en · de
cardarine-notes.peptides3081.com › Info › Identity And Regulatory Status — Background and Details

Identity And Regulatory Status — Background and Details

By Editorial Desk · published 2026-02-18 · last reviewed 2026-03-24 · Info

If you have been reading about LC-MS/MS 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.

Last reviewed on 2026-03-24. Where a claim depends on a specific study, the study is described rather than over-claimed.

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.

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.

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

Regulatory Status and Detection Context

Analytical laboratories typically identify cardarine and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is a common matrix in anti-doping testing, while blood and tissue may be used in research settings. Detection windows depend on the assay, the sample matrix, and the compound's metabolism. Because cardarine is extensively metabolized, laboratories often target specific metabolites to improve sensitivity and confirmation. Reference standards are required for reliable quantification. Method validation includes checks for selectivity, linearity, and carryover.

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.

Related pages on this site

Mechanism and Safety Research

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.

Early clinical research explored GW501516 for lipid disorders, obesity, and diabetes. Some short-term human studies reported changes in HDL cholesterol, LDL cholesterol, and triglycerides. The development program was discontinued after rodent studies showed dose-dependent tumor formation in multiple tissues, including liver, bladder, stomach, and skin. These findings raised concerns about long-term cancer risk in humans. Because human exposure data are limited, the clinical significance of the rodent tumors remains uncertain.

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.

Detection, Regulation, and Quality Context

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.

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.

Background from the literature

42. Adv Gerontol. 2004;14:105-13. [The influence of substances revealing geroprotective of spontaneous carcinogenesis in mice]. [Article in Russian] Popovich IG. The review presents the results of experimental studies conducted by the author. CBA, SHR, HER-2/neu and SAM mice revealed inhibition of age-related alterations in estrus function and spontaneous tumour development and showed life span extension under the influence of the pineal gland hormone Melatonin, synthetic peptide bioregulator Epitalon, delta-sleep-inducing peptide Deltaran, enterosorbent Aqualen and succinic acid containing preparation Neuronol (Noogam). The observed effect depended on the dose and conditions of administration, as well as genetic predisposition of the particular mice strains to tumour development.

90. ArXiv [Preprint]. 2026 Jul 29:arXiv:2605.17186v2. Operator splitting for exploiting linear-rate closure in solving infinite ODE hierarchies. Chang JC. We introduce an operator-splitting method for infinite hierarchies of linear ordinary differential equations (ODEs) indexed by nonnegative integers. When the coupling coefficients depend linearly on the count index, an exact transformation closes the equations on finite count-index windows without an upper-boundary value. For more general hierarchies, Strang splitting applies the linear-rate closure during the linear-rate substeps and a conventional capped solver to the remainder. We derive the closure from generating functions and the method of characteristics and extend it to multi-indexed systems. The derivation requires neither positivity nor mass conservation, so it applies to a wider class of systems than the examplar stochastic models presented here. We discuss branching processes, stochastic predator-prey dynamics, the Schlögl chemical kinetics model, and a telegraph model for gene expression. Through numerical experiments and computational cost analyses we demonstrate that our operator splitting method is typically advantageous for solving large scale systems in terms of memory usage and computational time, while retaining accuracy competitive with finite state projection (FSP) methods. PMCID: PMC13618430

Aviation Safety Network Established in 1996. The ASN Safety Database contains descriptions of over 15800 airliner, military and corporate jet aircraft accidents/incidents since 1921. Bureau of Aircraft Accidents Archives Established in 2000. The B3A contains descriptions of over 22,000 airliner, military and corporate jet aircraft accidents since 1918. National Transportation Safety Board Aviation Accident Synopses – by month Aviation Statistics Statistical and geospatial analysis of general aviation accidents. Aviation Accidents App Access the NTSB Aviation Accidents Database and Final Reports from all over the world on your mobile device Aviation Accidents Map Explore an interactive map showcasing airplane crash sites Air Crash Map | Interactive Aviation Accident Database

Sources: pubmed.ncbi.nlm.nih.gov

Further detail

Bruce Glick grew up in Pittsburgh, Pennsylvania and was interested in birds as a child. His father, Peter Glick, was the Secretary of Labor for Pennsylvania. Glick served in World War II. He went to Rutgers University and studied birds majoring in poultry science, graduating in 1951. In 1950 he married Kay McCall. He received an M.S. degree from the University of Massachusetts in genetics in 1952 and attended Ohio State University as a Ph.D. student, graduating with a PhD in physiology in 1955. While there, he worked on determining the purpose of the Bursa of Fabricius, a gland that he was able to remove from a goose without any apparent effect. A fellow graduate student, Timothy Chang, worked with Glick's geese in a different study, and noticed that the birds without the Bursa of Fabricius did not produce expected antibodies. Glick and Chang wrote up the results of this study and were unable to get it published in Science, so it was published in Poultry Science in 1956. Their publication, considered a landmark paper, is one of the most cited works from Poultry Science.

