If you have been reading about Investigational drug 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 2026-03-10. Numbers and descriptions here follow the published literature rather than marketing material.
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.
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.
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.
| Property | Value | Notes |
|---|---|---|
| Molecular target | PPAR delta (NR1C2) | Ligand-activated nuclear receptor. |
| Primary tissues studied | Skeletal muscle, liver, adipose | Effects on fatty acid oxidation and energy use. |
| Typical detection matrix | Urine | Used in anti-doping analysis. |
| Common analytical method | LC-MS/MS | Detects parent compound and metabolites. |
| Sport regulatory class | Prohibited at all times | Listed as a metabolic modulator by WADA. |
Handling and quality assessment of cardarine reference material follow general laboratory practices for poorly characterized compounds. It typically appears as a white to off-white powder and is sparingly soluble in water but soluble in organic solvents such as dimethyl sulfoxide and ethanol. Storage recommendations usually specify a cool, dry, dark place, with long-term storage at low temperature and desiccation. Purity may be checked by high-performance liquid chromatography with ultraviolet detection, while identity is confirmed by mass spectrometry and nuclear magnetic resonance. No pharmacopeial monograph exists, so reported purity and stability depend on the supplier’s methods.
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.
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 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.
PPARδ is a nuclear receptor that regulates gene expression related to fatty acid oxidation, glucose homeostasis, and mitochondrial function. GW501516 binds to this receptor with high affinity and activates downstream signaling in skeletal muscle and other tissues. Animal studies reported increased endurance and altered fuel preference, but human data remain limited and inconsistent. The precise relationship between receptor activation and observed physiological changes is still an area of active investigation. Researchers have also examined whether the compound affects inflammation or cell proliferation. No approved therapeutic indication exists for cardarine.
Cardarine is prohibited in competitive sport under the World Anti-Doping Agency code, where it is classified as a metabolic modulator. It is not approved as a prescription medicine in the United States, European Union, or other major markets. Regulatory action has focused on its presence in sports and in products marketed as research chemicals. Because it has no accepted medical indication, supply is often unregulated. This status creates legal and safety uncertainties for anyone who encounters the substance.
Anti-doping laboratories detect GW501516 and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is the most common matrix, though blood and dried blood spots may also be used in some programs. Detection depends on factors such as dose, timing, metabolism, and the sensitivity of the assay. Published methods describe limits of detection in the low nanogram per milliliter range for related compounds. Exact detection windows are not fixed for all situations and remain an area of ongoing study.
Products sold as cardarine have been found to contain incorrect compounds, variable amounts, or no active ingredient at all. Independent testing is required to verify identity and purity. Common analytical approaches include high-performance liquid chromatography, mass spectrometry, and nuclear magnetic resonance for structural confirmation. These methods can distinguish GW501516 from related PPAR agonists and from unrelated steroids. For regulators and researchers, such verification is central to interpreting both biological results and adverse event reports.
Codon reassignment is the biological process via which the way the genetic code of a cell is read is changed as a response to the environment. Typically codons, sets of three mRNA nucleotides, correspond to one specific amino acid. Codon reassignment is the exception to this rule. When a codon is reassigned, it codes for a new amino acid. This change in code can have immense consequences for the cell as protein structures are altered.
== Special cases == Examples of tangential quadrilaterals are the kites, which include the rhombi, which in turn include the squares. The kites are exactly the tangential quadrilaterals that are also orthodiagonal. A right kite is a kite with a circumcircle. If a quadrilateral is both tangential and cyclic, it is called a bicentric quadrilateral, and if it is both tangential and a trapezoid, it is called a tangential trapezoid.
