This is a working overview of anti-doping, written for readers who want more than a one-paragraph summary but less than a textbook.
Reviewed 2025-10-07. Anything still debated is marked as such rather than presented as settled.
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.
Preclinical research reported that GW501516 increased running endurance in mice and improved lipid profiles in some animal species. Early human trials explored effects on high-density lipoprotein cholesterol, triglycerides, and glucose handling, but the program was discontinued. Published human data are sparse and do not establish efficacy for any condition. Studies also examined PPAR delta in cancer biology, with conflicting findings across models. The relationship between receptor activation, tissue context, and disease risk remains an active area of investigation.
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.
| Property | Value | Notes |
|---|---|---|
| IUPAC name | {4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]phenoxy}acetic acid | Systematic name for GW501516 |
| CAS Registry Number | 317318-70-0 | Unique identifier for the parent compound |
| Molecular formula | C21H18F3NO3S2 | Includes carbon, hydrogen, fluorine, nitrogen, oxygen, and sulfur |
| Molecular weight | 453.5 g/mol | Approximate value for the neutral form |
| Appearance | White to off-white powder | Typical description for purified laboratory material |
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.
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.
Published human data are sparse and mostly come from early-phase trials. Those studies examined short-term changes in lipids, glucose, and exercise capacity, but they were not large enough to establish efficacy or long-term safety. Some animal experiments reported increased running endurance, yet such findings do not prove a performance benefit in people. Anti-doping laboratories detect GW501516 and its metabolites in urine or blood using liquid chromatography-tandem mass spectrometry. Detection windows depend on dose, sample type, and individual metabolism. The method is sensitive enough to identify trace residues in tested samples.
Laboratory handling focuses on identity, purity, and stability. Reference standards are typically stored cold and dry, protected from light, because solutions can degrade over time. Analytical checks may use high-performance liquid chromatography with ultraviolet detection or mass spectrometry. Impurities and related substances can be separated chromatographically and compared with a known standard. Because cardarine is not an approved drug, compendial monographs are absent, and laboratories often rely on in-house methods. Reported purity varies among unregulated products and should not be assumed from a label.
GW501516 acts as a selective agonist at PPARδ, a nuclear receptor that regulates transcription of genes involved in lipid handling and energy metabolism. Activation of PPARδ in preclinical models increases fatty acid oxidation, mitochondrial biogenesis, and exercise endurance in rodents. These effects have made the compound a subject of metabolic research and also a target for sport anti-doping rules. In humans, however, controlled studies are limited, and whether similar endurance or metabolic changes occur at tolerated exposures remains an open question. The receptor’s broad tissue distribution also means downstream effects may vary by organ and condition.
Detection of GW501516 in biological samples generally relies on liquid chromatography coupled with tandem mass spectrometry. Urine is a common matrix in anti-doping analysis, while blood or plasma may be used in research settings. Sample preparation can involve enzymatic hydrolysis, protein precipitation, or solid-phase extraction before instrumental analysis. Because the compound undergoes metabolism, assays may target the parent molecule, one or more metabolites, or both. Detection windows are not fixed; they depend on factors such as dose, route, individual metabolism, and assay sensitivity. Reference standards are required for accurate identification and quantification.
Instrumentation is used to monitor and control the process plant in the oil, gas and petrochemical industries. Instrumentation ensures that the plant operates within defined parameters to produce materials of consistent quality and within the required specifications. It also ensures that the plant is operated safely and acts to correct out of tolerance operation and to automatically shut down the plant to prevent hazardous conditions from occurring. Instrumentation comprises sensor elements, signal transmitters, controllers, indicators and alarms, actuated valves, logic circuits and operator interfaces. An outline of key instrumentation is shown on Process Flow Diagrams (PFD) which indicate the principal equipment and the flow of fluids in the plant. Piping and Instrumentation Diagrams (P&ID) provide details of all the equipment (vessels, pumps, etc), piping and instrumentation on the plant in a symbolic and diagrammatic form.
== History == Anti-U1 RNP antibodies were first described in the early 1970s during studies of patients with mixed connective tissue disease. In 1972, rheumatologist Dr, Gordon Sharp and colleagues identified antibodies directed against extractable nuclear antigens (ENAs) in patients who had symptoms of several autoimmune connective tissue diseases. Their work helped establish mixed connective tissue disease (MCTD) as a distinct clinical syndrome and made anti-U1 RNP antibodies an important laboratory discovery in rheumatology. The discovery of anti-U1 RNP antibodies also improved the understanding of autoimmune connective tissue disease. Before these antibodies were identified, many patients with overlapping symptoms were difficult to classify because their conditions shared characteristics of several different autoimmune disorders. Identifying anti-U1 RNP antibodies gave healthcare physicians another way to recognize patterns of disease and support the diagnosis of mixed connective tissue disease. Although the antibodies are not exclusive to MCTD, they remain one of the most characteristic scientific findings associated with the condition. Since their discovery, advances in immunology and laboratory testing have improved the ability to detect anti-U1 RNP antibodies. Early testing methods were time-consuming and performed mainly in research laboratories, but newer techniques such as enzyme-linked immunosorbent assays (ELISA), immunoblotting, and multiplex immunoassays have made testing faster and more widely available.
