 and Vietnam the worst at 175. The World Press Freedom Index 2015: Reporters Without Borders ranked Thailand 134 of 180 (1=best, 180=worst) countries Freedom of the Press 2015: Thailand was ranked 166 of 199 (1=best, 199=worst) nations by Freedom House.

In the process prior to filling and sealing, individual bottles are always rinsed with deionised water to remove any particles that could cause a change in taste. Deionised and distilled water are used in lead–acid batteries to prevent erosion of the cells, although deionised water is the better choice as more impurities are removed from the water in the creation process.

== 3-Dimensional proximity-based technology (YoctoReactor technology) == The YoctoReactor (yR) is a 3D proximity-driven approach which exploits the self-assembling nature of DNA oligonucleotides into 3, 4 or 5-way junctions to direct small molecule synthesis at the center of the junction. Figure 5 illustrates the basic concept with a 4-way DNA junction.

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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