== Disease relevance == Diseases have been linked to R5P imbalances in cells. Cancers and tumors show upregulated production of R5P correlated to increased RNA and DNA synthesis. Ribose 5-phosphate isomerase deficiency, the rarest disease in the world, is also linked to an imbalance of R5P. Although the molecular pathology of the disease is poorly understood, hypotheses included decreased RNA synthesis. Another disease linked to R5P is gout. Higher levels of G6P lead to a buildup of glycolytic intermediates, that are diverted to R5P production. R5P converts to PRPP, which forces an overproduction of purines, leading to uric acid build up. Accumulation of PRPP is found in Lesch-Nyhan Syndrome. The build up is caused by a deficiency of the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRT), which leads to decreased nucleotide synthesis and an increase of uric acid production. Superactivity in PRPS1, the enzyme that catalyzes the R5P to PRPP, has also been linked to gout, as well as neurodevelopmental impairment and sensorineural deafness.
=== Fluorometric === Fluorescence is when a molecule emits light of one wavelength after absorbing light of a different wavelength. Fluorometric assays use a difference in the fluorescence of substrate from product to measure the enzyme reaction. These assays are in general much more sensitive than spectrophotometric assays, but can suffer from interference caused by impurities and the instability of many fluorescent compounds when exposed to light. An example of these assays is again the use of the nucleotide coenzymes NADH and NADPH. Here, the reduced forms are fluorescent and the oxidised forms non-fluorescent. Oxidation reactions can therefore be followed by a decrease in fluorescence and reduction reactions by an increase. Synthetic substrates that release a fluorescent dye in an enzyme-catalyzed reaction are also available, such as 4-methylumbelliferyl-β-D-galactoside for assaying β-galactosidase or 4-methylumbelliferyl-butyrate for assaying Candida rugosa lipase.
Sources: en.wikipedia.org
=== Non-nutrients === Ethanol (C2H5OH) is not an essential nutrient, but it does supply approximately 29 kilojoules (7 kilocalories) of food energy per gram. For spirits (vodka, gin, rum, etc.) a standard serving in the United States is 44 millilitres (1+1⁄2 US fluid ounces), which at 40% ethanol (80 proof) would be 14 grams and 410 kJ (98 kcal). At 50% alcohol, this would be 17.5 g and 513 kJ (122.5 kcal). Wine and beer contain a similar amount of ethanol in servings of 150 and 350 mL (5 and 12 US fl oz), respectively, but these beverages also contribute to food energy intake from components other than ethanol. A 150 mL (5 US fl oz) serving of wine contains 420 to 540 kJ (100 to 130 kcal). A 350 mL (12 US fl oz) serving of beer contains 400 to 840 kJ (95 to 200 kcal). According to the U.S. Department of Agriculture, based on NHANES 2013–2014 surveys, women ages 20 and up consume on average 6.8 grams of alcohol per day and men consume on average 15.5 grams per day. Ignoring the non-alcohol contribution of those beverages, the average ethanol contributions to daily food energy intake are 200 and 450 kJ (48 and 108 kcal), respectively. Alcoholic beverages are considered empty calorie foods because, while providing energy, they contribute no essential nutrients. By definition, phytochemicals include all nutritional and non-nutritional components of edible plants. Included as nutritional constituents are provitamin A carotenoids, whereas those without nutrient status are diverse polyphenols, flavonoids, and lignans that are present in numerous plant foods.
By the 1960s, Bryant Park had entered a state of deterioration, due to a lack of maintenance and its location in a business district with few nighttime activities. In an attempt to deter crime, new lighting was installed in Bryant Park in 1962. Nevertheless, in 1966, parks commissioner Thomas Hoving called a meeting to restore the park, noting its degraded condition. By the 1970s, Bryant Park had been taken over by drug dealers and the homeless, and was considered a no-go area by ordinary citizens and visitors. The condition of the park was so bad that in 1973, parks commissioner Richard M. Clurman threatened to "close Bryant Park and clear it of everybody—until we can get together and make it a place that New Yorkers want it to be." After a man was murdered at the park in 1976, the New York Times noted that gambling and drinking were commonplace at the park. In an opinion piece in the New York Daily News, Jerome Gartner, a coordinator for the Bryant Park Steering Committee, stated that the mugging of a Union Carbide executive in Bryant Park had been quoted as a reason for the company's moving out of New York City. An initial attempt at cleanup was commenced by the Bryant Park Community Fund in the mid-1970s. Free concerts were added in the hope that it would keep out criminals. The initiative was largely unsuccessful, though, and its funding was nearly depleted by 1977. Another initiative, the Bryant Park Steering Committee, was created in 1977 as a partnership between local businesses and the City University of New York.
