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Background And Regulatory Status — Background and Details

By Editorial Desk · published 2025-09-10 · last reviewed 2025-09-28 · Wiki

The short version of GW501516 fits in a sentence. The long version — which is the one that helps — is below.

This page was last updated on 2025-09-28 and is reviewed periodically as new material appears.

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.

Regulatory Status and Detection Context

A persistent misconception is that cardarine is a fat-burning drug or a safe alternative to anabolic steroids. No approved therapeutic product exists, and human safety data are limited. The tumor findings in rodents remain a central concern in scientific reviews. Products sold online may contain inaccurate labels, impurities, or different compounds entirely, which complicates any assessment of effects. Independent testing of such products has reported frequent mislabeling. For these reasons, discussions in the literature emphasize risks and unknowns rather than benefits.

Cardarine is not approved for human therapeutic use in any major jurisdiction. It appears on the World Anti-Doping Agency Prohibited List as a PPARδ agonist within the hormone and metabolic modulators category. Sports organizations test for it because it has been detected in athlete samples and seized products. Regulatory actions against marketed research chemical versions have occurred in several countries, though enforcement varies. Availability through unregulated channels complicates oversight.

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

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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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.

Background from the literature

== Physiology == A. parasiticus produces aflatoxins B1, B2, G1, and G2, named for the colours emitted under UV light on thin-layer chromatography plates—either blue and green. The numbers refer to the type of compound with 1 being major and 2 being minor. These aflatoxins are carcinogenic mycotoxins which have detrimental effects to humans and livestock. A. parasiticus also has the ability to produce kojic acid, aspergillic acid, nitropropionic acid and aspertoxin as secondary antimicrobial metabolites in response to different environments, all of which can be useful in identification. A. parasiticus also differs in sclerotia quantity number, volume, and shape. This fungus can be reliably identified using molecular methods. A. parasiticus produces aflatoxins at higher concentrations than A. flavus in temperatures ranging from 12–42 °C (54–108 °F) with pH ranging from 3 to greater than 8. Light exposure, oxidative growth conditions, fungal volatiles and nutrient availability (sugars and zinc) affect the production of these toxins. Greater zinc availability increases aflatoxin output. Environmental stress caused by drought and/or high temperatures during the latter part of the growing season of crops increases the likelihood of fungal growth. The aflatoxins produced by A. parasiticus are hazardous under normal food handling conditions and are especially stable when absorbed by starch or protein on the surfaces of seeds.

Charles Catania (1957), psychologist, professor at University of Maryland, Baltimore County Sheldon Saul Hendler (1957), scientist, physician, and musician Ralph Feigin (1958), pediatrician; former president and CEO of Baylor College of Medicine and physician-in-chief of Texas Children's Hospital Roald Hoffman (1958), winner of the Nobel Prize in Chemistry Norbert Hirschhorn (1958), public health physician and developed the Oral rehydration therapy Gerald T. Keusch (1958), professor of the Boston University School of Public Health and director of the John E. Fogarty International Center at the National Institutes of Health Harlan Lane (1958), professor of psychology at Northeastern University Hans Christian von Baeyer (1958), physicist at the College of William & Mary Joseph L. Fleiss (1959), professor of biostatistics at the Columbia University Mailman School of Public Health Allan Franklin (1959), physicist, historian of science at University of Colorado Boulder Paul B. Kantor (1959), information scientist, professor at Rutgers University Michael Lesch (1960), physician and medical educator who identified the Lesch–Nyhan syndrome Ira Black (1961), physician and neuroscientist, advocate of Stem cell research; former president of Society for Neuroscience Kenneth C.

SHIELD Illinois was the SHIELD Deployment Unit of the University of Illinois System charged with administering the covidSHIELD SARS-CoV-2 assay throughout the State of Illinois. SHIELD Illinois performed over 7.2 million SARS-CoV-2 assays during its initial program. This represented 12% of all SARS-CoV-2 tests in Illinois and more tests than 24 entire states.

