A practical reference on GW501516: what it is, how it behaves, what the literature reports, and where the honest uncertainties sit.
Reviewed 2026-04-10. Anything still debated is marked as such rather than presented as settled.
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.
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.
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.
| 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.
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.
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.
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.
The type of fats in the diet is also important, with saturated fat and trans fats increasing the risk and polyunsaturated and monounsaturated fat decreasing the risk. Eating white rice excessively may increase the risk of diabetes, especially in Chinese and Japanese people. Adverse childhood experiences, including abuse, neglect, and household difficulties, increase the likelihood of type 2 diabetes later in life by 32%, with neglect having the strongest effect. Antipsychotic medication, SSRI, and SNRI side effects (specifically metabolic abnormalities, dyslipidemia and weight gain) are also potential risk factors.
Natural GnRH was previously prescribed as gonadorelin hydrochloride (Factrel) and gonadorelin diacetate tetrahydrate (Cystorelin) for use in treating human and dairy cattle diseases respectively. Modifications of the decapeptide structure of GnRH to increase half life have led to GnRH1 analog medications that either stimulate (GnRH1 agonists) or suppress (GnRH antagonists) the gonadotropins. These synthetic analogs have replaced the natural hormone in clinical use. Its analogue leuprorelin is used for continuous infusion, to treat breast cancer, endometriosis, prostate cancer, and following research in the 1980s by researchers, including Dr. Florence Comite of Yale University, it was used to treat precocious puberty. The expression of GnRH receptors in cancers has led to the use of GnRH as a targeting molecule to deliver toxins specifically to the receptor-expressing cancer cells. In a similar concept, its use to deliver toxins to pituitary gonadotropes in animals has been explored as a means of sterilization, with limited success. GnRH was also shown to successfully deliver DNA into the pituitary gonadotropes where the expressed protein blocked expression of the hormones that regulate reproduction. A Cochrane Review is available which investigates whether GnRH analogues, given before or alongside chemotherapy, could prevent damage to women's ovaries caused by chemotherapy. GnRH agonists appear to be effective in protecting the ovaries during chemotherapy, in terms of menstruation recovery or maintenance, premature ovarian failure and ovulation.
The concept of a steady state has relevance in many fields, in particular thermodynamics, economics, and engineering. If a system is in a steady state, then the recently observed behavior of the system will continue into the future. In stochastic systems, the probabilities that various states will be repeated will remain constant. For example, see Linear difference equation § Conversion to homogeneous form for the derivation of the steady state. In many systems, a steady state is not achieved until some time after the system is started or initiated. This initial situation is often identified as a transient state, start-up or warm-up period. For example, while the flow of fluid through a tube or electricity through a network could be in a steady state because there is a constant flow of fluid or electricity, a tank or capacitor being drained or filled with fluid is a system in transient state, because its volume of fluid changes with time. Often, a steady state is approached asymptotically. An unstable system is one that diverges from the steady state. See for example Linear difference equation#Stability. In chemistry, a steady state is a more general situation than dynamic equilibrium. While a dynamic equilibrium occurs when two or more reversible processes occur at the same rate, and such a system can be said to be in a steady state, a system that is in a steady state may not necessarily be in a state of dynamic equilibrium, because some of the processes involved are not reversible. In other words, dynamic equilibrium is just one manifestation of a steady state.
== External links == Center for Oral History. "Miguel A. Ondetti". Science History Institute. Bohning, James J. (12 January 1995). Miguel Angel Ondetti, Transcript of an Interview Conducted by James J. Bohning at Princeton, New Jersey on 12 January 1995 (PDF). Philadelphia, PA: Chemical Heritage Foundation. Hall of Fame, Inventor Profile: Miguel Ondetti
Sources: en.wikipedia.org
Load-induced non-rupture tendinopathy in humans is associated with an increase in the ratio of collagen III:I proteins, a shift from large to small diameter collagen fibrils, buckling of the collagen fascicles in the tendon extracellular matrix, and buckling of the tenocyte cells and their nuclei.
== Bibliography == Greenwood, Norman N.; Earnshaw, Alan (1997). Chemistry of the Elements (2nd ed.). Oxford: Butterworth-Heinemann. ISBN 978-0-08-037941-8. Holleman, Arnold F.; Wiberg, Nils (2007). Textbook of Inorganic Chemistry (102nd ed.). Berlin: de Gruyter. ISBN 978-3-11-017770-1. Peterson, J. R.; Hobart, D. E. (1984). "The Chemistry of Berkelium". In Emeléus, Harry Julius (ed.). Advances in inorganic chemistry and radiochemistry. Vol. 28. Academic Press. pp. 29–64. doi:10.1016/S0898-8838(08)60204-4. ISBN 978-0-12-023628-2.
As of the direct-to-video anniversary special Tokusou Sentai Dekaranger: 10 Years After, he has joined S.P.D.'s Earth unit and married Jasmine, with whom they have a son named Taiga. Hikaru Hiwatari is portrayed by Yuto Uemura (上村 祐翔, Uemura Yūto). Zamuzan Myra (ザムザ星人マイラ, Zamuza Seijin Maira): A young woman from Planet Zamuza who was the subject of a stakeout conducted by the Dekarangers due to her ex-boyfriend, an Alienizer named Sheik, having recently escaped from prison. However, Ban becomes enamored by her and goes undercover as her apartment building's plumber to socialize with her. After Sheik attacks Myra and the Dekarangers delete him, Myra loses respect for Ban for lying to her, but chooses to remain friends with him since he kept his promise to protect her. Myra is portrayed by Nana Nakamoto (中本 奈奈, Nakamoto Nana). Ocarnan Amy (オカーナ星人エイミー, Okāna Seijin Eimī): A giant alien baby from planet Ocarna who possesses currently uncontrollable size-changing capabilities limited by a special pacifier and shockwave-inducing cries. After Amy's cradle pod lands on Earth, Umeko is assigned to protect her until the former's parents can come for her. Agent Abrella sends an Igaroid to pilot a Kaijuki called Devil Capture 3 (デビルキャプチャー3, Debiru Kyapuchā Surī) and capture Amy, but Umeko destroys them with Dekaranger Robo before Amy's parents arrive and take their daughter back. Amy is voiced by Sara Nakayama (中山 さら, Nakayama Sara).
Singapore's urbanisation means that it has lost 95% of its historical forests, and now over half of the naturally occurring fauna and flora in Singapore is present in nature reserves, such as the Bukit Timah Nature Reserve and the Sungei Buloh Wetland Reserve, which comprise only 0.25% of Singapore's land area. In 1967, to combat this decline in natural space, the government introduced the vision of making Singapore a "garden city", aiming to improve quality of life. Since then, nearly 10% of Singapore's land has been set aside for parks and nature reserves. The government has created plans to preserve the country's remaining wildlife. Singapore's well known gardens include the Singapore Botanic Gardens, a tropical garden and Singapore's first UNESCO World Heritage Site.
The exact frequency of clubbing in the population is not known. A 2008 study found clubbing in 1%, or 15 patients, of 1511 patients admitted to a department of internal medicine in Belgium. Of these, 40%, or 6 patients, had significant underlying disease of various causes, while 60%, or nine patients, had no medical problems after further investigation and remained well over the subsequent year.
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.