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Cardarine As Investigational Pparδ Agonist — 2026 Update

By Editorial Desk · published 2026-02-16 · last reviewed 2026-04-07 · Topic

PPARδ agonist raises a handful of sensible questions. This page answers them in order, starting with the fundamentals and moving to applications.

This page was last updated on 2026-04-07 and is reviewed periodically as new material appears.

Cardarine as Investigational PPARδ Agonist

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.

Mechanism and Detection

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 at a glance

PropertyValueNotes
Common synonymsGW501516, GW-501516, GW 501516, endurobolNames vary in research and anti-doping documents.
Chemical classSynthetic PPARδ agonistSmall-molecule nuclear receptor ligand.
CAS Registry Number317318-70-0Identifier commonly associated with GW501516.
AppearanceWhite to off-white powderTypical for purified research material.
SolubilityLow in water; soluble in DMSO and ethanolOrganic solvents are common for laboratory stock solutions.

Regulation and Detection

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.

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Background and Regulatory Status

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.

Notes from published material

== Role in cancer == Studies indicate significant HB-EGF gene expression elevation in a number of human cancers as well as cancer-derived cell lines. Evidence indicates that HB-EGF plays a significant role in the development of malignant phenotypes contributing to the metastatic and invasive behaviors of tumors. The proliferative and chemotactic effects of HB-EGF results from the target influence on particular cells including fibroblasts, smooth muscles cells, and keratinocytes. For numerous cell types such as breast and ovarian tumor cells, human epithelial cells and keratinocytes HB-EGF is a potent mitogen resulting in evidenced upregulation of HB-EGF in such specimens. Both in vivo and in vitro studies of tumor formation in cancer derived cell lines indicate that expression of HB-EGF is essential for tumor development. As a result, studies implementing the use of specific HB-EGF inhibitors and monoclonal antibodies against HB-EGF show the potential for the development of novel therapies for treating cancers by targeting HB-EGF expression.

== Early life == Jones was born in Cincinnati, Ohio on May 17, 1893, to an Irish father and Black American mother. Little is known about his mother who left his life when Jones was a child. His father, John Jones, was a railroad worker who struggled to raise him on his own. Jones was raised by a Catholic priest, Father Ryan, at a rectory in Cincinnati, Ohio, near Covington. Father Ryan took in Jones around the age of seven, and two years later, John Jones died. Jones left school at age 11 after the sixth grade. He went to nearby Cincinnati, Ohio, working odd jobs including a role as a garage cleaning boy. By age 14, Jones was working as an automobile mechanic and was later named garage foreman. Jones was largely self taught.

== History == The practice of salting fish dates back to ancient times. In classical antiquity, the town of Magdala on the Sea of Galilee, located in present-day Israel, was also known by its Greek name, Taricheae, meaning "place of fish salting." The Greek geographer Strabo even praised the quality of its fish (Geographica 16.2.45).

Five years later, GSK shuttered the Sirtris program without successful drug development. In 2006, Sinclair co-founded Genocea Biosciences, a company founded based on the work of Harvard scientist Darren E. Higgins around antigens that stimulate T cells and the use of these antigens to create vaccines; The company delisted from the NASDAQ and closed in 2022 due to lack of funding. In 2008, Sinclair was promoted to tenured professor at Harvard Medical School. A few years later, he also became a conjoint professor at the School of Medical Sciences at the University of New South Wales. In 2008, he also joined the scientific advisory board of Shaklee and helped them devise and introduce a product containing resveratrol called "Vivix". He later disputed the use of his name and words to promote the supplement, and resigned from the board. In 2011, Sinclair co-founded OvaScience along with Michelle Dipp, Aldrich, Westphal, and Jonathan Tilly. The company was based on scientific work done by Tilly concerning mammalian oogonial stem cells and work on mitochondria by Sinclair. The company merged with Millendo Therapeutics in 2018. In 2011, he also co-founded CohBar along with Nir Barzilai and other colleagues. CohBar aimed to discover and develop novel peptides derived from mitochondria. CohBar delisted from the NASDAQ upon belief that it was a public shell. In 2015, he co-founded Metro Biotech along with Washington University in St. Louis professor Dr. Rajendra Apte. The pharmaceutical company focused on NAD+ precursors such as NMN.

Sources: en.wikipedia.org

Background from the literature

=== Protection of the wall === The Berlin Wall was made up of two walls. Both walls were 4 metres tall and had a length of 155 kilometres. They were separated by a mined corridor called the death strip. This strip was heavily guarded and included 302 watchtowers (by 1989). Guards had authorization to shoot people who attempted to go through this strip.

The United States House of Representatives passes a bill to curb university boycotts of Israel. OpenAI launches GPT-6, the next major version of ChatGPT. The National Fish and Wildlife Foundation announces $1.2 million in grants to reduce the extinction risk for Hawaiian forest birds and restore essential watershed habitats in Hawaii. September 4 The US military announces that it had disabled ad trackers on devices following reports that commercially available location data had been used to target its soldiers in the Middle East. The judge in the trial of Lindsay Clancy, a mother accused of murdering her three children, says he will declare a mistrial. The US Treasury announces that it has cut off Turkish investment bank Golden Global Yatirim Bankasi Anonim Sirketi and two subsidiaries from dollar transactions because of their dealings with the Iranian government. The price of diesel hits an all-time high of $5.85 per gallon, compared to an average of $3.71 a year ago and exceeding the previous high following Russia's full-scale invasion of Ukraine. September 5 The US military reports that it destroyed three IRGC-connected oil tankers in response to the latter's fire on its warships. Steve Witkoff and Jared Kushner meet Russian president Vladimir Putin in Moscow to deliver a proposal to end the war in Ukraine. In college football, ESPN College GameDay announces the inaugural "Hall of Fan" award, with the Ol’ Crimson flag from the Washington State Cougars as its first inductee.