== Other major examples == The cytochrome P450 isozymes play important roles in metabolism and steroidogenesis. The multiple forms of phosphodiesterase also play major roles in various biological processes. Although more than one form of these enzymes have been found in individual cells, these isoforms of the enzyme are unequally distributed in the various cells of an organism. From the clinical standpoint they have been found to be selectively activated and inhibited, an observation which has led to their use in therapy.
Radionuclides are incorporated either into compounds normally used by the body such as glucose (or glucose analogues), water, or ammonia, or into molecules that bind to receptors or other sites of drug action. Such labelled compounds are known as radiotracers. PET technology can be used to trace the biologic pathway of any compound in living humans (and many other species as well), provided it can be radiolabeled with a PET isotope. Radiotracers for new target molecules and processes are continuing to be synthesized. As of this writing there are already dozens in clinical use and hundreds applied in research. In 2020 by far the most commonly used radiotracer in clinical PET scanning is the carbohydrate derivative FDG. This radiotracer is used in essentially all scans for oncology and most scans in neurology, thus makes up the large majority of radiotracer (>95%) used in PET and PET–CT scanning. Due to the short half-lives of most positron-emitting radioisotopes, the radiotracers have traditionally been produced using a cyclotron in close proximity to the PET imaging facility. The half-life of fluorine-18 is long enough that radiotracers labeled with fluorine-18 can be manufactured commercially at offsite locations and shipped to imaging centers. Recently rubidium-82 generators have become commercially available. These contain strontium-82, which decays by electron capture to produce positron-emitting rubidium-82. The use of positron-emitting isotopes of metals in PET scans has been reviewed, including elements not listed above, such as lanthanides.
Sources: en.wikipedia.org
=== Pharmacokinetics === The bioavailability of methamphetamine is 67% orally, 79% intranasally, 67 to 90% via inhalation (smoking), and 100% intravenously. Following oral administration, methamphetamine is well-absorbed into the bloodstream, with peak plasma methamphetamine concentrations achieved in approximately 3.13–6.3 hours post ingestion. Methamphetamine is also well absorbed following inhalation and following intranasal administration. Because of the high lipophilicity of methamphetamine due to its methyl group, it can readily move through the blood–brain barrier faster than other stimulants, where it is more resistant to degradation by monoamine oxidase. The amphetamine metabolite peaks at 10–24 hours. Methamphetamine is excreted by the kidneys, with the rate of excretion into the urine heavily influenced by urinary pH. When taken orally, 30–54% of the dose is excreted in urine as methamphetamine and 10–23% as amphetamine. Following IV doses, about 45% is excreted as methamphetamine and 7% as amphetamine. The elimination half-life of methamphetamine varies with a range of 5–30 hours, but it is on average 9 to 12 hours in most studies. The elimination half-life of methamphetamine does not vary by route of administration, but is subject to substantial interindividual variability. CYP2D6, dopamine β-hydroxylase, flavin-containing monooxygenase 3, butyrate-CoA ligase, and glycine N-acyltransferase are the enzymes known to metabolize methamphetamine or its metabolites in humans.
In obesity, a decreased sensitivity to leptin occurs (similar to insulin resistance in type 2 diabetes), resulting in an inability to detect satiety despite high energy stores and high levels of leptin.
== Activities == The activity in Chromatography spans HPLC, LC/MS, FPLC, MPLC - GC, GC/MS, GPC, GFC - RMN - AA, IR, ICP, UV – SPE. Interchim notably introduced new generation silica chromatography media (UptiSphere that has become a standard worldwide, Strategy, Atoll). The activity in Fine Chemistry deals with compounds libraries (Chirals, Fluorines, Building blocks for Combi-Chemistry) and flash chromatography. Interchim developed a unique flash chromatography system (PuriFlashEvo430 - integrated functions). The activity in BioSciences focuses on Immunodetection, Biochemistry, Electrophoresis and Cell Assays. Interchim manufactures protein assays (BC Assay, Coo Assay), superior fluorescent dyes known as FluoProbes, Cell Assays reagents and kits (i.e. FluoProbes indicators, high sensitive viability assay UptiBlue) and an innovate transfection agent UptiFectin.
