This is a working overview of Cardarine, written for readers who want more than a one-paragraph summary but less than a textbook.
This page was last updated on 2025-08-22 and is reviewed periodically as new material appears.
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.
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.
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.
| Property | Value | Notes |
|---|---|---|
| Common name | Cardarine | Common internet and media name. |
| Research code | GW501516 | Also written GW-1516. |
| Drug class | PPARδ agonist | Not a selective androgen receptor modulator. |
| Development status | Discontinued | Clinical development halted after rodent cancer findings. |
| Regulatory status | Prohibited in sport | Listed by WADA; not approved as medicine. |
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.
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.
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.
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.
=== Regulatory role in cell differentiation === In addition to its well-known role as a cellular energy source, glucose has been identified as a master regulator of tissue maturation. A 2025 study by Stanford Medicine uncovered that glucose, in its intact (non-metabolized) form, can bind to various regulatory proteins involved in gene expression. One such protein is IRF6, which alters its conformation upon glucose binding, thereby influencing the expression of genes associated with stem cell differentiation. This regulatory role is independent of glucose's catabolic function and has been observed across multiple tissue types, including skin, bone, fat, and white blood cells. The research demonstrated that even glucose analogs incapable of metabolism could promote differentiation, suggesting a signaling function for glucose. These findings have potential implications in understanding and treating diseases characterized by impaired differentiation, such as diabetes and certain cancers.
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==== Amputations ==== Save the Children reported 10 children a day in Gaza had lost their limbs, which would result in a lifetime of medical needs. A UNICEF spokesperson James Elder was quoted after returning from Gaza in mid-December 2023, that around 1,000 children had lost one or both legs since the 7 October attacks and the start of the war. According to the British doctor Ghassan Abu-Sittah, "This is the biggest cohort of pediatric amputees in history". In mid-December 2023, a teenager's amputation performed without anesthesia on her families kitchen table by her uncle who is a doctor went viral on social media. She and a sibling had climbed to the top of the building to call their father who is overseas before the building was reportedly struck by IDF tank fire, and she was rushed inside to her uncle. In early-January 2024, an 11-year-old speaking to reporters about her injuries which included an amputated leg and with the other severely injured expressed her hope in getting an artificial limb, and lamented how her life has become "ugly and sad" after the injury. Other children's stumps after amputation had to be re-opened after infections had set in. By June 2024, doctors in Gaza estimated as many as 3,000 children had lost limbs since October 2023. A WHO Emergency Medical Team coordinator also cautioned that due to lack of medical expertise and time, some of the amputations done were unnecessary or due to a time delay. The head of Humanity & Inclusion stated child amputees needed "immediate support" for prosthetics but that wasn't happening.
Sources: en.wikipedia.org
== Manufacturing == It is frequently sold as a sulfate salt known as hydroxychloroquine sulfate. In the sulfate salt form, 200 mg is equal to 155 mg of the pure form. Brand names of hydroxychloroquine include Plaquenil, Hydroquin, Axemal (in India), Dolquine, Quensyl, and Quinoric.
Because testing methods differ between laboratories, reference ranges may vary. A positive anti-U1 RNP antibody test should always be interpreted together with a patient's symptoms and other significant research.
=== Pharmacokinetics === Suzetrigine is well-absorbed from the GI tract, with the 50mg maintenance dose being relatively unaffected by meal timing, and the 100mg initial dose requiring an empty stomach for proper absorption. Suzetrigine has a mean effective half-life of 23.6 hours and is 99% protein-bound; its active metabolite, M6-SUZ, has a mean effective half-life of 33 hours and is 96% protein-bound. Steady-state concentrations are reached within 3 days. The primary metabolic pathway is via CYP3A isozymes, followed by excretion via feces (49.9%) and urine (44%). Suzetrigine may potentially interact with certain hormonal birth controls, resulting in reduced efficacy. During clinical trials, it was observed that the efficacy of levonorgestrel and ethinyl estradiol were not reduced by suzetrigine administration, and can be safely used together.
Sources: en.wikipedia.org
=== Republic of Zimbabwe (1980) === On 18 April 1980, the country became independent within the Commonwealth of Nations as the Republic of Zimbabwe, and its capital, Salisbury, was renamed Harare two years later.
==== MeSH D12.776.422.220.286 – cytochrome c group ==== MeSH D12.776.422.220.286.100 – cytochromes c MeSH D12.776.422.220.286.150 – cytochromes c' MeSH D12.776.422.220.286.200 – cytochromes c1 MeSH D12.776.422.220.286.300 – cytochromes c2 MeSH D12.776.422.220.286.600 – cytochromes c6
=== Recreational use === Illicit use of pharmaceutical fentanyl and its analogues first appeared in the mid-1970s in the medical community and continues in the present. More than 12 different analogues of fentanyl, all unapproved and clandestinely produced, have been identified in the U.S. drug traffic. In February 2018, the US Drug Enforcement Administration indicated that illicit fentanyl analogs have no medically valid use, and thus applied a "Schedule I" classification to them. Fentanyl analogues may be hundreds of times more potent than heroin. Fentanyl is used orally, smoked, snorted, or injected. Fentanyl is sometimes sold as heroin or oxycodone, which can lead to overdose. Many fentanyl overdoses are initially classified as heroin overdoses. Estonia has the highest rate of 3-methylfentanyl overdose deaths in the EU, due to its high rate of recreational use. Another form of fentanyl that has appeared on the streets is the Actiq lollipop formulation. The pharmacy retail price ranges from US$15 to US$50 per unit based on the strength of the lozenge, with the black market cost ranging from US$5 to US$25 in 2007, depending on the dose. The attorneys general of Connecticut and Pennsylvania have launched investigations into its diversion from the legitimate pharmaceutical market, including Cephalon's "sales and promotional practices for Provigil, Actiq and Gabitril." Non-medical use of fentanyl by individuals without opioid tolerance can be very dangerous and has resulted in numerous deaths. Even those with opiate tolerances are at high risk for overdoses.
=== Research parks and commercialization === Tech Parks Arizona is the research park of the University of Arizona. It comprises three primary facilities: the UA Tech Park at Rita Road, the UA Tech Park at The Bridges, and the University of Arizona Center for Innovation (UACI).
Sources: en.wikipedia.org
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.
Preclinical rodent studies reported cancers, including liver and bladder tumors, at tested doses. The human relevance of those findings is uncertain, but development was discontinued. No approved human product resulted.
No. It remains an investigational compound without approved therapeutic labeling. Sports regulators prohibit its use, and health agencies have warned against consuming it.
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.