Cleavage of proteins is an irreversible post-translational modification carried out by enzymes known as proteases. These proteases are often highly specific and cause hydrolysis of a limited number of peptide bonds within the target protein. The resulting shortened protein has an altered polypeptide chain with different amino acids at the start and end of the chain. This post-translational modification often alters the protein's function; the protein can be inactivated or activated by the cleavage and can display new biological activities.

Atomoxetine, sold under the brand name Strattera, is a selective norepinephrine reuptake inhibitor (SNRI) medication used to treat attention deficit hyperactivity disorder (ADHD) and, to a lesser extent, cognitive disengagement syndrome (CDS). It may be used alone or along with psychostimulant medication. It enhances the executive functions of self-motivation, sustained attention, inhibition, working memory, reaction time, and emotional self-regulation. Use of atomoxetine is only recommended for those who are at least six years old. It is taken orally. The effectiveness of atomoxetine is comparable to the commonly prescribed stimulant medication methylphenidate. Common side effects of atomoxetine include abdominal pain, decreased appetite, nausea, feeling tired, and dizziness. Serious side effects may include angioedema, liver problems, stroke, psychosis, heart problems, suicide, and aggression. There is a lack of data regarding its safety during pregnancy; as of 2019, its safety during pregnancy and for use during breastfeeding is not certain. It was approved for medical use in the United States in 2002. In 2023, it was the 161st most commonly prescribed medication in the United States, with more than 3 million prescriptions.

Sources: en.wikipedia.org

Reference notes

== External links == "Datopotamab Deruxtecan (Code C151967)". NCI Thesaurus. Clinical trial number NCT05104866 for "A Phase-3, Open-Label, Randomized Study of Dato-DXd Versus Investigator's Choice of Chemotherapy (ICC) in Participants With Inoperable or Metastatic HR-Positive, HER2-Negative Breast Cancer Who Have Been Treated With One or Two Prior Lines of Systemic Chemotherapy (TROPION-Breast01)" at ClinicalTrials.gov Clinical trial number NCT04484142 for "Study of DS-1062a in Advanced or Metastatic Non-small Cell Lung Cancer With Actionable Genomic Alterations (TROPION-Lung05)" at ClinicalTrials.gov Clinical trial number NCT04656652 for "Study of DS-1062a Versus Docetaxel in Previously Treated Advanced or Metastatic Non-small Cell Lung Cancer With or Without Actionable Genomic Alterations (TROPION-LUNG01)" at ClinicalTrials.gov Clinical trial number NCT05374512 for "A Study of Dato-DXd Versus Investigator's Choice Chemotherapy in Patients With Locally Recurrent Inoperable or Metastatic Triple-negative Breast Cancer, Who Are Not Candidates for PD-1/PD-L1 Inhibitor Therapy (TROPION-Breast02)" at ClinicalTrials.gov

Mechanism The reaction of tetrazines with trans-cyclooctenes is a highly specific biorthogonal reaction recognized for its rapid reaction rates, compatibility with physiological environments, and its metal-free characteristics. Commonly referred to as tetrazine ligation, the reaction was initially reported in 2008 and has since become a widely adopted bioorthogonal chemistry tool in both in vivo and in vitro studies. The tetrazine ligation is a specific type of inverse electron demand Diels-Alder (shown in the second mechanism in Figure 13) (iEDDA) [4+2] cycloaddition. The mechanism involves an electron-deficient tetrazine, typically a substituted 3,6-diaryl-s-tetrazine functioning as the diene and an electron-rich strained alkene, typically a trans-cyclooctene (TCO) compound, serving as the dienophile (shown in Figure 14). Trans-cyclooctenes have a high strain energy of 17.9 kcal/mol due to their non-planar double bond, making it very reactive and a strong dienophile. Following the initial iEDDA, a retro-Diels-Alder (shown in the last mechanism in Figure 13) reaction occurs, resulting in the expulsion of nitrogen gas (N2), driving the reaction forward. This promotes the irreversible nature of the reaction, which enhances its suitability for bio-labeling applications. This reaction has fast reactivity at low concentrations, with second order rate constants ranging from 1–106 M−1 s−1 depending on the specific tetrazine and TCO pair.

