If you have been reading about PPARδ agonist 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 2025-12-12. Where a claim depends on a specific study, the study is described rather than over-claimed.
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.
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.
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 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.
| 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 |
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.
Safety discussions about cardarine frequently cite rodent carcinogenicity findings reported in the 2000s. In those studies, treated animals developed tumors at multiple sites, leading sponsors to discontinue clinical development. The relevance of these findings to humans has not been resolved, but they are a major reason the compound is not approved. Current literature emphasizes uncertainty about long-term effects and the risks of unregulated use. Regulators and health agencies have not established a safe human exposure level.
Cardarine is a synthetic compound also known as GW501516, GW-501516, and sometimes endurobol. It was developed as a selective agonist of peroxisome proliferator-activated receptor delta, a nuclear receptor involved in fatty acid oxidation and energy metabolism. The compound was studied in preclinical models for metabolic and cardiovascular conditions, but it did not become a marketed human medicine. In regulatory and anti-doping contexts, it is treated as a prohibited substance rather than a licensed medicine.
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.
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.
A geroprotector aims to affect the root cause of aging and age-related diseases, and thus prolong the life span of animals. Some possible geroprotectors include melatonin, carnosine, metformin, rapamycin, nicotinamide mononucleotide (NMN), delta sleep-inducing peptide,glycine, and psilocin. Geroprotectors could belong to multiple classes, depending on which of the hallmarks of aging they influence. The distinction between geroprotectors and senotherapeutics is an evolving area of aging research. Geroprotectors broadly aim to target multiple mechanisms of aging, prolonging lifespan and healthspan by addressing the fundamental causes of aging. Senotherapeutics, on the other hand, are a subset of therapies that specifically target senescent cells, which are dysfunctional cells that accumulate with age and contribute to inflammation and age-related diseases.
== DPP-4 mechanism == Fig.1: During a meal, the incretins glucagon-like peptide 1 (GLP-1) and glucose-dependent gastric inhibitory polypeptide (GIP) are released by the small intestine into the blood stream. These hormones regulate insulin secretion in a glucose-dependent manner. (GLP-1 has many roles in the human body. It stimulates insulin biosynthesis, inhibits glucagon secretion, slows gastric emptying, reduces appetite and stimulates regeneration of islet β-cells.) GLP-1 and GIP have extremely short plasma half-lives due to very rapid inactivation, catalyzed by the enzyme DPP-4. Inhibition of DPP-4 slows their inactivation, thereby potentiating their action, leading to lower plasma glucose levels, hence its utility in the treatment of type 2 diabetes. (Figure 1).
== Merchandising == The Guinness Storehouse at St. James's Gate Brewery in Dublin is the most popular tourist attraction in Ireland (attracting over 1.7 million visitors in 2019) where a self-guided tour includes an account of the ingredients used to make the stout and a description of how it is made. Visitors can sample the smells of each Guinness ingredient in the Tasting Rooms, which are coloured with a unique lighting design that emits Guinness's gold and black branding. The Guinness Book of Records started as a Guinness marketing giveaway, based on an idea of its then Managing Director, Sir Hugh Beaver. Its holding company, Guinness World Records Ltd, was owned by Guinness plc, subsequently Diageo, until 2001. The 2025 drama series House of Guinness deals with the growth of the business in 19th century Ireland.
==== Combine technology ==== The Combine use an arsenal of science fiction technologies. They have access to teleportation technology, which transports them between dimensions. However, their teleporter technology is restrictive in comparison to that developed by Eli Vance, Isaac Kleiner and Judith Mossman in that it cannot be used to teleport to other locations within the same dimension. Throughout the games, various futuristic computer consoles, doors, power sources and weapon emplacements are encountered. In addition, the Combine employ the use of robotic drones called city scanners, to observe the citizens of Earth. They monitor individuals and take photographs, while combat drones called shield scanners are used to drop mines. Civil Protection makes use of smaller drones called manhacks, which are equipped with razor-sharp rotating blades to attack targets with laceration injuries. These are often deployed in closed-in areas. The Combine also use two types of land mines; hopper mines throw themselves into the air and detonate when an enemy is detected nearby, while spherical rollermines roll towards vehicles or enemies, attach themselves and deliver electrical attacks. Combine technology is also used to transform humans into Overwatch soldiers or Stalkers, deformed and mutilated humans with no memory of their past selves who act as slaves and maintenance workers in Combine facilities. Transformation into a Stalker is considered among the Combine's worst punishments for dissidents.
where δ2HA is the delta value of pool A relative to VSMOW. As many delta values do not vary greatly from one another the α value is often very close to unity. A related measure called epsilon (ε) is often used which is given simply by:
Sources: en.wikipedia.org
==== Bill 5 ==== Many Indigenous and environmental advocacy groups opposed his government's Protecting Ontario by Unleashing Our Economy Act, or Bill 5, which gives Ford's cabinet the ability to create special economic zones and exempt companies or projects from having to comply with any provincial law, provincial regulation or municipal bylaw. Ford also apologized for saying that First Nations "keep coming hat in hand" for government money in June 2025.
=== Designation process === The NIH funds cancer centers through a P30 Cancer Center Support Grant (CCSG) mechanism. To be eligible to apply, a cancer center must receive at least $10 million in cancer research funding annually. Preparation for these grant applications can be extensive. The most recent grant application prepared by MD Anderson Cancer Center took 24 months to prepare and ran to 2,963 pages. Cancer centers must renew their status with the NIH every 5 years. The NCI considers the certain characteristics essential to a cancer center, and requires that applications address the institutions' resources in the areas of: Physical Space, Organizational Capabilities, Transdisciplinary Collaboration and Coordination, Cancer Focus, Institutional Commitment, Center Director. Independent or freestanding cancer centers are entities unto themselves and are not considered to be part of a larger institution or university. The center’s administration controls all space, appointments and budgets. These institutions may have university affiliations, but they remain administratively and financially distinct. The NCI also supports Consortium Centers, wherein scientists and clinicians from multiple institutions enter into formal agreements to expand cancer research programs. Importantly, Consortium Partners are not themselves considered NCI-designated. The NCI has strict guidelines on how Consortium Partners can refer to their relationship with their parent Consortium Center.
In the US, esketamine (brand name Spravato) is a nasal spray indicated, as monotherapy, or in conjunction with an oral antidepressant as a therapy for treatment-resistant depression (TRD) as well as major depressive disorder (MDD) associated with suicidal ideation or behavior in adults. In the clinical trials that led to approval of esketamine, TRD was defined as major depressive disorder with inadequate response to at least two different conventional antidepressants. The nasal spray formulation of esketamine used for depression delivers two sprays containing a total of 28 mg esketamine and doses of 56 mg (2 devices) to 84 mg (3 devices) are used. Esketamine has modest short-term efficacy on TRD (similar in efficacy to atypical antipsychotics); there is limited long-term safety data available and some concerning signals regarding adverse events and abuse potential. Due to concerns about sedation, dissociation, and misuse, esketamine is available for treatment of depression only from certified providers through a restricted program under a Risk Evaluation and Mitigation Strategy (REMS) called Spravato REMS.
== Medical uses == Metenolone, as its esters, is used almost exclusively in the treatment of anemia due to bone marrow failure. It has also been used to treat wasting syndromes due to major surgery, infection, long-term corticosteroid therapy, malnutrition, or other causes. It has also been used to treat osteoporosis and sarcopenia, to inhibit the natural loss of muscle mass with aging, and to promote weight gain in underweight premature infants and children.
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.
Legal status varies by country. It is not approved as a medicine, and it is prohibited in sport. Some jurisdictions restrict import, sale, or possession.