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Identity And Pharmacological Classification — Reference Sheet

By Editorial Desk · published 2025-07-18 · last reviewed 2025-08-17 · Data

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

Reviewed 2025-08-17. Anything still debated is marked as such rather than presented as settled.

Identity and Pharmacological Classification

Published studies have examined GW501516 in animal models of obesity, insulin resistance, and exercise endurance. Early human trials reportedly ended, and development was discontinued after preclinical findings raised concerns about cancer in some rodent studies. Regulatory agencies have not approved cardarine for any medical use. Its availability through non-pharmaceutical channels raises questions about identity, purity, and legal status that are separate from its laboratory pharmacology. Those questions are often addressed through analytical testing rather than assumptions about product labels.

Cardarine is a common name for GW501516, also GW-1516, a synthetic compound developed as a peroxisome proliferator-activated receptor delta (PPARδ) agonist. It belongs to a class of agents that modulate gene transcription related to lipid and energy metabolism. The compound was studied in preclinical and early clinical research for metabolic and cardiovascular conditions, but it did not progress to approved therapeutic use. Its name appears in fitness and sports contexts despite not being approved as a drug.

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.

Cardarine at a glance

PropertyValueNotes
Chemical classPPARδ agonistNot an anabolic steroid.
Common synonymsGW501516, GW-1516Cardarine is an informal name.
AppearanceWhite to off-white powderTypical for research-grade solid.
Solubility classPoorly soluble in water; soluble in some organic solventsSuch as DMSO or ethanol in laboratory settings.
Typical storage temperatureCool, dry, protected from lightSpecific conditions vary by supplier and form.

Cardarine as Investigational PPARδ Agonist

Safety discussions about cardarine frequently cite rodent carcinogenicity findings reported in the 2000s. In those studies, treated animals developed tumors at multiple sites, leading sponsors to discontinue clinical development. The relevance of these findings to humans has not been resolved, but they are a major reason the compound is not approved. Current literature emphasizes uncertainty about long-term effects and the risks of unregulated use. Regulators and health agencies have not established a safe human exposure level.

Cardarine is a synthetic compound also known as GW501516, GW-501516, and sometimes endurobol. It was developed as a selective agonist of peroxisome proliferator-activated receptor delta, a nuclear receptor involved in fatty acid oxidation and energy metabolism. The compound was studied in preclinical models for metabolic and cardiovascular conditions, but it did not become a marketed human medicine. In regulatory and anti-doping contexts, it is treated as a prohibited substance rather than a licensed medicine.

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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.

Regulation and Analytical Detection

Products sold as cardarine have been found to contain incorrect compounds, variable amounts, or no active ingredient at all. Independent testing is required to verify identity and purity. Common analytical approaches include high-performance liquid chromatography, mass spectrometry, and nuclear magnetic resonance for structural confirmation. These methods can distinguish GW501516 from related PPAR agonists and from unrelated steroids. For regulators and researchers, such verification is central to interpreting both biological results and adverse event reports.

Cardarine is prohibited in competitive sport under the World Anti-Doping Agency code, where it is classified as a metabolic modulator. It is not approved as a prescription medicine in the United States, European Union, or other major markets. Regulatory action has focused on its presence in sports and in products marketed as research chemicals. Because it has no accepted medical indication, supply is often unregulated. This status creates legal and safety uncertainties for anyone who encounters the substance.

Anti-doping laboratories detect GW501516 and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is the most common matrix, though blood and dried blood spots may also be used in some programs. Detection depends on factors such as dose, timing, metabolism, and the sensitivity of the assay. Published methods describe limits of detection in the low nanogram per milliliter range for related compounds. Exact detection windows are not fixed for all situations and remain an area of ongoing study.

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.

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.

Reference notes

== Description and history == The Chicken McNugget is a small piece of processed chicken meat that is fried in batter and flash-frozen at a central manufacturing facility, then shipped out and sold at McDonald's restaurants. It was conceived by Keystone Foods founder Herb Lotman in the late 1970s. McDonald's first executive chef, René Arend, a native of Luxembourg, created the Chicken McNuggets recipe in 1979. "The McNuggets were so well-received that every franchise wanted them", said Arend in a 2009 interview. "There wasn't a system to supply enough chicken". Supply problems were solved by 1983, and Chicken McNuggets became available nationwide in the United States. In Canada, the national release was in late January 1984. According to McDonald's, the nuggets come in four shapes: the bell, the bone (or the bow-tie), the ball and the boot. The reason for the four different shapes is to ensure consistent cooking times for food safety. Four shapes were chosen because McDonalds states "The 4 shapes we make Chicken McNuggets in was the perfect equilibrium of dipability and fun. 3 would’ve been too few. 5 would’ve been, like, wacky." In 2014, as part of McDonald's U.S. "Our Food. Your Questions." transparency campaign, the company released a behind-the-scenes video explaining how Chicken McNuggets are made.

RA affects 0.5–1% of adults in the developed world, with between 5 and 50 per 100,000 people newly developing the condition each year. In 2010, it resulted in about 49,000 deaths globally. Onset is uncommon under the age of 15, and from then on, the incidence rises with age until the age of 80. Women are affected three to five times as often as men. The age at which the disease most commonly starts is in women between 40 and 50 years of age, and for men, somewhat later. RA is a chronic disease, and although rarely, a spontaneous remission may occur, the common course of progression consists of persistent symptoms that wax and wane in intensity, along with continued deterioration of joint structures, leading to deformation and disability. There is an association between periodontitis and rheumatoid arthritis (RA), hypothesised to lead to enhanced generation of RA-related autoantibodies. Oral bacteria that invade the blood may also contribute to chronic inflammatory responses and the generation of autoantibodies.

