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Identity And Pharmacological Classification — Evidence Review

By Editorial Desk · published 2025-11-10 · last reviewed 2025-12-17 · Guide

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 2025-12-17. 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.

PPARδ is a nuclear receptor that influences transcription of genes involved in fatty acid oxidation, lipid transport, and energy homeostasis. GW501516 binds and activates this receptor with high selectivity relative to PPARα and PPARγ in laboratory assays. Activation alters expression of target genes in skeletal muscle, liver, and adipose tissue in animal models. The exact clinical consequences of these changes in humans remain incompletely characterized, and observed effects in animals do not establish therapeutic benefit or safety.

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.

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.

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.

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Cardarine as Investigational PPARδ Agonist

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.

The pharmacological interest in cardarine centers on PPARδ activation and its downstream effects on lipid handling and mitochondrial function. In animal studies, PPARδ agonists have been associated with changes in exercise endurance and fatty acid utilization, though results vary by model and protocol. Human data remain sparse, and the absence of large controlled trials limits conclusions about efficacy. Researchers often describe the compound as a tool for probing PPARδ biology rather than a proven therapeutic agent.

Regulation and Detection

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.

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.

Background from the literature

On Thursday, February 1, 1866, Mary Baker Eddy, then known as Mary Patterson, fell on the ice in Lynn, Massachusetts. She had been on the way to a Good Templars meeting, an organization supporting the temperance movement, with friends from the organization. After her fall, the Lynn Reporter wrote that she was "in an insensible condition" and had internal injuries, and the notes of Dr. Alvin M. Cushing, a homeopathic doctor, who was called to the scene, state that he found Eddy "partially unconscious, semi-hysterical and complaining by word and action of severe pain in the back of her head and neck." She was taken to the nearest house, that of Samuel M. Bubier the future mayor of Lynn, and spent the night there. Cushing attended to her multiple times that day and during the night, which Gill writes "indicates that he considered the accident serious," and he gave orders that homeopathic medicine be continually given her at intervals of every half hour when she was awake while he was not present. Cushing later told Sibyl Wilbur that Eddy "was taken up unconscious and remained unconscious during the night" and that he thought she was "suffering from a concussion, and possible spinal dislocation." The next morning Eddy asked to be taken to her home in Swampscott, which Cushing arranged for against his own professional advice. In order to dull the pain of moving, Cushing gave Eddy "one-eighth of a grain of morphine" (a common painkiller at the time) according to his notes from the period.

CAL interdentally is >2mm on at least 2 non-adjacent teeth CAL buccally/orally is >3mm with pocket depths of >3mm on at least two teeth. As periodontitis is not the sole cause of clinical attachment loss, any CAL attributed to the following factors is not considered during diagnosis.

Some meteorologists prefer the hectopascal (hPa) for atmospheric air pressure, which is equivalent to the older unit millibar (mbar). Similar pressures are given in kilopascals (kPa) in most other fields, except aviation where the hecto- prefix is commonly used. The inch of mercury is still used in the United States. Oceanographers usually measure underwater pressure in decibars (dbar) because pressure in the ocean increases by approximately one decibar per metre depth. The standard atmosphere (atm) is an established constant. It is approximately equal to typical air pressure at Earth mean sea level and is defined as 101325 Pa (IUPAC recommends the value 100000 Pa, but prior to 1982 the value 101325 Pa (= 1 atm) was usually used). Because pressure is commonly measured by its ability to displace a column of liquid in a manometer, pressures are often expressed as a depth of a particular fluid (e.g., centimetres of water, millimetres of mercury or inches of mercury). The most common choices are mercury (Hg) and water; water is nontoxic and readily available, while mercury's high density allows a shorter column (and so a smaller manometer) to be used to measure a given pressure. The pressure exerted by a column of liquid of height h and density ρ is given by the hydrostatic pressure equation p = ρgh, where g is the gravitational acceleration. Fluid density and local gravity can vary from one reading to another depending on local factors, so the height of a fluid column does not define pressure precisely.

=== Displacement === The UN reported that more than 93,000 Syrians have been displaced in Sweida, the Daraa governorate, and rural Damascus due to the violence, said UN spokesperson Stéphane Dujarric.

== Definition, regulatory aspects == The International Council on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use, a 2015 Swiss NGO of pharmaceutical companies and others, defined a contract research organization (CRO), specifically pertaining to clinical trials services as: "A person or an organization (commercial, academic, or other) contracted by the sponsor to perform one or more of a sponsor's trial-related duties and functions." It further details the sponsor's responsibilities in its good clinical practice guidelines:

