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Background And Regulatory Status — Complete Guide

By Editorial Desk · published 2026-01-07 · last reviewed 2026-01-26 · Info

If you have been reading about unapproved substance and want a single page that covers the useful parts, this is it: definitions, context, how it is studied, and the questions that come up repeatedly.

Updated 2026-01-26. 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

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.

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 Research Context

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.

Cardarine is a common name for GW501516, a synthetic compound developed in the 1990s through research collaborations involving GlaxoSmithKline. It belongs to a class of molecules known as peroxisome proliferator-activated receptor delta agonists. Early studies explored its effects on lipid metabolism and energy expenditure in animal models. The compound was never approved as a human medicine, and clinical development was discontinued. In the years since, it has appeared in fitness and bodybuilding communities as a performance-enhancing substance. Regulatory agencies classify it as an unapproved drug.

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.

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Mechanism and Laboratory Detection

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.

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.

Mechanism and Detection Methods

GW501516 acts as a selective agonist at PPARδ, a nuclear receptor that regulates transcription of genes involved in lipid handling and energy metabolism. Activation of PPARδ in preclinical models increases fatty acid oxidation, mitochondrial biogenesis, and exercise endurance in rodents. These effects have made the compound a subject of metabolic research and also a target for sport anti-doping rules. In humans, however, controlled studies are limited, and whether similar endurance or metabolic changes occur at tolerated exposures remains an open question. The receptor’s broad tissue distribution also means downstream effects may vary by organ and condition.

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.

Reference notes

Aminoglycosides display concentration-dependent bactericidal activity against "most gram-negative aerobic and facultative anaerobic bacilli" but not against gram-negative anaerobes and most gram-positive bacteria. They require only short contact time, and are most effective against susceptible bacterial populations that are rapidly multiplying. These activities are attributed to a primary mode of action as protein synthesis inhibitors, though additional mechanisms are implicated for some specific agents, and/or thorough mechanistic descriptions are as yet unavailable. These agents exhibit a post-antibiotic effect in which there is no or very little drug level detectable in blood, but there still seems to be inhibition of bacterial re-growth. This is due to strong, irreversible binding to the ribosome, and remains intracellular long after plasma levels drop, and allows a prolonged dosage interval. Depending on their concentration, they act as bacteriostatic or bactericidal agents.

== Toxicity == Studies carried out on the toxicity of convulxin show that symptoms are a function of the dose. The effects of the toxin stand out through the sudden and brief duration of the symptoms after exposure. In mice, low doses (5 μg/animal) administered intravenously (I.V) elicited tachypnea, followed by apnea, within 20 seconds. The ED50 for brief duration apnea was determined to be 180 μg/kg. Higher doses (10 μg/animal) evoked intense convulsive crisis, and usually ended with the death of the animal. LD50 was determined to be 524 μg/kg. Intraperitoneal (I.P.) administration of up to 200 μg/animal proved to be ineffective. In cats, I.V. injections of 100 μg/kg showed respiratory disturbances, miosis, salivation, abdominal cramps, nystagmus, loss of equilibrium, convulsions and sometimes a brief phase of hypotonia. The ED50 dose for convulsions is 80 μg/kg. The majority of animals recovered within 30 minutes. In dogs, the effect of convulxin showed two stages. After I.V. injection of 100-125 μg/kg they became excited, barked and exhibited loss of equilibrium, respiratory disturbances, nystagmus, urination, defecation and vomiting. After recovery, two out of five animals had intermittent crisis of clonic convulsions that appeared after 24 hours and lasted until their death. The other three dogs showed periods of vivid agitation alternating with torpor. While the lethal dose in humans is not yet known, what has been discovered is that the level of toxic effects depends on the origin of the snake. As for a cure, so far a polyvalent snake antivenom is being used.

=== Available forms === Mephedrone can come in capsules, tablets, or white powder, which users may swallow, insufflate, inject, smoke, or use rectally. When taken orally, users reported they could feel the effects within 15–45 minutes; when snorted, the effects were felt within minutes and peaked within half an hour. The effects last for between two and three hours when taken orally or nasally, but only half an hour if taken intravenously. It is sometimes sold mixed with methylone in a product called bubbles in the UK and also mixed with other cathinones, including ethcathinone, butylone, fluoromethcathinone and methedrone.

Biopolymers are polymers produced by living organisms. Cellulose and starch, proteins and peptides, and DNA and RNA are all examples of biopolymers, in which the monomeric units, respectively, are sugars, amino acids, and nucleotides. Cellulose is both the most common biopolymer and the most common organic compound on Earth. About 33% of all plant matter is cellulose. On a similar manner, silk (a proteinaceous biopolymer) has garnered tremendous research interest across various domains, including tissue engineering, regenerative medicine, microfluidics, and drug delivery. Bionics Hydrogel Polymeric surface Surface modification of biomaterials with proteins Synthetic biodegradable polymer List of biomaterials Oxygen generating biomaterial Journal of Biomaterials Applications CREB – Biomedical Engineering Research Centre Archived 2021-05-07 at the Wayback Machine Department of Biomaterials at the Max Planck Institute of Colloids and Interfaces in Potsdam-Golm, Germany Open Innovation Campus for Biomaterials Archived 2009-04-19 at the Wayback Machine

