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Background And Regulatory Status — Common Mistakes

By Editorial Desk · published 2025-09-25 · last reviewed 2025-10-13 · News

If you have been reading about PPARδ 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 2025-10-13. Numbers and descriptions here follow the published literature rather than marketing material.

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.

Mechanism and Safety Research

Literature on cardarine often separates receptor pharmacology from toxicology. Mechanistic papers describe PPARδ activation and gene expression changes, while safety assessments focus on carcinogenicity and species differences. Questions remain about whether rodent tumors arise through PPARδ-dependent or off-target mechanisms. Another open area is how human metabolism and exposure compare with those in animal studies. Analytical methods such as liquid chromatography–mass spectrometry are used to confirm identity in biological and product samples.

GW501516 acts as an agonist at the peroxisome proliferator-activated receptor delta, a nuclear receptor that regulates gene expression. Activation shifts transcription toward genes involved in fatty acid uptake, oxidation, and energy expenditure. The compound does not bind the androgen receptor and therefore differs from anabolic steroids and SARMs. In rodent models, this metabolic shift has been linked to increased running endurance and reduced fat accumulation. The exact downstream pathways in humans remain incompletely 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

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.

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Identity and Regulatory Status

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.

Cardarine is a common name for GW501516, an investigational compound developed in the 1990s for metabolic conditions. It acts as an agonist at peroxisome proliferator-activated receptor delta, a nuclear receptor involved in lipid and energy metabolism. The compound is frequently mislabeled as a selective androgen receptor modulator, or SARM, but its molecular target is different. GW501516 reached early clinical testing before development was discontinued. It has no approved therapeutic use in any country. The name cardarine is not a formal international nonproprietary name.

Mechanism and Detection

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.

GW501516 acts as a ligand for PPAR delta, a nuclear receptor that regulates transcription of genes involved in fatty acid oxidation and energy use. Activation of this receptor in skeletal muscle shifts metabolism toward fat burning in animal models. The compound does not burn fat directly; it changes gene expression over hours to days. Researchers study it to understand metabolic flexibility and exercise adaptation. Effects observed in rodents are not automatically expected in humans.

Identity and Pharmacological Mechanism

The compound is typically described as a laboratory compound rather than a therapeutic product. Published reports have explored its role in lipid disorders, insulin sensitivity, and exercise metabolism, yet no major drug regulator has approved it for medical use. Commercial samples sold under the cardarine name may vary in purity and identity. Analytical confirmation is therefore necessary when the material is discussed in scientific or regulatory contexts. Its classification as a prohibited substance in sport further shapes how it is studied and reported.

Cardarine is a common name for GW501516, a synthetic compound studied for its effects on lipid and glucose metabolism. It functions as an agonist at peroxisome proliferator-activated receptor delta, or PPARδ, a nuclear receptor that influences gene expression. The molecule is not a steroid, nor is it a selective androgen receptor modulator. It is also known in research and sports literature as GW-501516 and endurobol. Early laboratory work examined its metabolic activity in cell cultures and animal models.

Activation of PPARδ changes transcription of genes involved in fatty acid transport, mitochondrial function, and skeletal muscle fuel preference. In rodent studies, pharmacological PPARδ activation was associated with increased endurance and altered body composition. These findings generated interest in performance enhancement, but species differences and study designs limit direct extrapolation to humans. Small human trials were conducted in the 2000s and later discontinued. The extent to which cardarine produces similar metabolic or performance effects in people remains an open question.

Background from the literature

It is considered to be one of several antidepressants with a greater risk of hepatotoxicity. The prescribing information warns about bupropion triggering an angle-closure glaucoma attack. On the other hand, bupropion may decrease the risk of development of open angle glaucoma. Bupropion has rarely been associated with instances of Stevens–Johnson syndrome. Bupropion use by mothers in the first trimester of pregnancy is associated with a 23% increase in the odds of congenital heart defects in their children.

The country has networks of cooperatives at the local, regional, state and national levels that assist in agricultural marketing. The commodities that are mostly handled are food grains, jute, cotton, sugar, milk, fruit and nuts. Support by the state government led to more than 25,000 cooperatives being set up by 1990s in Maharashtra.

