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.
Updated 2026-01-29. Numbers and descriptions here follow the published literature rather than marketing material.
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.
The pharmacological interest in cardarine centers on PPARδ activation and its downstream effects on lipid handling and mitochondrial function. In animal studies, PPARδ agonists have been associated with changes in exercise endurance and fatty acid utilization, though results vary by model and protocol. Human data remain sparse, and the absence of large controlled trials limits conclusions about efficacy. Researchers often describe the compound as a tool for probing PPARδ biology rather than a proven therapeutic agent.
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.
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.
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.
| Property | Value | Notes |
|---|---|---|
| Common synonyms | GW501516, GW-501516, GW 501516, endurobol | Names vary in research and anti-doping documents. |
| Chemical class | Synthetic PPARδ agonist | Small-molecule nuclear receptor ligand. |
| CAS Registry Number | 317318-70-0 | Identifier commonly associated with GW501516. |
| Appearance | White to off-white powder | Typical for purified research material. |
| Solubility | Low in water; soluble in DMSO and ethanol | Organic solvents are common for laboratory stock solutions. |
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.
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.
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 binds and activates PPARδ, a nuclear receptor that influences transcription of genes involved in fatty acid oxidation and energy use. Activation shifts some metabolic pathways in preclinical models, which is why the compound has been studied for lipid disorders and exercise-related endpoints. The exact downstream effects in humans are incompletely mapped. PPARδ is expressed in many tissues, including skeletal muscle, liver, and adipose tissue, so broad activation may have varied consequences. Researchers continue to examine how selective or partial activation might alter the balance between benefits and risks.
== Biosynthesis == The DNA sequence of these transporters is transcribed in the nucleus of the cell by RNA polymerase and undergoes splicing and capping before it travels to the cytoplasm. In the cytoplasm, translation begins via a sequence in exon 2 of the mRNA. Subsequently, protein folding and packaging insert the transporter into the membrane. The protein has a signal recognition particle that is recognized as it leaves the ribosome. N-glycosylation at various sites on hPAT1 is necessary for its transport function. Three of its extracellular residues are glycosylated and determine transport efficacy.
== Pyrogen removal (depyrogenation) == Pyrogens can often be difficult to remove from solution due to the high variability of their molecular weight. Pyrogens are also relatively thermally stable and insensitive to pH changes. However, several removal techniques exist.
Reptilian skin is covered in a horny cornified epidermis, making it watertight and enabling reptiles to live on dry land, in contrast to amphibians. Compared to mammalian skin, that of reptiles is rather thin and lacks the thick dermal layer that produces leather in mammals. The scaly skin typical of reptiles was likely inherited from the mutual common ancestor of amniotes, as early synapsids (as well as close relatives of amniotes like diadectomorphs) also had scaly reptile-like skin. This epidermis has differentiated alpha- and beta-keratin layers. Reptile skin varies from being highly pliable (snakes, geckoes) to inflexible (crocodilians, many turtles, many lepidosaurs) and the scales from highly overlapping (skinks and snakes) to having very little overlap (crocodilians, geckoes and agamids). Some areas of the body may not covered in scales (such as large areas of the body in turtles), but still generally have a rough appearance. Large plate-like scales, such as those covering the shells of turtles and the bodies of crocodilians, are referred to as scutes. The tips of reptile digits are generally capped with hard, curved cornified claws.
An individual who both initiates and conducts, alone or with others, a clinical trial, and under whose immediate direction the investigational product is administered to, dispensed to, or used by a subject. The term does not include any person other than an individual (e.g., it does not include a corporation or an agency). The obligations of a sponsor-investigator include both those of a sponsor and those of an investigator. (ICH E6) An individual who both initiates and actually conducts, alone or with others, a clinical investigation, i.e., under whose immediate direction the test article is administered or dispensed to, or used involving, a subject. The term does not include any person other than an individual, e.g., corporation or agency. (21CFR50.3) Standard treatment
Sources: en.wikipedia.org
anhydrous Having or containing no water molecules, referring especially to water of hydration. Because many processes in chemistry are impeded in the presence of water, it is often of critical importance that water-free reagents and techniques are used. Anhydrous compounds tend to gradually absorb water from the atmosphere. Contrast hydrous.