The 5,10-methenyltetrahydromethanopterin hydrogenase (or Hmd), the so-called iron-sulfur cluster-free hydrogenase, is an enzyme found in methanogenic archea such as Methanothermobacter marburgensis. It was discovered and first characterized by the Thauer group at the Max Planck Institute in Marburg. Hydrogenases are enzymes that either reduce protons or oxidize molecular dihydrogen.

Transuranium elements do not occur in sizeable quantities in nature and are commonly synthesized via nuclear reactions conducted with nuclear reactors. For example, under irradiation with reactor neutrons, uranium-238 partially converts to plutonium-239:

4 On 21 December 1995, a major reshuffle took place amongst existing Ministers, mainly to discharge particular Ministers of portfolios which had proven troublesome for the government. 5 On 26 April 1996, George Cash resigned from the ministry due to ill health. Graham Kierath and Kevin Minson adopted his portfolios, whilst Norman Moore was elected leader of the Government in the Legislative Council four days later.

Sources: en.wikipedia.org

Reference notes

The team is commonly known as Los Cafeteros ("The Coffee Growers"), after Colombia's coffee industry, and as La Tricolor, after the yellow, blue and red of the national flag. The Colombian state broadcaster's archive service has described the shirt as having become "a new national symbol", worn across regions and social classes on match days. Colombia's yellow shirt, blue shorts and red socks are a relatively recent settlement rather than an inherited palette. Early sides alternated white and blue, with white worn at the 1945 South American Championship and dark blue at the 1962 FIFA World Cup. From 1971 the team wore orange, known domestically as zapote. In 1985 the Colombian Football Federation commissioned the designer María Elvira Pardo to base a kit on the national flag; her design made red the first-choice shirt, worn through the 1990 FIFA World Cup, with yellow as the alternative. Yellow was promoted to first choice in the early 1990s. Subsequent departures have been tournament-specific: a red change kit at the 2014 FIFA World Cup referencing the 1990s alternates, and a white first-choice shirt at the Copa América Centenario echoing the 1945 side. Adidas has supplied the team since January 2011 under an agreement signed in November 2010, subsequently extended to 2030; earlier suppliers included Le Coq Sportif, Adidas, Puma, Kelme, Umbro, Reebok and Lotto.

C57BL/6 mice have a dark brown, nearly black coat. They are more sensitive to noise and odours and are more likely to bite than the more docile laboratory strains such as BALB/c. Group-housed C57BL/6 mice (and other strains) display barbering behaviour, which used to be seen as a sign of dominance. However, it is now known that this is more of a stereotypical behaviour triggered by stress, comparable to trichotillomania in humans or feather plucking in parrots. Mice that have been barbered extensively can have large bald patches on their bodies, commonly around the head, snout, and shoulders, although barbering may appear anywhere on the body. Also self-barbering can occur. Both hair and vibrissae may be removed. Barbering is more frequently seen in female mice; male mice are more likely to display dominance through fighting. C57BL/6 has several unusual characteristics which make it useful for some research studies but inappropriate for others: It is unusually sensitive to pain and to cold, and analgesic medications are less effective in this strain. Unlike most laboratory mouse strains, the C57BL/6 drinks alcoholic beverages voluntarily. It is more susceptible than average to morphine addiction, atherosclerosis, and age-related hearing loss. When compared directly to BALB/c mice, C57BL/6 mice also express both a robust response to social rewards and empathy.

Although districts are not formally designated by income, areas closer to the city center, metro stations, or green zones are considered more prestigious. Moscow also contains some government bodies of the Moscow Oblast, although the city is not part of the oblast.

The mechanism by which toxicity results is complex, but is believed to involve reaction between unconjugated NAPQI and critical proteins as well as increased susceptibility to oxidative stress caused by the depletion of glutathione.

AB-103 is a minoxidil sulfotransferase stimulant which is under development for the treatment of alopecia (hair loss) as an adjunct to the hair loss drug minoxidil. It is used topically. The drug works by stimulating the enzyme SULT1A1 in hair follicles which converts minoxidil into its active form minoxidil sulfate and which has been found to predict minoxidil's clinical effectiveness. It was originated by Applied Biology and is under development by Safety Shot. As of February 2024, AB-103 is in phase 3 clinical trials for treatment of alopecia. It has been in this stage of development since at least April 2019, but there have been no more recent updates on its development since then. The chemical structure of AB-103 does not yet appear to have been disclosed.

Sources: en.wikipedia.org

Frequently asked questions

What is cardarine?

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.

Is cardarine a steroid?

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.

Why was cardarine not developed further?

Early rodent studies reported tumor formation at multiple sites, which raised safety concerns. Sponsors stopped clinical development, and no approved human product exists.

How does cardarine work in the body?

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.

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