=== Graphene superlattices === Periodically stacked graphene and its insulating isomorph provide a fascinating structural element in implementing highly functional superlattices at the atomic scale, which offers possibilities for designing nanoelectronic and photonic devices. Various types of superlattices can be obtained by stacking graphene and its related forms. The energy band in layer-stacked superlattices is found to be more sensitive to the barrier width than that in conventional III–V semiconductor superlattices. When adding more than one atomic layer to the barrier in each period, the coupling of electronic wavefunctions in neighboring potential wells can be significantly reduced, which leads to the degeneration of continuous subbands into quantized energy levels. When varying the well width, the energy levels in the potential wells along the L-M direction behave distinctly from those along the K-H direction. A superlattice corresponds to a periodic or quasi-periodic arrangement of different materials and can be described by a superlattice period which confers a new translational symmetry to the system, impacting their phonon dispersions and subsequently their thermal transport properties. Recently, uniform monolayer graphene-hBN structures have been successfully synthesized via lithography patterning coupled with chemical vapor deposition (CVD). Furthermore, superlattices of graphene-HBN are ideal model systems for the realization and understanding of coherent (wave-like) and incoherent (particle-like) phonon thermal transport.

The 100K Wellness Project was a 10-month Framingham-style longitudinal study, organized by Leroy Hood. The pilot phase took place between March and December 2014. Participants submitted integrated data from whole-genome sequencing, gut microbiome, clinical laboratory tests and quantified self measures to provide actionable results for health coaching. It showed actionable opportunities in all participants, and participants followed actionable guidelines about 70 percent of the time. It later would transition into the wellness startup Arivale.

== Structure and characteristics == Although many (>100) forms of pyoverdine have been isolated and studied, they all have certain characteristics in common. Each pyoverdine molecule has three parts: a dihydroxyquinoline core, a 6-14 amino acid peptide that varies among strains, and a side chain (usually composed of a 4-5 carbon α-ketoacid from the Krebs/citric acid cycle). The core of pyoverdine is responsible for several of its properties, including its well-known yellowish color and fluorescence.

Sources: en.wikipedia.org

Further detail

Tianeptine/naloxone (developmental code names TNX-601, TNX-601-CR, TNX-601-ER), or naloxone/tianeptine, is an extended-release combination of tianeptine, an atypical μ-opioid receptor agonist, and naloxone, an orally inactive μ-opioid receptor antagonist, which was under development for the treatment of major depressive disorder, post-traumatic stress disorder (PTSD), and neurocognitive dysfunction associated with corticosteroid use but was never marketed. Whereas tianeptine is marketed widely throughout Europe, Asia, and Latin America but is not available in the United States or the United Kingdom, tianeptine/naloxone was under development for registration in the United States and other countries. In addition, whereas tianeptine has a short duration of action and requires administration three times per day, tianeptine/naloxone was developed as an extended-release formulation with enhanced pharmacokinetics suitable for once-daily administration. The combination formulation employs tianeptine as the oxalate salt, which is said to have improved physicochemical properties for use in the extended-release formulation compared to the amorphous tianeptine sodium that is used in immediate-release tianeptine-only formulations. Naloxone is used in misuse-resistant oral drug formulations as it is inactive if taken orally but becomes active if oral tablets are crushed and administered parenterally, such as by injection.

However, selegiline can strongly potentiate the reinforcing effects of exogenous β-phenethylamine by inhibiting its MAO-B-mediated metabolism. Misuse of the combination of selegiline and β-phenethylamine has been reported.

Promising results of health and medical research are reported: phase 2-trialed GLP-1 receptor agonist diabetes 2 drug lixisenatide against (early) Parkinson's disease motor disability (3 April). Hazard research is published: a study assesses the global extent of PFAS contamination of surface waters and groundwaters, finding many samples exceed PFAS drinking water guidance values and a "need to better understand the use, fate and impacts of anthropogenic chemicals" (8 April), a study estimates how much inorganic carbon soils store globally and projects that they would emit 23 billion tons over the next 30 years in a business-as-usual scenario (11 April), a study of satellite data suggests because of city subsidence and sea-level rise, by 2120, 22 to 26% of China's coastal lands will be below sea level, hosting 9 to 11% of the coastal population (18 April), a study suggests vitamin D deficiency may be a determinant of cancer immunity and immunotherapy success (25 April), and researchers report H5N1 bird flu was found in raw milk (29 April).