When the B cells get activated, class switching can occur. The class switching involves switch regions that made up of multiple copies of short repeats (GAGCT and TGGGG). These switches occur at the level of rearrangements of the DNA because there is a looping event that chops off the constant regions for IgM and IgD and form the IgG mRNAs. Any continuous looping occurrence will produce IgE or IgA mRNAs. In addition, cytokines are factors that have great effects on class switching of different classes of antibodies. Their interaction with B cells provides the appropriates signals needed for B cells differentiation and eventual class switching occurrence. For example, interleukin-4 induces the rearrangements of heavy chain immunoglobulin genes. That is IL- 4 induces the switching of Cμ to Cγ to Cκ

28. Adv Gerontol. 2007;20(1):74-85. [Normalizing effect of the pineal gland peptides on the daily melatonin rhythm in old monkeys and elderly people]. [Article in Russian] Korkushko OV, Lapin BA, Goncharova ND, Khavinson VKh, Shatilo VB, Vengerin AA, Antoniuk-Shcheglova IA, Magdich LV. In the course of aging both monkeys and people reveal decreased night and average daily level of melatonin in the blood plasma and reduced hormone circadian rhythm amplitude, which evidence the disorder of the pineal gland melatonin releasing function. Peptide preparations of the pineal gland (Epithalamin--a complex of peptides isolated from the pineal gland and Epitalon--synthetic tetrapeptide) recover night release of endogenous melatonin and lead to the normalization of the hormone circadian rhythm in the blood plasma. In elderly people Epithalamin and Epitalon modulate pineal gland functional state: people with pineal gland functional insufficiency report an increase of night melatonin level. The preparations of the pineal gland, effectively increasing melatonin concentration and having no side effects, can be used in clinical geriatric practice.

Cardiac alpha actin is a 42.0 kDa protein composed of 377 amino acids. Cardiac alpha actin is a filamentous protein extending from a complex mesh with cardiac alpha-actinin (ACTN2) at Z-lines towards the center of the sarcomere. Polymerization of globular actin (G-actin) leads to a structural filament (F-actin) in the form of a two-stranded helix. Each actin can bind to four others. The atomic structure of monomeric actin was solved by Kabsch et al., and closely thereafter this same group published the structure of the actin filament. Actins are highly conserved proteins; the alpha actins are found in muscle tissues and are a major constituent of the contractile apparatus. Cardiac (ACTC1) and skeletal (ACTA1) alpha actins differ by only four amino acids (Asp4Glu, Glu5Asp, Leu301Met, Ser360Thr; cardiac/skeletal). The actin monomer has two asymmetric domains; the larger inner domain comprised by sub-domains 3 and 4, and the smaller outer domain by sub-domains 1 and 2. Both the amino and carboxy-termini lie in sub-domain 1 of the outer domain.

Sources: en.wikipedia.org

Supporting material

January 19 – March 25: 2018 FIBA Americas League San Lorenzo defeated Mogi das Cruzes, 79–71, to win their first FIBA Americas League title. Regatas Corrientes took third place. June 11 – 16: 2018 FIBA Under-18 Americas Championship in St. Catharines The United States defeated Canada, 113–74, to win their fifth consecutive and ninth overall FIBA Under-18 Americas Championship title. Argentina took third place. August 1 – 7: 2018 FIBA Under-18 Women's Americas Championship in Mexico City The United States defeated Canada, 84–60, to win their ninth consecutive and tenth overall FIBA Under-18 Women's Americas Championship title. Argentina took third place.

Aerotolerant anaerobes use fermentation to produce ATP. They do not use oxygen, but they can protect themselves from reactive oxygen molecules. In contrast, obligate anaerobes can be harmed by reactive oxygen molecules. There are three categories of anaerobes. Where obligate aerobes require oxygen to grow, obligate anaerobes are damaged by oxygen, aerotolerant organisms cannot use oxygen but tolerate its presence, and facultative anaerobes use oxygen if it is present but can grow without it. Most aerotolerant anaerobes have superoxide dismutase and (non-catalase) peroxidase but do not have catalase. More specifically, they may use a NADH oxidase/NADH peroxidase (NOX/NPR) system or a glutathione peroxidase system. An example of an aerotolerant anaerobe is Cutibacterium acnes.

Thioesters are prominent active esters, as illustrated by the esters of coenzyme A. Terpenes and terpenoids are generated from active esters. Some biosynthetically significant active esters include isopentenyl pyrophosphate, dimethylallyl pyrophosphate, and geranyl pyrophosphate. Hydroxybenzotriazole is used in peptide synthesis by forming an active ester from acyl isoureas. Classically, activated esters are derivatives of nitrophenols and pentafluorophenol. These esters react with nucleophiles much more rapidly than the related aryl and especially alkyl esters. Active esters of acrylic acid are precursors to polymers with reactive side chains. The concept of active esters extends to esters of phosphoric and sulfuric acids. One such case is dimethylsulfate, a strong methylating agent.

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.

How does cardarine work in the body?

It binds and activates PPARδ, a nuclear receptor that influences gene expression related to fatty acid metabolism and energy balance. This mechanism has been studied mainly in animals and cell models, not established as a safe human therapy.

Network