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Background And Regulatory History — Beginner to Advanced

By Editorial Desk · published 2025-07-24 · last reviewed 2025-08-07 · Data

fatty acid oxidation is one of those subjects where the details matter more than the headlines. This page pulls together the background, the mechanisms, and the practical points readers ask about most.

Updated 2025-08-07. Numbers and descriptions here follow the published literature rather than marketing material.

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.

Identity and Regulatory Status

Clinical development stopped after rodent studies showed tumors at multiple sites. Whether those findings predict human cancer risk remains an open question, but they led sponsors to discontinue programs. Human safety data are limited to small, short-term studies that were not designed to assess cancer risk. Reported effects in those studies included changes in blood lipids, but the evidence is insufficient for medical use. Long-term consequences of nonmedical use are not well characterized. Questions about dose, duration, and individual susceptibility remain unresolved.

Cardarine is a common name for GW501516, an investigational compound developed in the 1990s for metabolic conditions. It acts as an agonist at peroxisome proliferator-activated receptor delta, a nuclear receptor involved in lipid and energy metabolism. The compound is frequently mislabeled as a selective androgen receptor modulator, or SARM, but its molecular target is different. GW501516 reached early clinical testing before development was discontinued. It has no approved therapeutic use in any country. The name cardarine is not a formal international nonproprietary name.

Cardarine at a glance

PropertyValueNotes
Common nameCardarineCommon internet and media name.
Research codeGW501516Also written GW-1516.
Drug classPPARδ agonistNot a selective androgen receptor modulator.
Development statusDiscontinuedClinical development halted after rodent cancer findings.
Regulatory statusProhibited in sportListed by WADA; not approved as medicine.

Mechanism and Detection Methods

Detection of GW501516 in biological samples generally relies on liquid chromatography coupled with tandem mass spectrometry. Urine is a common matrix in anti-doping analysis, while blood or plasma may be used in research settings. Sample preparation can involve enzymatic hydrolysis, protein precipitation, or solid-phase extraction before instrumental analysis. Because the compound undergoes metabolism, assays may target the parent molecule, one or more metabolites, or both. Detection windows are not fixed; they depend on factors such as dose, route, individual metabolism, and assay sensitivity. Reference standards are required for accurate identification and quantification.

Handling and quality assessment of cardarine reference material follow general laboratory practices for poorly characterized compounds. It typically appears as a white to off-white powder and is sparingly soluble in water but soluble in organic solvents such as dimethyl sulfoxide and ethanol. Storage recommendations usually specify a cool, dry, dark place, with long-term storage at low temperature and desiccation. Purity may be checked by high-performance liquid chromatography with ultraviolet detection, while identity is confirmed by mass spectrometry and nuclear magnetic resonance. No pharmacopeial monograph exists, so reported purity and stability depend on the supplier’s methods.

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Mechanism and Research Context

GW501516 acts as an agonist at peroxisome proliferator-activated receptor delta, a nuclear receptor involved in transcription of genes related to lipid handling and energy use. Activation of PPARδ can shift skeletal muscle toward greater fatty acid oxidation in animal models, which is one reason it drew interest for metabolic disease and exercise research. The exact downstream effects depend on tissue, species, dose, and duration. Human data are sparse, so many proposed benefits remain hypotheses rather than established clinical outcomes.

Laboratory studies have examined GW501516 in cell cultures and rodents for conditions such as dyslipidemia, insulin resistance, and obesity. Some trials in humans were initiated, but development was discontinued after preclinical findings raised concerns about cancer in certain models. Those findings do not prove that the compound causes cancer in people, but they contributed to regulatory caution. Later reviews often describe the evidence as preliminary and insufficient for assessing long-term safety.

Regulation and Detection

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.

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.

Reference notes

The Peruvian government declares that an ENSO Costero is under way if the sea surface temperature deviation in the Niño 1+2 regions equal or exceed 0.4 °C (0.72 °F) for at least three months. The United Kingdom's Met Office also uses a several month period to determine ENSO state. When this warming or cooling occurs for only seven to nine months, it is classified as El Niño/La Niña "conditions"; when it occurs for more than that period, it is classified as El Niño/La Niña "episodes". The India Meteorological Department (IMD) incorporates ENSO monitoring into its operational forecasting framework, as ENSO is one of the principal drivers of interannual variability in the Indian summer monsoon. According to the IMD, ENSO conditions are assessed alongside the Indian Ocean Dipole (IOD) using surface and upper-air observations, satellite and radar data, ocean observations and numerical weather prediction models.