A nanocapsule is a nanoscale shell made from a nontoxic polymer. They are vesicular systems made of a polymeric membrane which encapsulates an inner liquid core at the nanoscale. Nanocapsules have many uses, including promising medical applications for drug delivery, food enhancement, nutraceuticals, and for self-healing materials. The benefits of encapsulation methods are for protection of these substances to protect in the adverse environment, for controlled release, and for precision targeting. Nanoencapsulation is the technique that uses nanocapsules to pack substances to be released in a controlled and effective way. Nanocapsules can be made of various types of nanomaterials; the most common ones are liposomes, nanoparticles, micelles, nanospheres, nanoemulsions and nanocochleates. Nanocapsules can potentially be used as MRI-guided nanorobots or nanobots, although challenges remain.
A research study in which the medical records of groups of individuals who are alike in many ways but differ by a certain characteristic (for example, female nurses who smoke and those who do not smoke) are compared for a particular outcome. Also called a retrospective cohort study. (NCI) Historical control subject
Sources: en.wikipedia.org
==== Disease resistant cultivars ==== Resistant varieties are available. In Indian cultivars, Nataraj et al. 2020 find that anthracnose caused by Colletotrichum truncatum is resisted by a combination of 2 major genes.
butyl The alkyl functional group derived from either of the two isomers of butane, with the generic chemical formula –C4H9. It may occur as a substituent in organic compounds or exist independently as an ion or radical. In IUPAC nomenclature, the presence of a butyl substituent is indicated with the prefix butyl in the name of the compound, or with the abbreviation Bu in chemical formulae; e.g. butyl alcohol (butanol), which may occur in any of five different isomeric forms depending on the arrangement of the four carbon atoms, is often written with the generic formula CH4CH9OH or BuOH.
=== February === 12 February Using observations by ESA's CHEOPS telescope, scientists describe a unique configuration of a planetary system around the star LHS 1903, where the innermost and outermost planets are rocky, while the two middle planets have extended atmospheres. This provides support for the "inside-out" model of planet formation. A small polymerase ribozyme is described which can synthesize both its complementary strand and a copy of itself. This is interpreted as a substantial support for the "RNA world" hypothesis of the origin of life. Researchers at Iceberg Quantum publish a study describing the "Pinnacle Architecture", a fault-tolerant quantum computing design based on quantum low-density parity-check (qLDPC) codes. They show that a 2048-bit RSA integer could be factored with fewer than 100,000 physical qubits under standard hardware assumptions – an order-of-magnitude reduction compared to previous estimates. 24 February – Researchers in Switzerland report that centenarians show "youthful" blood profiles across 37 proteins, including markedly lower oxidative stress markers, suggesting that specific aging-related biological pathways are slowed in exceptional longevity. 26 February – Researchers in Australia report that serum bicarbonate levels in U.S. population data have risen by 7% since 1999, tracking increases in atmospheric carbon dioxide. Modelling suggests that, if current trends continue, average bicarbonate levels could approach the upper limit of today's accepted healthy range within 50 years.
== Adenylylators == Enzymes responsible for AMPylation, called AMPylators or Adenylyltransferase, fall into two different families, all depending on their structural properties and mechanism used. AMPylator is created by two catalytic homologous halves. One half is responsible for catalyzing the adenylylation reaction, while the other half catalyzes the phosphorolytic deadenylylation reaction. These two families are the DNA-β-polymerase-like and the Fic family. DNA-β-polymerase-like, is a family of Nucleotidyltransferase. It more specifically is known as the GlnE family. There is a specific motif that is used to clarify this particular family. The motif consists of a three stranded β-sheet which is part of magnesium ion coordination and phosphate binding. Aspartate is essential for the activity to occur in this family. The Fic domain belongs to Fido (Fic/Doc) superfamilyFic family, which is a filamentation induced by cyclic AMP domain, is known to perform AMPylation. This term was coined when VopS from Vibrio parahaemolyticus was discovered to modify RhoGTPases with AMP on a serine. This family of proteins are found in all domains of life on earth. It is mediated via a mechanism of ATP-binding-site alpha helix motif. Infectious bacteria use this domain to interrupt phagocytosis and cause cell death. Fic domains are evolutionarily conserved domains in prokaryotes and eukaryotes that belong to the Fido domain superfamily.
Sources: en.wikipedia.org
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.
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.
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.
It binds to and activates PPAR delta, a nuclear receptor that controls expression of genes related to fatty acid oxidation. This mechanism can alter energy metabolism in animal models. It is not a direct stimulant or fat-burning enzyme.