Sources: en.wikipedia.org

Further detail

CPA is widely used as an antiandrogen and progestogen in feminizing hormone therapy for transgender individuals. It has been historically used orally at a dosage of 10 to 100 mg/day and by intramuscular injection at a dosage of 300 mg once every 4 weeks. Many transgender individuals seeking feminizing hormone therapy have breast growth as one of the goals for undergoing feminizing hormone therapy, making this particular side effect of CPA generally viewed as a beneficial outcome rather than an issue. Studies have found that 10, 25, 50, and 100 mg/day CPA in combination with estrogen all result in equivalent and full testosterone suppression in transgender women. In light of risks of CPA such as fatigue, blood clots, benign brain tumors, and liver damage, the use of lower dosages of CPA may help to minimize such risks. As a result, a CPA dosage of 10 mg/day and no greater is now recommended by the World Professional Association for Transgender Health (WPATH) Standards of Care for the Health of Transgender and Gender Diverse People, Version 8 (SOC8). CPA has an advantage over spironolactone as an antiandrogen in transgender people, as the combination of estrogen and CPA consistently suppresses testosterone levels into the normal female range whereas estrogen with spironolactone does not. Spironolactone is the most widely used antiandrogen in transgender women in the United States, whereas CPA is widely used in Europe and throughout the rest of the world.

Impaired wound healing and thrombocytopenia are possible side effects of sirolimus; therefore, some transplant centers prefer not to use it immediately after the transplant operation, but instead administer it only after a period of weeks or months. Its optimal role in immunosuppression has not yet been determined, and it remains the subject of a number of ongoing clinical trials.

The water of vitriol and sulphur which is used to irrigate the drugs: yellow vitriol three parts, yellow sulphur one part, grind them and distil them in the manner of rose-water. A recipe for the preparation of sulfuric acid is mentioned in Risālat Jaʿfar al-Sādiq fī ʿilm al-ṣanʿa, an Arabic treatise falsely attributed to the Shi'i Imam Ja'far al-Sadiq (died 765). Julius Ruska dated this treatise to the 13th century, but according to Ahmad Y. al-Hassan it likely dates from an earlier period:

=== Legality of South West Africa, 1946–1960 === After World War II, Jan Smuts headed the South African delegation to the United Nations Conference on International Organization. As a result of this conference, the League of Nations was formally superseded by the United Nations (UN) and former League mandates by a trusteeship system. Article 77 of the United Nations Charter stated that UN trusteeship "shall apply...to territories now held under mandate"; furthermore, it would "be a matter of subsequent agreement as to which territories in the foregoing territories will be brought under the trusteeship system and under what terms". Smuts was suspicious of the proposed trusteeship, largely because of the vague terminology in Article 77. Heaton Nicholls, the South African high commissioner in the United Kingdom and a member of the Smuts delegation to the UN, addressed the newly formed UN General Assembly on 17 January 1946. Nicholls stated that the legal uncertainty of South West Africa's situation was retarding development and discouraging foreign investment; however, self-determination for the time being was impossible since the territory was too undeveloped and underpopulated to function as a strong independent state. In the second part of the first session of the General Assembly, the floor was handed to Smuts, who declared that the mandate was essentially a part of the South African territory and people.

Sources: en.wikipedia.org

Background from the literature

NMR quantum computing uses the spin states of nuclei within molecules as qubits. NMR differs from other implementations of quantum computers in that it uses an ensemble of systems; in this case, molecules.

Sex hormones, which influence sex differences and support puberty and reproduction. These hormones include androgens, estrogens, and progestogens. Corticosteroids, including most synthetic steroid drugs, with natural product classes the glucocorticoids (which regulate many aspects of metabolism and immune function) and the mineralocorticoids (which help maintain blood volume and control renal excretion of electrolytes) Anabolic steroids, natural and synthetic, which interact with androgen receptors to increase muscle and bone synthesis. In popular use, the term "steroids" often refers to anabolic steroids.

The first humans to form substantial settlements in what is now Knoxville arrived during the Woodland period (c. 1000 B.C. – 1000 A.D). Knoxville's two most prominent prehistoric structures are Late Woodland period burial mounds, one located along Cherokee Boulevard in Sequoyah Hills, and the other located along Joe Johnson Drive on the University of Tennessee campus. Substantial Mississippian period (c. 1100–1600 A.D.) village sites have been found at Post Oak Island (along the river near the Knox-Blount line), and at Bussell Island (near Lenoir City). The Spanish expedition of Hernando de Soto is believed to have traveled down the French Broad Valley and visited the Bussell Island village in 1540 en route to the Mississippi River. A follow-up expedition led by Juan Pardo may have visited village sites in the Little Tennessee Valley in 1567. The records of these two expeditions suggest the area was part of a Muskogean chiefdom known as Chiaha, which was subject to the Coosa chiefdom further to the south. By the 18th century, the Cherokee had become the dominant tribe in the East Tennessee region, although they were consistently at war with the Creeks and Shawnee. The Cherokee people called the Knoxville area kuwanda'talun'yi, which means "Mulberry Place." Most Cherokee habitation in the area was concentrated in the Overhill settlements along the Little Tennessee River, southwest of Knoxville.

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.

Is cardarine legal to buy?

Legal status varies by country, but cardarine is not approved as a medicine in major jurisdictions. It is often sold as a research chemical, a category that may not be lawful for human use. Buyers should check local laws and product labels carefully.

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