== V == Vagus nerve Cranial nerve X, responsible for parasympathetic control of the heart, lungs, and digestive tract. It also conveys sensory information from the viscera to the brainstem. Vasopressin Also known as antidiuretic hormone (ADH), it regulates water balance and blood pressure. In the brain, vasopressin influences social behavior and memory. Ventral A directional term meaning "toward the front" in the spinal cord or "toward the bottom" in the brain. Opposite of dorsal. Ventral horn The anterior portion of the spinal cord’s gray matter, containing motor neurons that project to skeletal muscles. Ventral stream A visual processing pathway ("what" pathway) that travels from the occipital lobe to the temporal lobe and is involved in object recognition and form representation. Ventral tegmental area (VTA) A midbrain structure containing dopaminergic neurons that project to the nucleus accumbens and prefrontal cortex, central to reward and motivation. Ventricles A set of interconnected cavities in the brain filled with cerebrospinal fluid (CSF), which cushions the brain and maintains intracranial pressure. Vestibular system The sensory system that contributes to balance, spatial orientation, and coordination of head and eye movements. Includes the semicircular canals and otolith organs. Vestibulo-ocular reflex (VOR) A reflex that stabilizes vision by producing eye movements in the opposite direction of head movement, allowing steady gaze.

Sources: en.wikipedia.org

Supporting material

The pores permitted cationss transport after short oxidation periods, consistent with electrostatic repulsion from negatively charged functional groups at pore edges. After longer oxidation periods, sheets were permeable to salt but not larger organic molecules. In 2015, a team fabricated a graphene oxide home water purification system resembling a "tea bag" that, over the course of a day, can remove 95% of heavy metals when immersed in a drinking-water pot. A composite comprising small NiFe2O4 ferrimagnetic nanoparticles and partially reduced graphene oxide functionalized with nitrogen atoms was successfully used to remove Cr(III) ions from water. The advantage of this nanocomposite is that it can be magnetically separated from water. One project layered carbon atoms in a honeycomb structure, forming a hexagon-shaped crystal that measured about 0.1 millimeters in width and length, with subnanometer holes. Later work increased the membrane size to on the order of several millimeters. Graphene attached to a polycarbonate support structure was initially effective at removing salt. However, defects formed in the graphene. Filling larger defects with nylon and small defects with hafnium metal, followed by a layer of oxide, restored the filtration effect. In 2016, engineers developed graphene-based films powered by the sun that can filter dirty/salty water. Bacteria were used to produce a material consisting of two nanocellulose layers. The lower layer contains pristine cellulose, while the top layer contains cellulose and graphene oxide, which absorb sunlight and produce heat.

Calpainopathy is the most common type of autosomal recessive limb-girdle muscular dystrophy (LGMD). It preferentially affects the muscles of the hip girdle and shoulder girdle. No disease modifying pharmaceuticals have been developed as of 2019, although physical therapy, lifestyle modification, and orthopedic surgery can address symptoms.

The tapetum lucidum (Latin for 'bright tapestry, coverlet'; tə-PEE-təm LOO-sih-dəm; pl.: tapeta lucida) is a layer of tissue in the eye of many vertebrates and some other animals. Lying immediately behind the retina, it is a retroreflector. It reflects visible light back through the retina, increasing the light available to the photoreceptors (although slightly blurring the image). The tapetum lucidum contributes to the superior night vision of some animals. Many of these animals are nocturnal, especially carnivores, while others are deep-sea animals. Similar adaptations occur in some species of spiders. Haplorhine primates, including humans, are diurnal and lack a tapetum lucidum.

The Aviation Safety Reporting System (ASRS) collects voluntarily submitted aviation safety incident/situation reports from pilots, controllers and others. The ASRS uses reports to identify system deficiencies, issue alert messages, and produce two publications, CALLBACK, and ASRS Directline. The collected information is made available to the public, and is used by the FAA, NASA and other organizations working in research and flight safety.

Due to actinium's intense radioactivity, only a limited number of actinium compounds are known. These include: AcF3, AcCl3, AcBr3, AcOF, AcOCl, AcOBr, Ac2S3, Ac2O3, AcPO4 and Ac(NO3)3. They all contain actinium in the oxidation state +3. In particular, the lattice constants of the analogous lanthanum and actinium compounds differ by only a few percent.

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.

What is the main molecular target of cardarine?

It targets PPARδ, a nuclear receptor involved in lipid and energy metabolism. It does not act primarily on androgen receptors. This distinction separates it from SARMs.

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