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Identity And Regulatory Status — Deep Dive

By Editorial Desk · published 2025-11-04 · last reviewed 2025-12-08 · Guide

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

This page was last updated on 2025-12-08 and is reviewed periodically as new material appears.

Identity and Regulatory Status

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.

Clinical development stopped after rodent studies showed tumors at multiple sites. Whether those findings predict human cancer risk remains an open question, but they led sponsors to discontinue programs. Human safety data are limited to small, short-term studies that were not designed to assess cancer risk. Reported effects in those studies included changes in blood lipids, but the evidence is insufficient for medical use. Long-term consequences of nonmedical use are not well characterized. Questions about dose, duration, and individual susceptibility remain unresolved.

Identity and Pharmacological Classification

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.

Cardarine at a glance

PropertyValueNotes
Common synonymsGW501516; GW-1516; endurobolGW501516 is the research code
Drug classPPARδ agonistNot a selective androgen receptor modulator
Molecular formulaC21H18F3NO3S2Established chemical formula
Molar mass453.5 g/molCalculated from the formula
Regulatory statusProhibited in sport; not approved as medicineStatus varies by country

Cardarine Identity and Mechanism

At the molecular level, GW501516 binds and activates PPARδ, a nuclear receptor that regulates transcription. Activation shifts expression of genes involved in fatty acid oxidation, energy expenditure, and lipid transport in skeletal muscle and liver. Animal studies report increased endurance and altered lipid profiles after exposure. Human data are limited to small trials and do not establish long-term safety or efficacy. PPARδ also has roles in cell proliferation, so the relationship between activation and cancer risk remains an open question.

Published literature on cardarine includes in vitro assays, rodent experiments, and a small number of human studies. Reports describe effects on exercise capacity and lipid metabolism in animals, while human evidence is sparse. Many online descriptions present the compound as a proven endurance aid, a claim not supported by regulatory approval or large clinical trials. Analytical studies focus on identifying the parent compound and its metabolites in biological samples. Important uncertainties include species differences, dose-response relationships, and the relevance of rodent tumor findings to humans.

Cardarine is the common name for GW501516, a synthetic compound studied as a peroxisome proliferator-activated receptor delta agonist. Researchers developed it to explore treatments for lipid disorders and metabolic conditions. It is not an approved medicine in any country. Early clinical work examined changes in HDL cholesterol and triglycerides, but development was discontinued after animal studies raised concerns about cancer. The compound remains available as a research chemical and appears in discussions of performance enhancement.

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Background and Research Context

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.

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.

Supporting material

=== Fish === Lungs are found in three groups of fish; the coelacanths, the bichirs and the lungfish. Like in tetrapods, but unlike fish with swim bladder, the opening is at the ventral side of the oesophagus. The coelacanth has a nonfunctional and unpaired vestigial lung surrounded by a fatty organ. Bichirs, the only group of ray-finned fish with lungs, have a pair which are hollow unchambered sacs, where the gas-exchange occurs on very flat folds that increase their inner surface area. The lungs of lungfish show more resemblance to tetrapod lungs. There is an elaborate network of parenchymal septa, dividing them into numerous respiration chambers. In the Australian lungfish, there is only a single lung, albeit divided into two lobes. Other lungfish, however, have traditionally been considered having two lungs, but newer research defines paired lungs as bilateral lung buds that arise simultaneously and are both connected directly to the foregut, which is only seen in tetrapods. In all lungfish, including the Australian, the lungs are located in the upper dorsal part of the body, with the connecting duct curving around and above the oesophagus. The blood supply also twists around the oesophagus, suggesting that the lungs originally evolved in the ventral part of the body, as in other vertebrates.

In chemistry, matter is defined as anything that has rest mass and volume (it takes up space) and is made up of particles. The particles that make up matter have rest mass as well – not all particles have rest mass, such as the photon. Matter can be a pure chemical substance or a mixture of substances.

