If you have been reading about anti-doping 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 2026-01-21. Where a claim depends on a specific study, the study is described rather than over-claimed.
Laboratory detection of GW501516 commonly uses liquid chromatography coupled with tandem mass spectrometry. The method can identify the parent compound or its metabolites in urine and blood after sample cleanup. Protein precipitation, solid-phase extraction, or enzymatic hydrolysis may precede analysis, depending on the matrix. Reference standards are required for accurate quantification and confirmation. Because the compound is not approved, testing often occurs in anti-doping, forensic, or research settings rather than routine clinical care. Results are reported with limits of detection and quantification.
Stability of GW501516 depends on form, temperature, light exposure, and moisture. Solid reference material is typically stored frozen or refrigerated in a desiccator and protected from light. Solutions in organic solvents such as dimethyl sulfoxide are often kept frozen in aliquots to reduce freeze-thaw cycling. Aqueous solubility is low, so aqueous stock solutions can be difficult to prepare without cosolvents. Degradation may appear as changes in chromatographic purity or mass spectral signal. Stability studies are needed to establish shelf life for any specific preparation.
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.
Sporting authorities added GW501516 to prohibited lists after it appeared in athlete samples and online markets. The World Anti-Doping Agency classifies it as a hormone and metabolic modulator, and its use can lead to an anti-doping rule violation. Some early laboratory work suggested effects on fatty acid oxidation and endurance-related metabolism in animals, but those findings do not establish safe or effective use in people. Reports of adverse events in humans are scarce and often anecdotal, which complicates risk assessment.
| Property | Value | Notes |
|---|---|---|
| Appearance | White to off-white powder | Common for reference-grade material. |
| Solubility | Low in water | Dissolves in DMSO and some organic solvents. |
| Typical storage | -20 °C, desiccated | Protect from light and moisture. |
| Analytical method | LC-MS/MS | Used for trace detection in biological matrices. |
| Purity assessment | HPLC with UV detection | Often combined with NMR and mass spectrometry. |
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.
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.
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.
=== Lipid and inflammatory outcomes === Moreover, it also promotes decreases in total cholesterol (TC), triglycerides (TG), low-density lipoprotein (LDL), and C-reactive protein (CRP) as well as increases in high-density lipoprotein (HDL) and adiponectin concentrations.
The dharmachakra (Sanskrit: धर्मचक्र dharmacakra, Pali: dhammacakka) or wheel of dharma is a symbol used in the Dharmic religions. It has a widespread use in Buddhism. The dharmachakra is considered one of the ashtamangala (auspicious signs) in Hinduism and Buddhism. In some specific regional sites like in Odisha, dharmachakra imagery in Hindu temples has been linked to sites with an earlier Buddhist presence. The symbol also finds its usage in modern India, most notably at the centre of the flag of India. Outside India, the dharmachakra has also been used as a decoration in Southeast Asian statues and inscriptions, beginning with the earliest period of Buddhism in Southeast Asia. It remains a major symbol of the Buddhist religion today.
== Adverse effects == Adverse effects almost solely occur in humans that suffer from glucose-6-phosphate dehydrogenase deficiency. This deficiency causes a shortage of glutathione in erythrocytes and glutathione is needed for the neutralization of ROS (reactive oxygen species) created by the strongly oxidizing agent divicine. Glucose-6-phosphate dehydrogenase deficiency is a common genetic condition, with a global prevalence of approximately 4.9%, affecting over 400 million individuals worldwide. It is important to recognize that glucose-6-phosphate dehydrogenase deficiency can still be life-threatening if not promptly diagnosed and managed. Effective management often includes interventions as blood transfusions, but with appropriate care, full recovery from favism without lasting complications is the expected outcome.
Sources: en.wikipedia.org
μ-Opioid receptor (MOR): extremely high affinity partial agonist: at low doses, the MOR-mediated effects of buprenorphine are comparable to those of other narcotics, but these effects reach a "ceiling" as the receptor population is saturated. This behavior is responsible for several unique properties: buprenorphine greatly reduces the effect of most other MOR agonists, can cause precipitated withdrawal when used in actively opioid dependent persons, and has a lower incidence of respiratory depression relative to full MOR agonists. κ-Opioid receptor (KOR): High affinity antagonist/weak partial agonist —this activity is hypothesized to underlie some of the effects of buprenorphine on mood disorders and addiction. δ-Opioid receptor (DOR): High affinity antagonist Nociceptin receptor (NOP, ORL-1): Weak affinity, very weak partial agonist In simplified terms, buprenorphine can essentially be thought of as a nonselective, mixed agonist–antagonist opioid receptor modulator, acting as an unusually high affinity, weak partial agonist of the MOR, a high affinity antagonist of the KOR and DOR, and a relatively low affinity, very weak partial agonist of the ORL-1/NOP. Although buprenorphine is a partial agonist of the MOR, human studies have found that it acts like a full agonist with respect to analgesia in opioid-intolerant individuals. Conversely, buprenorphine behaves like a partial agonist of the MOR with respect to respiratory depression. Buprenorphine is also known to have high binding affinity with antagonistic activity at the putative ε-opioid receptor.
Cyclophosphamide (Cytoxan, Procytox), Doxorubicin (Adriamycin) and Vincristine (Oncovin) Paclitaxel (Taxol) Irinotecan (Camptosar) Guidelines recommended as of 2018 that patients who relapse > 6 months from initial therapy should be retreated with the original chemotherapy regimen. For patients who relapse in < 6 months, single-agent chemotherapy either topotecan second-line therapy, or paclitaxel can be used.
=== Scratch-resistant lenses === A sunglasses manufacturer called Foster Grant first licensed a NASA technology for scratch-resistant lenses, developed for protecting space equipment from scratching in space, especially helmet visors.
=== PnuC of Haemophilus influenzae === The H. influenzae homologue has been shown to transport NR from the periplasm into the cytoplasm. Phosphorylation of NR by NadR is required for NR uptake. The ribonucleoside kinase (RNK) domain has both Walker A and Walker B motifs, responsible for ATP binding and phosphoryl transfer. In addition, a proposed LID domain was identified in RNK. LID domains have been found in other kinases, and these domains are regions which are able to move after substrate binding. They are responsible for coordination of three distinct conformations, an open state in the absence of substrate, a partially closed state after substrate binding, and a fully closed state when both substrates are present. In H. influenzae, NR enters the NAD+ resynthesis pathway after phosphorylation to NMN, and subsequently, NAD+ is synthesized from NMN and ATP via an NMN adenylyl transferase activity. NadR represents a multifunctional regulator/enzyme complex able to integrate several functions, such as enzymatic catalysis, transport, and transcriptional regulatory activities.
Sources: en.wikipedia.org
LC-MS/MS is common, often after sample cleanup. The assay targets GW501516 or its metabolites.
Reference material is usually kept cold, dry, and protected from light. Frozen aliquots reduce repeated freeze-thaw cycles.
No approved pharmaceutical product exists, so manufacturing and quality controls are not standardized. Products may contain different compounds or impurities.
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.