Small amounts of melamine have also been reported in foodstuff as a metabolite product of cyromazine, an insecticide used on animals and crops. The Food Safety and Inspection Service (FSIS) of the United States Department of Agriculture (USDA) provides a test method for analyzing cyromazine and melamine in animal tissues. In 2007, the FDA began using a high performance liquid chromatography test to determine the melamine, ammeline, ammelide, and cyanuric acid contamination in food. Another procedure is based on surface-enhanced Raman spectroscopy (SERS). Member states of the European Union are required under Commission Decision 2008/757/EC to ensure that all composite products containing at least 15% of milk product, originating from China, are systematically tested before import into the Community and that all such products which are shown to contain melamine in excess of 2.5 mg/kg are immediately destroyed. Following the 2008 melamine milk scandal, China restructured its food safety system by implementing the Food Safety Law, introducing stricter dairy industry regulations, and establishing independent third-party inspections to strengthen oversight and restore public trust. The 2009 Food Safety Law also reorganized government oversight by placing food safety regulation under a uniform national framework that employs risk-based standards and adheres to international Codex Alimentarius Commission guidelines.

Copper-alloy surfaces have natural intrinsic antimicrobial properties and can kill microorganisms such as E. coli and Staphylococcus. The United States Environmental Protection Agency approved the registration of antimicrobial copper alloy surfaces for use in addition to regular cleaning and disinfection to control infections. Antimicrobial copper alloys are being installed in some healthcare facilities and subway transit systems as a public hygienic measure. Copper nanoparticles are attracting interest for the intrinsic antimicrobial behaviours.

Sources: en.wikipedia.org

Reference notes

== External links == Gastrin-Releasing+Peptide at the U.S. National Library of Medicine Medical Subject Headings (MeSH) Nosek TM. "Section 6/6ch2/s6ch2_35". Essentials of Human Physiology. Archived from the original on 2016-03-24.

=== Other FDA measures === One exception occurred during the 2010 Swine Flu Epidemic when the FDA authorized expired Tamiflu based on SLEP Data. The US FDA is able to extend the shelf life of drugs throughout national, state, local, tribal, and territorial stockpiles through two legal means: by issuing an Emergency Use Authorization on using a drug past its expiration date (which is legally an unapproved use of a drug), or by a "expiration dating extension authority" established by the Pandemic and All-Hazards Preparedness Reauthorization Act of 2013 (PAHPRA). The PAHPRA authority only applies to so-called medical countermeasures (MCMs), which are drugs and other tools used to counter CBRN emergencies. Furthermore, FDA can choose to not take enforcement action against use of a drug past its expiration date using its enforcement discretion, but this kind of discretion is not covered by Public Readiness and Emergency Preparedness Act liability protections. The FDA has, using these three measures, provided shelf life extensions on Covid-19 vaccines, Covid-19 antibody therapeutics, Covid-19 in vitro diagnostics, flu antivirals (Tamiflu, Relenza), doxycycline, the Jynneos Mpox vaccine (one single lot), nerve agent autoinjectors, and potassium iodide.

=== Natural non-canonical bases === In a cell, there are several non-canonical bases present: CpG islands in DNA (often methylated), all eukaryotic mRNA (capped with a methyl-7-guanosine), and several bases of rRNAs (methylated). Often, tRNAs are heavily modified postranscriptionally in order to improve their conformation or base pairing, in particular in or near the anticodon: inosine can base pair with C, U, and even with A, whereas thiouridine (with A) is more specific than uracil (with a purine). Other common tRNA base modifications are pseudouridine (which gives its name to the TΨC loop), dihydrouridine (which does not stack as it is not aromatic), queuosine, wyosine, and so forth. Nevertheless, these are all modifications to normal bases and are not placed by a polymerase.

== Veterinary use == Paroxetine may be useful in the treatment of canine or feline behavioral diagnoses and is effective in the treatment of social anxiety, depression, and agitation associated with depression.

== History == In 1935, Hans Adolf Krebs discovered D-amino acid oxidase after an experiment with porcine kidney homogenates and amino acids. Shortly after, Warburg and Christian observed the oxidase had a FAD cofactor making it the second flavoenzyme to be discovered. In the upcoming years other scientists developed and improved the purification procedure for a porcine D-amino acid oxidase. In 1983, inhibitors for the oxidase were discovered. In 2006, the 3D structure of the oxidase was published. Currently, the link between human D-amino acid oxidase (hDAAO) activity and schizophrenia is being researched.

Sources: en.wikipedia.org

Frequently asked questions

What is cardarine also known as?

Cardarine is commonly known as GW501516 or GW-1516. These names refer to the same synthetic compound. It is not a brand-name approved medicine.

Is cardarine a steroid?

No, cardarine is not a steroid. It is classified as a PPARδ agonist. Its structure and receptor target differ from anabolic steroids.

Has cardarine been approved for human use?

No regulatory agency has approved cardarine as a medicine. It was investigated in early research but development was discontinued. It is not available as a prescription drug.

How is cardarine detected in samples?

Anti-doping and clinical laboratories commonly use liquid chromatography-tandem mass spectrometry. The method can identify GW501516 and its metabolites in urine or blood. Detection depends on sample timing and the amount present.

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