Accurate radiometric dating generally requires that the parent has a long enough half-life that it will be present in significant amounts at the time of measurement (except as described below under "Dating with short-lived extinct radionuclides"), the half-life of the parent is accurately known, and enough of the daughter product is produced to be accurately measured and distinguished from the initial amount of the daughter present in the material. The procedures used to isolate and analyze the parent and daughter nuclides must be precise and accurate. This normally involves isotope-ratio mass spectrometry. The precision of a dating method depends in part on the half-life of the radioactive isotope involved. For instance, carbon-14 has a half-life of 5,730 years. After an organism has been dead for 60,000 years, so little carbon-14 is left that accurate dating cannot be established. On the other hand, the concentration of carbon-14 falls off so steeply that the age of relatively young remains can be determined precisely to within a few decades.

=== Interaction with nucleic acids === One of the important properties of lactoferrin is its ability to bind with nucleic acids. The fraction of protein extracted from milk, contains 3.3% RNA, but, the protein preferably binds to double-stranded DNA rather than single-stranded DNA. The ability of lactoferrin to bind DNA is used for its isolation and purification using affinity chromatography with columns containing immobilized DNA-containing sorbents, such as agarose with the immobilized single-stranded DNA.

== Further reading == Görlich D (Jun 1997). "Nuclear protein import". Current Opinion in Cell Biology. 9 (3): 412–9. doi:10.1016/S0955-0674(97)80015-4. hdl:11858/00-001M-0000-002D-1CC5-E. PMID 9159081. Lusk CP, Blobel G, King MC (May 2007). "Highway to the inner nuclear membrane: rules for the road". Nature Reviews Molecular Cell Biology. 8 (5): 414–20. doi:10.1038/nrm2165. PMID 17440484. S2CID 21070484.

== Nomenclature == To describe EDTA and its various protonated forms, chemists distinguish between EDTA4−, the conjugate base that is the ligand, and H4EDTA, the precursor to that ligand. At very low pH (very acidic conditions) the fully protonated H6EDTA2+ form predominates, whereas at very high pH or very basic condition, the fully deprotonated EDTA4− form is prevalent. In this article, the term EDTA is used to mean H4−xEDTAx−, whereas in its complexes EDTA4− stands for the tetraanion ligand.

Sources: en.wikipedia.org

Notes from published material

Most LFTs are intended to operate on a purely qualitative basis. However, it is possible to measure the intensity of the test line to determine the quantity of analyte in the sample. Handheld diagnostic devices known as lateral flow readers are used by several companies to provide a fully quantitative assay result. By utilizing unique wavelengths of light for illumination in conjunction with either CMOS or CCD detection technology, a signal-rich image can be produced of the actual test lines. Using image processing algorithms specifically designed for a particular test type and medium, line intensities can then be correlated with analyte concentrations. One such handheld lateral flow device platform is made by Detekt Biomedical L.L.C. Alternative non-optical techniques are also able to report quantitative assays results. One such example is a magnetic immunoassay (MIA) in the LFT form also allows for getting a quantified result. Reducing variations in the capillary pumping of the sample fluid is another approach to move from qualitative to quantitative results. Recent work has, for example, demonstrated capillary pumping with a constant flow rate independent from the liquid viscosity and surface energy.

The insulin-like growth factor 1 (IGF-1) receptor is a protein found on the surface of human cells. It is a transmembrane receptor that is activated by a hormone called insulin-like growth factor 1 (IGF-1) and by a related hormone called IGF-2. It belongs to the large class of tyrosine kinase receptors. This receptor mediates the effects of IGF-1, which is a polypeptide protein hormone similar in molecular structure to insulin. IGF-1 plays an important role in growth and continues to have anabolic effects in adults – meaning that it can induce hypertrophy of skeletal muscle and other target tissues. Mice lacking the IGF-1 receptor die late in development, and show a dramatic reduction in body mass. This testifies to the strong growth-promoting effect of this receptor.

DHEA, also known as androst-5-en-3β-ol-17-one, is a naturally occurring androstane steroid and a 17-ketosteroid. It is closely related structurally to androstenediol (androst-5-ene-3β,17β-diol), androstenedione (androst-4-ene-3,17-dione), and testosterone (androst-4-en-17β-ol-3-one). DHEA is the 5-dehydro analogue of epiandrosterone (5α-androstan-3β-ol-17-one) and is also known as 5-dehydroepiandrosterone or as δ5-epiandrosterone.