== Other Branded Generics == Biqi is the brand name for its generic OTC anti-diarrhea pharmaceutical. The Company obtained approval to manufacture and sell Biqi in November 1999. Zaiqi is the brand name for the company's azithromycin granules antibiotics for the treatment of infections. Zaike is the brand name for its cefaclor in dry suspension antibiotics for the treatment of infections. Simcere Kechuanning is the brand name for Simcere Pharmaceutical's OTC herbal medicine used for the treatment of coughs. It comes in oral liquid and tablet formulations. Zaikang is the brand name for its OTC compound zinc gluconate and ibuprofen granules for the treatment of cold symptoms, such as fever, nasal congestion, running nose and sneezing. Faneng is the brand name for the company's alfacalcidol soft capsules for the treatment of osteoporosis.
DMT is inactive when ingested orally due to metabolism by monoamine oxidase (MAO), and DMT-containing drinks such as ayahuasca have been found to contain monoamine oxidase inhibitors (MAOIs), in particular, harmine and harmaline. Life-threatening lethalities such as serotonin syndrome (SS) may occur when MAOIs are combined with certain serotonergic medications such as selective serotonin reuptake inhibitor (SSRI) antidepressants. Serotonin syndrome has also been reported with tricyclic antidepressants (TCAs), certain opioids, certain analgesics, and antimigraine drugs; it is advised to exercise caution when an individual has used dextromethorphan (DXM), MDMA, ginseng, or St. John's wort recently. Chronic use of SSRIs, TCAs, and MAOIs diminish subjective effects of psychedelics due to presumed serotonin 5-HT2A receptors downregulation and/or desensitization secondary to elevated serotonin levels. However, a clinical study of people with depression found that SSRIs did not diminish the effects of DMT and instead resulted in greater mystical experience, emotional breakthrough, and ego dissolution scores with DMT than in people with depression not on antidepressants. This was in contrast to previous research finding that SSRIs diminished the effects of serotonergic psychedelics. The interaction between psychedelics and antipsychotics and anticonvulsants are not well documented; however, reports reveal that co-use of psychedelics with mood stabilizers such as lithium may provoke seizure and dissociative effects in individuals with bipolar disorder.
7 January Hunt for the Death Star, about lethal energy bursts across the universe; Ray Klebesadel; music from the opening of You Only Live Twice; Bohdan Paczyński of Princeton University and unknown gamma-ray bursts; Stan Woosley of the University of California, Santa Cruz; the Compton Gamma Ray Observatory was deployed from 1991; Canadian Dale Frail of the Very Large Array in Socorro, New Mexico, and the W. M. Keck Observatory; the High Energy Transient Explorer 1 (HETE), launched incorrectly by a Northrop Grumman Pegasus on 4 November 1996, due to a faulty battery; music from Moonraker- Flight Into Space; Dutch researchers from the Anton Pannekoek Institute for Astronomy; the Italian BeppoSAX satellite, launched in April 1996; HETE 2 was launched on 9 October 2000.
Sources: en.wikipedia.org
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.
Early-stage trials examined lipid and glucose markers, but the development program was discontinued. Published human results are limited and do not support approved use for any indication. Claims of performance or health benefits remain unproven.
Yes. Laboratories use LC-MS/MS to detect GW501516 and its metabolites in urine. Detection depends on timing and sensitivity, but the substance is banned at all times.
No. Cardarine is a PPARδ agonist, while selective androgen receptor modulators act on androgen receptors. The two classes differ in receptor target and downstream effects.