Radiopharmacology is radiochemistry applied to medicine and thus the pharmacology of radiopharmaceuticals (medicinal radiocompounds, that is, pharmaceutical drugs that are radioactive). Radiopharmaceuticals are used in the field of nuclear medicine as radioactive tracers in medical imaging and in therapy for many diseases (for example, brachytherapy). Many radiopharmaceuticals use technetium-99m (Tc-99m) which has many useful properties as a gamma-emitting tracer nuclide. In the book Technetium a total of 31 different radiopharmaceuticals based on Tc-99m are listed for imaging and functional studies of the brain, myocardium, thyroid, lungs, liver, gallbladder, kidneys, skeleton, blood and tumors. The term radioisotope, which in its general sense refers to any radioactive isotope (radionuclide), has historically been used to refer to all radiopharmaceuticals, and this usage remains common. Technically, however, many radiopharmaceuticals incorporate a radioactive tracer atom into a larger pharmaceutically-active molecule, which is localized in the body, after which the radionuclide tracer atom allows it to be easily detected with a gamma camera or similar gamma imaging device. An example is fludeoxyglucose in which fluorine-18 is incorporated into deoxyglucose. Some radioisotopes (for example gallium-67, gallium-68, and radioiodine) are used directly as soluble ionic salts, without further modification. This use relies on the chemical and biological properties of the radioisotope itself, to localize it within the body.

Sources: en.wikipedia.org

Supporting material

=== Selegiline inhibition of cytochrome P450 enzymes === Selegiline has been reported to inhibit several cytochrome P450 enzymes, including CYP2D6, CYP3A4/5, CYP2C19, CYP2B6, and CYP2A6. It is a mechanism-based inhibitor (suicide inhibitor) of CYP2B6 and has been said to "potently" or "strongly" inhibit this enzyme in vitro. It may inhibit the metabolism of bupropion, a major CYP2B6 substrate, into its active metabolite hydroxybupropion. However, a study predicted that inhibition of CYP2B6 by selegiline would non-significantly affect exposure to bupropion. Selegiline has not been listed or described as a clinically significant CYP2B6 inhibitor by the Food and Drug Administration (FDA) as of 2023. One small study observing three patients found that selegiline was safe and well-tolerated in combination with bupropion. In addition to CYP2B6 and other cytochrome P450 enzymes, selegiline is a potent mechanism-based inhibitor of CYP2A6 and may increase exposure to nicotine (a major CYP2A6 substrate). By inhibiting cytochrome P450 enzymes like CYP2B6 and CYP1A2, selegiline may inhibit its own metabolism and thereby interact with itself.

The standard enthalpy change can be determined by calorimetry or by using the van 't Hoff equation, though the calorimetric method is preferable. When both the standard enthalpy change and acid dissociation constant have been determined, the standard entropy change is easily calculated from the equation above. In the following table, the entropy terms are calculated from the experimental values of pKa and ΔH⊖. The data were critically selected and refer to 25 °C and zero ionic strength, in water.

== Signs and symptoms == Arthritis entails inflammation within the joint, and presents as swelling, pain, stiffness and restricted joint movement. Symptoms of JIA vary. This is because JIA has several subtypes, which differ according to the number of affected joints, severity of disease, age of onset, prognosis and presence or absence of inflammation in other parts of the body. The key clinical feature in JIA is persistent swelling of the affected joints. Any joint can be affected, but large joints such as the knee and ankle are most commonly involved. Involvement of small joints of the hands and feet is more likely when many joints are affected ('polyarthritis'). Swollen joints may also feel warmer to touch. Swelling may be difficult to detect clinically, especially for joints such as those of the spine, sacroiliac joints, shoulder, hip, and jaw. Joint pain is an important symptom, although some children experience minimal or no pain with their arthritis. In these children, the first sign of arthritis may be limping, especially in the morning. Swelling and pain usually result in limited movement of the affected joints, for example a knee held bent causing a limp, or being unable to make a full fist. Limited movement may reduce a child's ability to fully participate in activities and undertake usual tasks such as those used for self-care. In some JIA subtypes, more non-specific symptoms of being unwell may be present, such as lethargy, fatigue and poor appetite. Children with systemic JIA usually present with fever and a classic rash and may become quite ill.

