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Cardarine As Investigational Pparδ Agonist — Common Mistakes

By Editorial Desk · published 2026-01-02 · last reviewed 2026-02-23 · Info

Everything below concerns preclinical models. We keep the language plain, cite what the science says, and separate well-supported claims from open questions.

Last reviewed on 2026-02-23. Where a claim depends on a specific study, the study is described rather than over-claimed.

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.

Detection, Regulation, and Quality Context

Because cardarine is not an approved medicine, no pharmacopeial monograph defines its identity, purity, or storage requirements. Laboratories typically rely on in-house methods and reference standards when testing materials labeled as GW501516. Certificates of analysis may report purity and identity for a specific batch, but their scope varies and they do not guarantee safety or legal status. Independent verification can include high-performance liquid chromatography, mass spectrometry, nuclear magnetic resonance, and elemental analysis. The distinction between research chemical labeling and human use is significant because quality standards and oversight differ.

Cardarine can be detected in biological samples and product materials using liquid chromatography coupled to tandem mass spectrometry (LC-MS/MS). The method separates compounds by chromatography and identifies them by mass-to-charge transitions, allowing low-level detection in urine or blood. Sample preparation often involves enzymatic hydrolysis, solid-phase extraction, or protein precipitation. Certified reference materials and isotope-labeled internal standards improve quantification. Detection windows depend on metabolism, matrix, and assay sensitivity, so no single universal window applies.

Regulatory treatment of cardarine differs by context and jurisdiction. In competitive sport, the World Anti-Doping Agency lists PPARδ agonists, including GW501516, as prohibited at all times. Outside sport, it lacks approval as a prescription medicine in major drug markets, and products sold for human consumption may be treated as unapproved drugs. Some countries also restrict importation or sale through general consumer protection and medicines laws. These classifications affect availability, testing, and legal risk without establishing therapeutic value.

Cardarine at a glance

PropertyValueNotes
Common synonymsGW501516, GW-501516, GW 501516, endurobolNames vary in research and anti-doping documents.
Chemical classSynthetic PPARδ agonistSmall-molecule nuclear receptor ligand.
CAS Registry Number317318-70-0Identifier commonly associated with GW501516.
AppearanceWhite to off-white powderTypical for purified research material.
SolubilityLow in water; soluble in DMSO and ethanolOrganic solvents are common for laboratory stock solutions.

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.

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Mechanism and Research Context

GW501516 acts as an agonist at peroxisome proliferator-activated receptor delta, a nuclear receptor involved in transcription of genes related to lipid handling and energy use. Activation of PPARδ can shift skeletal muscle toward greater fatty acid oxidation in animal models, which is one reason it drew interest for metabolic disease and exercise research. The exact downstream effects depend on tissue, species, dose, and duration. Human data are sparse, so many proposed benefits remain hypotheses rather than established clinical outcomes.

Laboratory studies have examined GW501516 in cell cultures and rodents for conditions such as dyslipidemia, insulin resistance, and obesity. Some trials in humans were initiated, but development was discontinued after preclinical findings raised concerns about cancer in certain models. Those findings do not prove that the compound causes cancer in people, but they contributed to regulatory caution. Later reviews often describe the evidence as preliminary and insufficient for assessing long-term safety.

Background and Regulatory History

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.

Regulatory bodies treat GW501516 as a prohibited substance in competitive sport. The World Anti-Doping Agency added it to the prohibited list, and it falls under classes covering metabolic modulators and hormone-related agents. It is not approved by drug regulators for human use, and it is not a lawful dietary supplement. Products sold under the cardarine name may contain unlisted ingredients or different compounds. Because no approved product exists, quality and identity are not guaranteed by pharmaceutical manufacturing standards.

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.

Reference notes

Indolyl-3-acryloylglycine, also known as trans-indolyl-3-acryloylglycine, or IAG for short, is a compound consisting of an indole group attached to an acrylic acid moiety, which is in turn attached to a glycine molecule. This compound has been shown to isomerize when exposed to light. It is likely a metabolic intermediate in the biosynthesis of tryptophan, and is synthesized from tryptophan via indolepropionic acid and indoleacrylicacid (IAcrA). It is also likely that IAcrA is converted into IAG in the gut wall. It may also be produced by certain elements of the mammalian gut microbiota by phenylalanine ammonia-lyase. Identifiable in the urine by high-performance liquid chromatography, it may be a biomarker for autism spectrum disorders, as demonstrated by the research of Paul Shattock and other researchers from Australia. These researchers have reported that urinary levels of IAG are much higher in autistic children than in controls; however, other researchers have found no association between IAG concentrations in the urine and autism. Its excretion in the urine may also be changed in Hartnup disease and celiac disease, as well as photodermatosis, muscular dystrophy, and liver cirrhosis.