Sources: en.wikipedia.org

Notes from published material

By some estimates, this might account for most of the internal radiation damage, as the recoil nucleus is part of an atom that is much larger than an alpha particle, and causes a very dense trail of ionization; the atom is typically a heavy metal, which preferentially collect on the chromosomes. In some studies, this has resulted in an RBE approaching 1,000 instead of the value used in governmental regulations. The largest natural contributor to public radiation dose is radon, a naturally occurring, radioactive gas found in soil and rock. If the gas is inhaled, some of the radon particles may attach to the inner lining of the lung. These particles continue to decay, emitting alpha particles, which can damage cells in the lung tissue. The death of Marie Curie at age 66 from aplastic anemia was probably caused by prolonged exposure to high doses of ionizing radiation, but it is not clear if this was due to alpha radiation or X-rays. Curie worked extensively with radium, which decays into radon, along with other radioactive materials that emit beta and gamma rays. However, Curie also worked with unshielded X-ray tubes during World War I, and analysis of her skeleton during a reburial showed a relatively low level of radioisotope burden. The Russian defector Alexander Litvinenko's 2006 murder by radiation poisoning is thought to have been carried out with polonium-210, an alpha emitter.

=== Metabolic disorders === Preclinical evidence from animal models suggests that S. boulardii supplementation may reduce body weight in the context of type 2 diabetes; however, clinical evidence in humans is currently lacking. Additional studies in diet-induced obesity models further support these findings, showing that S. boulardii can attenuate weight gain, reduce food intake, and increase energy expenditure. These effects are accompanied by coordinated changes in gut microbiota composition, microbial metabolic activity, and host immune signaling, including reduced inflammatory pathways (e.g., TNFα/NF-κB) and shifts in metabolites linked to metabolic regulation, suggesting modulation of the gut–immune–metabolic axis.

=== Locus === The Homo sapiens FGFR1OP2 gene is located on chromosome 12, with its specific locus being 12p11.23. The Homo sapiens asunder spermatogenesis regulator (ASUN) gene (NCBI Reference Sequence NM_018164.2) is located directly upstream from FGFR1OP2. The ASUN gene is a regulator of development and the mitotic cell cycle. The Homo sapiens transmembrane 7 superfamily member 3 (TM7SF3) gene is located slightly downstream from FGFR1OP2.

Patrick Brenan, Finance Director, Minories Finance Ltd. For services to Banking. Linda Broadhead, Senior Management Pay Band 2, the Employment Service, Department for Education and Employment. Rosemary Anne Brown, Member, Occupational Pensions Board. For services to Pensions Legislation. Barbara Kathleen Bryant, Grade 7, Department of Social Security. Keith Patrick Burke, Managing Director, Dana Spicer Europe Ltd., Dana Corporation. For services to Industry and to the Environment. David Burnett. For services to the Development and Application of Biochemistry to Health Care. William John Burnison. For public service. Derek Harold Calam, Member and Vice Chairman, British Pharmacopoeia Commission. For services to the Control of Medicines. Libby Campbell, Executive Director, Nursing and Quality, West Lothian NHS Trust. For services to Health Care. Dennis Duncan Carmichael, Honorary Treasurer, Lawn Tennis Association. For services to Lawn Tennis. Enid Castle, lately Principal, Cheltenham Ladies' College. For services to Education. Jonathan Joseph Chadwick, Secretary to the Imperial War Museum. Christopher Charlton, Director, Cromford Mill Project, Derbyshire. For services to Conservation. Professor Dennis Child. For services to Deaf People. Edward Samuel Childs, Executive Producer, Carlton UK Television. For services to Television Broadcasting. Brian James Clark, Principal Specialist Inspector, Health and Safety Executive, Department of the Environment. Harold Clarke, District Inspector, Board of Inland Revenue. Seamus Anthony Close. For public service.

The fifth season of the American television drama series Scandal was ordered on May 7, 2015, by ABC, and began airing on September 24, 2015, in the United States on ABC. The season was produced by ABC Studios, in association with ShondaLand Production Company; the showrunner being Shonda Rhimes. The season continues the story of Olivia Pope's crisis management firm, Olivia Pope & Associates, and its staff, as well as staff at the White House in Washington, D.C. Season five has eleven series regulars, all returning from the previous season, out of which six are part of the original cast of eight regulars from the first season and three new regulars were added. The season will continue to air in the Thursday 9:00 pm timeslot, the same as the previous season as it was moved to make room for ShondaLand Production Company's new TV series, How to Get Away with Murder. On March 3, 2016, ABC announced that Scandal was renewed for a sixth season.

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.

How does cardarine work in the body?

It binds to and activates PPAR delta, a nuclear receptor that controls expression of genes related to fatty acid oxidation. This mechanism can alter energy metabolism in animal models. It is not a direct stimulant or fat-burning enzyme.

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