Nitrogen has two stable isotopes: 14N and 15N. The first is much more common, making up 99.634% of natural nitrogen, and the second (which is slightly heavier) makes up the remaining 0.366%. This leads to an atomic weight of around 14.007 u. Both of these stable isotopes are produced in the CNO cycle in stars, but 14N is more common as its proton capture is the rate-limiting step. 14N is one of the five stable odd–odd nuclides (a nuclide having an odd number of protons and neutrons); the other four are 2H, 6Li, 10B, and 180mTa. The relative abundance of 14N and 15N is practically constant in the atmosphere but can vary elsewhere, due to natural isotopic fractionation from biological redox reactions and the evaporation of natural ammonia or nitric acid. Biologically mediated reactions (e.g., assimilation, nitrification, and denitrification) strongly control nitrogen dynamics in the soil. These reactions typically result in 15N enrichment of the substrate and depletion of the product. The heavy isotope 15N was first discovered by S. M. Naudé in 1929, and soon after heavy isotopes of the neighbouring elements oxygen and carbon were discovered. It presents one of the lowest thermal neutron capture cross-sections of all isotopes. It is frequently used in nuclear magnetic resonance (NMR) spectroscopy to determine the structures of nitrogen-containing molecules, due to its fractional nuclear spin of one-half, which offers advantages for NMR such as narrower line width.

Sources: en.wikipedia.org

Notes from published material

From the perspective of ground forces, apart from the occasional "oil rain" experienced by troops very close to spewing wells, one of the more commonly experienced effects of the oil field fires were the ensuing smoke plumes which rose into the atmosphere and then precipitated or fell out of the air via dry deposition and by rain. The pillar-like plumes frequently broadened and joined up with other smoke plumes at higher altitudes, producing a cloudy grey overcast effect, as only about 10% of all the fires corresponding with those that originated from "oil lakes" produced pure black soot filled plumes, 25% of the fires emitted white to grey plumes, while the remainder emitted plumes with colors between grey and black. For example, one Gulf War veteran stated:

== Epidemiology == Hypothyroidism is the most frequent endocrine disorder. Worldwide about one billion people are estimated to be iodine deficient; however, it is unknown how often this results in hypothyroidism. In large population-based studies in Western countries with sufficient dietary iodine, 0.3–0.4% of the population have overt hypothyroidism. A larger proportion, 4.3–8.5%, have subclinical hypothyroidism. Undiagnosed hypothyroidism is estimated to affect about 4–7% of community-derived populations in the US and Europe. Of people with subclinical hypothyroidism, 80% have a TSH level below the 10 mIU/L mark regarded as the threshold for treatment. Children with subclinical hypothyroidism often return to normal thyroid function, and a small proportion develops overt hypothyroidism (as predicted by evolving antibody and TSH levels, the presence of celiac disease, and the presence of a goiter). Women are more likely to develop hypothyroidism than men. In population-based studies, women were seven times more likely than men to have TSH levels above 10 mU/L. 2–4% of people with subclinical hypothyroidism will progress to overt hypothyroidism each year. The risk is higher in those with antibodies against thyroid peroxidase. Subclinical hypothyroidism is estimated to affect approximately 2% of children; in adults, subclinical hypothyroidism is more common in the elderly, and in White people. There is a much higher rate of thyroid disorders, the most common of which is hypothyroidism, in individuals with Down syndrome and Turner syndrome.

The galactic year, GY, is the time it takes the Solar System to revolve once around the galactic core, approximately 250 million years (megaannum or "Ma"). It is a convenient unit for long-term measurements. For example, oceans appeared on Earth after 4 GY, life is detectable at 5 GY, and multicellular organisms first appeared at 15 GY. The age of the Earth is estimated at 20 GY. This use of GY is not to be confused with Gyr for gigayear or Gy for Gray (unit).

Sources: en.wikipedia.org

Frequently asked questions

Is cardarine a SARM?

No. Cardarine is GW501516, a PPARδ agonist, while SARMs act on androgen receptors. The two classes are often grouped in informal discussions despite different mechanisms.

Is cardarine approved for human use?

No. It has no approved medical indication in any country. Regulatory agencies have not cleared it for treatment or prevention of any condition.

Why was its development discontinued?

Early clinical work stopped after rodent carcinogenicity findings. Those animal results raised concerns about long-term human risk, although direct human evidence is lacking. The human relevance of the tumors remains an open scientific question.

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.

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