Since 2015, the city of Le Havre is divided over six Cantons, some of which also cover neighbouring communes. For the parliamentary elections, Le Havre spans two constituencies: the seventh (former cantons I, V, VI, and VII) and the eighth (former cantons II, III, IV, VIII, IX).

=== Transforming growth factor β (TGF-β) === In normal conditions, alveolar macrophages adhere closely to alveolar epithelial cells, thus inducing the expression of the αvβ6 integrin. Integrins are dimeric cell-surface receptors composed of alpha and beta subunits, which activates TGF-β. TGF-β is a multifunctional cytokine that modulates a variety of biological processes such as cell growth, apoptosis, extracellular matrix synthesis, inflammation, and immune responses. TGF-β tightly regulates anti-inflammatory activity by suppressing pro-inflammatory cytokine production, thereby inhibiting T-lymphocyte function. Integrins avβ6 and avβ8 sequester latent TGF-β to the cell surface, where activation can be tightly coupled to cellular responses to environmental stress in the maintenance of homeostasis; integrins also localize activated TGFβ in the vicinity of the macrophages. Normally mature TGFβ is secreted as a latent complex with its N-terminal fragment, latency-associated peptide (LAP), which inhibits its activity. The latent complex is covalently linked to the extracellular matrix by binding to latent TGF-β-binding proteins. TGF-β is activated by diverse mechanisms in the lung, ultimately involving either proteolysis or conformational alteration of the LAP. αvβ6 integrin is able to mediate activation of TGF-β by binding to TGF-β1 LAP, which serves as a ligand binding site for the integrin, and is an essential component of the TGF-β activation apparatus. Once activated, TGFβ leads to the suppression of macrophage functionality (cytokine production and phagocytosis).

Sources: en.wikipedia.org

Notes from published material

==== Insecticides ==== RNAi is under development as an insecticide, employing multiple approaches, including genetic engineering and topical application. Cells in the midgut of some insects take up the dsRNA molecules in the process referred to as environmental RNAi. In some insects the effect is systemic as the signal spreads throughout the insect's body (referred to as systemic RNAi). Animals exposed to RNAi at doses millions of times higher than anticipated human exposure levels show no adverse effects. RNAi has varying effects in different species of Lepidoptera (butterflies and moths). Drosophila spp., Bombyx mori, Locusta spp., Spodoptera spp., Tribolium castaneum, Nilaparvata lugens, Helicoverpa armigera, and Apis mellifera are models that have been widely used to learn how RNAi works within particular taxa of insects. Musca domestica has two Ago2 genes and Glossina morsitans three, as found by Lewis et al. 2016 and Hain et al. 2010. In the case of the miRNA pathway Diuraphis noxia has two Ago1s, M. domestica two Dcr1s, Acyrthosiphon pisum two each of Ago1 and Loqs and Dcr1 and four of Pasha. While in the piRNA, G. morsitans and A. pisum have two or three Ago3s each. This has led to identification of future insecticide development targets, and the modes of action and reasons for insecticide resistance of other insecticides.

