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Background And Regulatory Status — Evidence Review

By Editorial Desk · published 2026-01-16 · last reviewed 2026-01-31 · Blog

PPARδ agonist comes up often in conversation and rarely with the context attached. Here we lay out the basics in order, then work through the practical considerations.

Updated 2026-01-31. Numbers and descriptions here follow the published literature rather than marketing material.

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.

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.

Background and Regulatory History

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 at a glance

PropertyValueNotes
IUPAC name{4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]phenoxy}acetic acidSystematic name for GW501516
CAS Registry Number317318-70-0Unique identifier for the parent compound
Molecular formulaC21H18F3NO3S2Includes carbon, hydrogen, fluorine, nitrogen, oxygen, and sulfur
Molecular weight453.5 g/molApproximate value for the neutral form
AppearanceWhite to off-white powderTypical description for purified laboratory material

Further detail

== Dosimetry == Therapeutic PRRT treatments typically involve several gigabecquerels (GBq) of activity. Several radiopharmaceuticals allow simultaneous imaging and therapy, enabling precise dosimetric estimates to be made. For example, the bremsstrahlung emission from 90Y and gamma emissions from 177Lu can be detected by a gamma camera. In other cases, imaging can be performed by labelling a suitable radionuclide to the same peptide as used for therapy. Radionuclides that can be used for imaging include gallium-68, technetium-99m and fluorine-18. Currently used peptides can result in high kidney doses, as the radiopharmaceutical is retained for relatively long periods. Renal protection is therefore used in some cases, taking the form of alternative substances that reduce the uptake of the kidneys.

Reactive neutrophilic cutaneous conditions constitute a spectrum of disease mediated by neutrophils, and typically associated with underlying diseases, such as inflammatory bowel disease and hematologic malignancy.

=== Diabetes mellitus === GCK mutations reduce the functional efficiency of the glucokinase molecule. Heterozygosity for alleles with reduced enzyme activity results in a higher threshold for insulin release and persistent, mild hyperglycemia. This condition is referred to as maturity onset diabetes of the young, type 2 (MODY2). The most recent overview of GCK mutation that were observed in patients claims 791 mutations, of which 489 are thought to cause the MODY diabetes and therefore reduce the functional efficiency of the glucokinase molecule. Homozygosity for GCK alleles with reduced function can cause severe congenital insulin deficiency, resulting in persistent neonatal diabetes.

=== Leaders of the Liberal Party === H. H. Asquith, 1st Earl of Oxford and Asquith, 1925 (1916–1926) Donald Maclean, Acting Leader (1919–1920) David Lloyd George (1926–1931) Sir Herbert Samuel (1931–1935) Sir Archibald Sinclair (1935–1945) Clement Davies (1945–1956) Jo Grimond (1956–1967) Jeremy Thorpe (1967–1976) Jo Grimond, Interim Leader (1976) David Steel (1976–1988)

Sources: en.wikipedia.org

Related pages on this site

Supporting material

Cannabidiol was isolated and identified from Cannabis sativa in 1940 by Roger Adams who was also the first to document the synthesis of THC (both delta-9-THC and delta-8-THC) from the acid-based cyclization of CBD in 1942. THC was first isolated from Cannabis in 1964.

== Conclusion == Ion milling revolutionized the fields of material engineering and mechanical engineering, allowing researchers and scientists to obtain high-quality specimens for advanced material analysis. Its applications in various industries and its role in advancing microelectronics make it an indispensable tool for modern research and development.

== Administration == Intravenous, usually 7.5 mg/kg every 8 hours (infections/life threatening VRSA); every 12 hours (skin infections). No renal dosing adjustments, hepatic dosing adjustments are not defined, consider reducing dose.

11 April – A study confirms antidepressant potential of psilocybin therapy protocols (which use the active ingredient in psilocybin mushrooms), providing fMRI data about a correlated likely major effect mechanism – global increases in brain network integration. 12 April – Science and the 2022 Russian invasion of Ukraine:An editorial in a scientific journal reports that relevant areas of food system research are patchy and lack independent assessments. An editorial projects significant gender and age imbalance in the population in Ukraine as a substantial problem if most refugees, as in other cases, do not return over time (4 Apr). A preprint reports impacts of the Ukrainian power grid synchronization with Continental Europe (15 Apr).

==== Iron import in some cancer cells ==== Iron can also enter cells via CD44 in complexes bound to hyaluronic acid during epithelial–mesenchymal transition (EMT). In this process, epithelial cells transform into mesenchymal cells with detachment from the basement membrane, to which they’re normally anchored, paving the way for the newly differentiated motile mesenchymal cells to begin migration away from the epithelial layer. While EMT plays a crucial role in physiological processes like implantation, where it enables the embryo to invade the endometrium to facilitate placental attachment, its dysregulation can also fuel the malignant spread of tumors empowering them to invade surrounding tissues and establish distant colonies (metastasis). Malignant cells often exhibit a heightened demand for iron, fueling their transition towards a more invasive mesenchymal state. This iron is necessary for the expression of mesenchymal genes, like those encoding transforming growth factor beta (TGF-β), crucial for EMT. Notably, iron’s unique ability to catalyze protein and DNA demethylation plays a vital role in this gene expression process. Conventional iron uptake pathways, such as those using the transferrin receptor 1 (TfR1), often prove insufficient to meet these elevated iron demands in cancer cells. As a result, various cytokines and growth factors trigger the upregulation of CD44, a surface molecule capable of internalizing iron bound to the hyaluronan complex.