Every gland is formed by an ingrowth from an epithelial surface. This ingrowth may in the beginning possess a tubular structure, but in other instances glands may start as a solid column of cells which subsequently becomes tubulated. As growth proceeds, the column of cells may split or give off offshoots, in which case a compound gland is formed. In many glands, the number of branches is limited, in others (salivary, pancreas) a very large structure is finally formed by repeated growth and sub-division. As a rule, the branches do not unite with one another. One exception to this rule is the liver; this occurs when a reticulated compound gland is produced. In compound glands the more typical or secretory epithelium is found forming the terminal portion of each branch, and the uniting portions form ducts and are lined with a less modified type of epithelial cell. Glands are classified according to their shape.

In Korea, lotus flower tea (Korean: 연꽃차; RR: yeonkkotcha) is made from the dried petals of the white lotus. The stamens can be dried and made into a fragrant herbal tea (Chinese: 蓮花 茶; pinyin: liánhuā cha; Cantonese Yale: lìhnfāa chah), or used to impart a scent to tea leaves (particularly in Vietnam). This Vietnamese lotus tea is called trà sen, chè sen, or chè ướp sen.

23 February A PAVN rocket attack on Da Nang Air Base destroyed a 450,000 gallon fuel tank beside the base and damaged a Marine A-6 Intruder. PAVN sappers attacked Hill 327 and the positions of the 2nd Battalion 7th Marines northwest of the Hill, both attacks were beaten back with 18 Marines killed and 80 wounded while the PAVN lost 75 killed or captured. A PAVN sapper attack on Dầu Tiếng Base Camp resulted in 21 U.S. and 73 PAVN killed. The PAVN 271st and 272nd Regiments attacked Patrol Base Diamond I occupied by the U.S. 2nd Battalion, 27th Infantry Regiment. The attack was repulsed with artillery and gunship fire with an estimated 118 PAVN killed and two captured.

The agent A-234 is also supposedly around five to eight times more potent than VX. The median lethal dose for inhaled A-234 has been estimated as 7 mg/m3 for two minute exposure (minute volume of 15 L, slight activity). The median lethal dose for inhaled A-230, likely the most toxic liquid Novichok, has been estimated as between 1.9 and 3 mg/m3 for two minute exposure. Thus the median lethal dose for inhaled A-234 is 0.2 mg (5000 lethal doses in a gram) and is below 0.1 mg for A-230 (10 000 lethal doses in a gram).

Sources: en.wikipedia.org

Reference notes

=== Medieval to early modern era === In medieval Europe, merchant guilds organized long-distance commerce and also participated in local wholesale trade. These guilds protected members, negotiated privileges, and in some places influenced city government and rules that shaped how goods were distributed and sold. In many regions, food distribution also relied on wholesale markets where trade concentrated in one place. Over time, wholesale markets became important for matching supply with demand and supporting price formation in urban food systems.

== External links == International Emergency Economic Powers Act as amended (PDF/details) in the GPO Statute Compilations collection International Emergency Economic Powers Act as enacted (details) in the US Statutes at Large

== External links == Skin graft. MedlinePlus Medical Encyclopedia. Parts of this US Federal Government public domain text were used in the article. An introduction to the use of vacuum assisted closure.

Nicotinamide is recommended as a treatment for niacin deficiency because it can be administered in remedial amounts without causing the flushing, considered an adverse effect. In the past, the group was loosely referred to as vitamin B3 complex. Extra-terrestrial nicotinic acid and nicotinamide have been detected in carbonaceous chondrite meteorites and in sample-returns from the asteroids 162173 Ryugu and 101955 Bennu.

Sources: en.wikipedia.org

Frequently asked questions

What is cardarine?

Cardarine is an investigational synthetic compound that acts as a PPARδ agonist. It is also known as GW501516 and has been studied mainly in preclinical research. It is not an approved medicine.

Is cardarine a steroid?

No. Cardarine is not a steroid hormone; it targets the nuclear receptor PPARδ. Its classification in anti-doping rules differs from anabolic steroids, though it remains prohibited in sport.

Why was cardarine not developed further?

Early rodent studies reported tumor formation at multiple sites, which raised safety concerns. Sponsors stopped clinical development, and no approved human product exists.

How is cardarine detected in anti-doping tests?

Anti-doping laboratories typically use LC-MS/MS to detect GW501516 and its metabolites in urine. The method is sensitive and can identify the compound at low concentrations. Detection depends on sample timing, metabolism, and the specific assay.

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