=== Solvent extraction and complexation chemistry === The liquid-liquid extraction for the selective actinide partitioning (SANEX-like processes) consists of an organic phase, containing an extracting agent dissolved in a suitable solvent mixture, and an aqueous phase, containing the irradiated fuel dissolution in hot nitric acid. The two phases are vigorously mixed to promote the extraction kinetics. The centrifugation process is performed to favour the phase separation and the transfer of the formed complexes from the depleted aqueous phase (raffinate) into the organic phase (extract) where they result more soluble. This solvent separation can be performed by neutral extracting agents dissolved in the solvent. As can be seen in the equation, the solvating ligand (L) extracts the interested metal cation (M) together with its anion (A). The products of this reaction represent all the potential complexes that can form during an extraction process such as

The transition to democracy took place in the early years of his reign, making Spain no longer the only non-communist dictatorship left in Europe. The new king assumed the project of the reformist sector of Franco's political elite that, facing the conservatives, defended the need to introduce gradual changes in the fundamental laws so that the new monarchy would be accepted in Europe as a whole. This project was the one that his first government tried to implement, and it was presided by Carlos Arias Navarro, who had already headed the last government of General Franco. However, in view of the incapacity demonstrated by Arias Navarro, Juan Carlos appointed in July 1976 the Francoist "reformist" Adolfo Suárez as the new Head of Government to lead the process of transition to democracy without any "rupture" with the "previous regime". This is how the Political Reform Act came about, which was approved by the Francoist Cortes and revalidated in the referendum of December 1976. According to this new fundamental law, free elections to democratically elected Cortes were to be called. Suarez's problem was to get the "controlled" transition process established in the Political Reform Act accepted by the democratic opposition, since the latter, in exchange for abandoning the "democratic rupture" and participating in the elections, demanded that Franco's institutions be dismantled and that all parties without exception ─ including the Communist Party of Spain ─ be legalized.

== Epidemiology == Each year, more than 2.5 million people in the United States develop pressure ulcers. In acute care settings in the United States, the incidence of bedsores is 0.4% to 38%; within long-term care it is 2.2% to 23.9%, and in home care, it is 0% to 17%. Similarly, there is wide variation in prevalence: 10% to 18% in acute care, 2.3% to 28% in long-term care, and 0% to 29% in home care. There is a much higher rate of bedsores in intensive care units because of immunocompromised individuals, with 8% to 40% of those in the ICU developing bedsores. However, pressure ulcer prevalence is highly dependent on the methodology used to collect the data. Using the European Pressure Ulcer Advisory Panel (EPUAP) methodology there are similar figures for pressure ulcers in acutely sick people in the hospital. There are differences across countries, but using this methodology, pressure ulcer prevalence in Europe was consistently high, from 8.3% (Italy) to 22.9% (Sweden). A recent study in Jordan also showed a figure in this range. Some research shows differences in pressure-ulcer detection among white and black residents in nursing homes.

In butterfly wing scales, chitin is organized into stacks of gyroids constructed of chitin photonic crystals that produce various iridescent colors serving phenotypic signaling and communication for mating and foraging. The elaborate chitin gyroid construction in butterfly wings creates a model of optical devices having potential for innovations in biomimicry. Scarab beetles in the genus Cyphochilus also utilize chitin to form extremely thin scales (five to fifteen micrometres thick) that diffusely reflect white light. These scales are networks of randomly ordered filaments of chitin with diameters on the scale of hundreds of nanometres, which serve to scatter light. The multiple scattering of light is thought to play a role in the unusual whiteness of the scales. In addition, some social wasps, such as Protopolybia chartergoides, orally secrete material containing predominantly chitin to reinforce the outer nest envelopes, composed of paper. Chitosan is produced commercially by deacetylation of chitin by treatment with sodium hydroxide. Chitosan has a wide range of biomedical applications including wound healing, drug delivery and tissue engineering. Due to its specific intermolecular hydrogen bonding network, dissolving chitin in water is very difficult. Chitosan (with a degree of deacetylation of more than ~28%), on the other hand, can be dissolved in dilute acidic aqueous solutions below a pH of 6.0 such as acetic, formic and lactic acids. Chitosan with a degree of deacetylation greater than ~49% is soluble in water.

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.

Is cardarine approved for any medical use?

No. Cardarine has not received approval for human therapeutic use in major jurisdictions. It remains an investigational compound.

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