For services to the community in Riseley, Bedfordshire. Christine Mary Gendall. For services to the community in Penzance, Cornwall. Terence Brian Gerry. For services to the community in Plymouth, Devon. Beth Laura Gevell. Co-Founder and Director, Arts for Life Project (UK). For services to Young People and to Charity. Amanda Elizabeth Giddins. Chair, Giddo's Gift. For voluntary and charitable services to Young People with Cancer. Kenneth Matthew Gillespie. For services to Young People through Scouting. James Bruce Gillett. For services to the community in Charvil and Reading, Berkshire. Janet Elizabeth Gloin. Manager and Coach, Women's Football, Orpington Football Club. For services to Association Football and to the community in the London Borough of Bromley. Geoffery Frederick Bewick Goldsbrough. Founder, Perennials Charity Rugby Club. For services to Charity in Northern Ireland. Sarah Louise Goodall. Watch Manager, West Yorkshire Fire and Rescue Service. For services to Fire and Rescue. Susan Joy Graham. Chair, Age UK Milton Keynes. For services to Older People in Milton Keynes and Buckinghamshire. Marc Anthony Grayston. Chief Instructor, Maru Karate Kai. For services to Disadvantaged Young People and to the community in Basildon, Essex. Beverley Michelle Greenwood. For services to the community in Glenfield, Leicestershire during Covid-19. Rachael Greenwood. For services to the community in Bramdean and Hinton Ampner, Hampshire. Richard Gregory. For services to the community in Basildon, Essex. Harbaksh Singh Grewal. Vice Chair, UK Punjab Heritage Association.
== Global Health Partnerships == CLSI provides direct assistance in Sub-Saharan Africa to combat HIV/AIDS and other infectious diseases. With grants from the US-based PEPFAR (President's Emergency Plan for AIDS Relief) program administered by a cooperative agreement from the Centers for Disease Control and Prevention (CDC) and the National Institute of Allergy and Infectious Diseases (NIAID), CLSI has worked on essential laboratory services. CLSI has provided technical assistance in Côte d'Ivoire, Democratic Republic of the Congo, Dominican Republic, Ethiopia, Georgia, Ghana, Kazakhstan, Kenya, Kyrgyzstan, Malawi, Mali, Mozambique, Namibia, Nigeria, Peru, Rwanda, Tajikistan, Tanzania, Ukraine, Vietnam, and Zambia.
=== β-Adrenergic receptor antagonism === Stimulation of β1 receptors by epinephrine and norepinephrine induces a positive chronotropic and inotropic effect on the heart and increases cardiac conduction velocity and automaticity. Stimulation of β1 receptors on the kidney causes renin release. Stimulation of β2 receptors induces smooth muscle relaxation, induces tremor in skeletal muscle, and increases glycogenolysis in the liver and skeletal muscle. Stimulation of β3 receptors induces lipolysis. Beta blockers inhibit these normal epinephrine- and norepinephrine-mediated sympathetic actions, but have minimal effect on resting subjects. That is, they reduce the effect of excitement or physical exertion on heart rate and force of contraction, and also tremor, and breakdown of glycogen. Beta blockers can have a constricting effect on the bronchi of the lungs, possibly worsening or causing asthma symptoms. Since β2 adrenergic receptors can cause vascular smooth muscle dilation, beta blockers may cause some vasoconstriction. However, this effect tends to be small because the activity of β2 receptors is overshadowed by the more dominant vasoconstricting α1 receptors. By far the greatest effect of beta blockers remains in the heart. Newer, third-generation beta blockers can cause vasodilation through blockade of alpha-adrenergic receptors. Accordingly, nonselective beta blockers are expected to have antihypertensive effects.
== Medical uses == In the US, sirolimus, as Rapamune, is indicated for the prevention of organ transplant rejection and for the treatment of lymphangioleiomyomatosis; and, as Fyarro, in the form of protein-bound particles, for the treatment of adults with locally advanced unresectable or metastatic malignant perivascular epithelioid cell tumour (PEComa). In the EU, sirolimus, as Rapamune, is indicated for the prophylaxis of organ rejection in adults at low to moderate immunological risk receiving a renal transplant and for the treatment of people with sporadic lymphangioleiomyomatosis with moderate lung disease or declining lung function; and, as Hyftor, for the treatment of facial angiofibroma associated with tuberous sclerosis complex.
Sources: en.wikipedia.org
Cardarine is an investigational synthetic compound that acts as a PPARδ agonist. It is also known as GW501516 and has been studied mainly in preclinical research. It is not an approved medicine.
No. Cardarine is not a steroid hormone; it targets the nuclear receptor PPARδ. Its classification in anti-doping rules differs from anabolic steroids, though it remains prohibited in sport.
Early rodent studies reported tumor formation at multiple sites, which raised safety concerns. Sponsors stopped clinical development, and no approved human product exists.
Cardarine is a common name for GW501516, a synthetic PPARδ agonist developed for research. It has not been approved as a medication in any country. It is classified as an unapproved drug and a prohibited substance in sport.