Sources: en.wikipedia.org

Notes from published material

Korolev's design bureau produced two prospectuses for circumlunar spaceflight (March 1962 and May 1963), the main spacecraft for which were early versions of his Soyuz design. At the same time, another bureau, OKB-52, headed by Vladimir Chelomey, was developing the LK-1 lunar flyby spacecraft, which would be launched by Chelomey's Proton UR-500 rocket. The Soviet government rejected Korolev's proposals, opting to support Chelomey's project, who gained favor with Khrushchev by employing his son. Officially, the Soviet lunar program was established on August 3, 1964, with the adoption of Soviet Communist Party Central Committee Command 655-268 (On Work on the Exploration of the Moon and Mastery of Space). The circumlunar flights were planned to occur in 1967, and the landings to start in 1968, intending to land a person on the Moon before the Apollo flights. Both of the bureaus submitted their projects for a crewed lunar landing. Korolev's lunar landing program was designated N1/L3, for its N1 super rocket and a more advanced Soyuz 7K-L3 spacecraft, also known as the lunar orbital module ("Lunniy Orbitalny Korabl", LOK), with a crew of two. A separate lunar lander ("Lunniy Korabl", LK), would carry a single cosmonaut to the lunar surface. The N1/L3 launch vehicle had three stages to Earth orbit, a fourth stage for Earth departure, and a fifth stage for lunar landing assist. The combined space vehicle was roughly the same height and takeoff mass as the three-stage US Apollo-Saturn V and exceeded its takeoff thrust by 28% (45,400 kN vs. 33,000 kN.

The transport landscape of Pakistan features various modern transit systems. The Orange Line Metro Train in Lahore, inaugurated in 2020, spans 27.1 km (16.8 mi), and includes both elevated and underground sections, accommodating over 250,000 passengers daily. Lahore also boasts the Lahore Metrobus, the first of its kind in Pakistan, operational since February 2013. The Rawalpindi-Islamabad Metrobus, stretching 48.1 km, commenced its first phase in June 2015, with subsequent extensions, and employs e-ticketing and an Intelligent Transportation System. Multan Metrobus, inaugurated in January 2017, serves Multan with its rapid transit services. Peshawar's Bus Rapid Transit, inaugurated in August 2020, marks the fourth BRT system in Pakistan. Karachi's Green Line Metrobus, operational since December 2021, is part of a larger metrobus project financed by the Government of Pakistan and initiated in February 2016. Meanwhile, Faisalabad awaits its proposed rapid transit project, the Faisalabad Metrobus. Karachi Circular Railway, partially revived in November 2020, offers public transit services in the Karachi metropolitan area. Additionally, plans are underway to resurrect Karachi's tramway service, which ceased operations in 1975, in collaboration with Austrian experts. As of 2013, Pakistan boasts approximately 151 airports and airfields, encompassing both military and civilian installations.

== Mechanism of action == Lebrikizumab blocks interleukin 13 (IL-13), a cytokine (cell-signalling protein) that is produced by a type of white blood cell called Th2 cells. IL-13 is thought to induce the expression of another signalling protein, periostin, by epithelial cells of the bronchi. Periostin in turn seems to partake in a number of asthma related problems, such as bronchial hyperresponsiveness, inflammation, and activation and proliferation of airway fibroblasts, which are involved in airway remodelling. This theory is supported by the fact that people with high periostin levels responded significantly better to lebrikizumab in the phase II study: the forced expiratory volume in 1 second (FEV1) was 8.2% higher than under placebo in this group (measured from the respective baselines), while low-periostin participants had 1.6% higher FEV1, and the average value for all participants was 5.5%. The FEV1 increase in low-periostin participants was not statistically significant.

Second Cup was founded in 1975 by Tom Culligan and Frank O'Dea in Toronto, Ontario. Culligan eventually purchased O'Dea's shares and expanded Second Cup into a 150-store chain. He sold it in 1988 to the founder of mmmuffins, Michael Bregman. As chairman and CEO, Khalil Al Gawad took Second Cup public in 1993. Between 1993 and 2002, it was owned by several American companies, including Coffee Plantation, Coffee People, and Caribou Coffee. Al Gawad sold Second Cup to Cara Operations Limited in 2002. In November 2006, Cara sold Second Cup to Dinecorp Hospitality, controlled by former Cara CEO Gabe Tsampalieros, who became chairman of Second Cup. Tsampalieros died on March 11, 2009. The trademark rights were subsequently split between Canada (the Second Cup Ltd.) and international (the Second Cup Coffee Company Inc.). Stacey Mowbray was head of the Canadian company, and Jim Ragas led the international side. Second Cup was featured in an episode of Undercover Boss that aired in March 2012 on the W Network. Under Mowbray's direction, Second Cup was presented as "a company that cares". In September 2012, the company launched Tassimo beverages. In April 2015, Second Cup started a rewards program, which allows users to earn points using a mobile app. Alix Box was the CEO and president at Second Cup Ltd. from 2014 until her sudden departure, in May 2017; she was temporarily replaced by Garry MacDonald. On April 12, 2018, Bregman announced an agreement with National Access Cannabis to develop and convert a network of recreational cannabis stores.

Sources: en.wikipedia.org

Frequently asked questions

Is cardarine approved for human use?

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.

Why is cardarine banned in sport?

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.

What is the difference between cardarine and GW501516?

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.

Is cardarine a selective androgen receptor modulator?

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.

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