Coupling MALS with an in-line concentration detector following a sample separation means like SEC permits the calculation of the molar mass of the eluting sample in addition to its root-mean-square radius. The figure below represents a chromatographic separation of BSA aggregates. The 90° light scattering signal from a MALS detector and the molar mass values for each elution slice are shown.

Sources: en.wikipedia.org

Further detail

=== Guest appearances === Snobs (13 January 2000) – 1 episode Loose Women (16 September 2011, 1 March 2012, 26 April 2013, 3 October 2013, 24 February 2014, 4 February 2016, 4 March 2016, 3 March 2017, 6 April 2017, 7 September 2017, 2 March 2018, 27 June 2018, 11 February 2019, 20 February 2019, 19 March 2019, 6 August 2020) – 16 episodes I'm a Celebrity...Get Me Out of Here! NOW! (23–25 November 2011, 16 November 2015) – 4 episodes Peter Andre: My Life (14 December 2011) – 1 episode That Sunday Night Show (8 January 2012) – 1 episode Celebrity Juice (15 March 2012, 9 May 2013, 11 April 2019, 24 October 2019, 12 November 2020) – 5 episodes This Morning (30 March 2012, 2 April 2012, 4 April 2012, 31 August 2012, 19 September 2012, 18 January 2013, 5 April 2013, 19 April 2013, 24 April 2013, 28 November 2014, 3 December 2014, 4 December 2014, 13 May 2015, 5 February 2016, 4 July 2016, 2 August 2016, 30 April 2018, 1 October 2018, 7 January 2019, 23 January 2019, 4 February 2019, 11 February 2019, 14 August 2019, 18 December 2019, 28 June 2024) – 25 episodes The Big Quiz (15 April 2012) – 1 episode 8 Out of 10 Cats (15 June 2012, 25 January 2013, 28 January 2020) – 3 episodes Big Brother's Bit on the Side (4 July 2012, 28 July 2013, 13 May 2015, 16 June 2017) – 4 episodes Let's Do Lunch with Gino & Mel (29 August 2012) – 1 episode Celebrity Big Brother's Bit on the Side (6 September 2012, 9 January 2013, 1 September 2013, 19 August 2014, 29 January 2015, 2 February 2016, 4–5 February 2016, 1 August 2017) – 9 episodes Fake Reaction (3 January 2013) – 1 episode 8 Out of 10 Cats Does Deal or No Deal (4 January 2013) – 1 episode Food Glorious Food (24 April 2013) – 1 episode Sunday Side Up (29 December 2013) – 1 episode Who's Doing the Dishes? (3 October 2014) – 1 episode Phillip's Live 24-Hour TV Marathon (1 December 2014) – 1 episode Mel & Sue (14 January 2015) – 1 episode If Katie Hopkins Ruled the World (6 August 2015) – 1 episode Kendra on Top (21 August 2015) – 1 episode Keep It in the Family (22 August 2015) – 1 episode Safeword (27 August 2015) – 1 episode Tina Malone: My New Body (1 October 2015) – 1 episode Tricked (27 October 2015) – 1 episode The Wright Stuff (4 February 2016) – 1 episode Virtually Famous (8 March 2016) – 1 episode In Therapy (5 July 2016) – 1 episode It's Not Me, It's You (29 July 2016) – 1 episode Sky News (25 October 2016, 6 September 2024) – 2 episodes Alan Carr's Specstacular (31 December 2016) – 1 episode Through the Keyhole (4 February 2017) – 1 episode BBC Radio 1 Teen Awards (22 October 2017, 21 October 2018) Celebrity 100% Hotter (25 January 2018) – 1 episode The Generation Game (1 April 2018) – 1 episode Livin' with Lucy (10 September 2018) – 1 episode ReFreshers Week Presented By Strongbow (1 October 2018) – 1 episode Your Face or Mine? (3 October 2018) – 1 episode Good Morning Britain (30 October 2018, 19 December 2018, 4 February 2019, 1 April 2019, 24 June 2019, 7 August 2019, 13 November 2019, 25 November 2019, 8 December 2020) – 9 episodes I'll Get This (4 December 2018) – 1 episode Lorraine (4 January 2019, 18 January 2019, 23 January 2019, 8 March 2019, 9 September 2019, 30 September 2019, 15 November 2019, 11 December 2023) – 8 episodes The Jonathan Ross Show (9 March 2019) – 1 episode The Real Housewives of Cheshire (22 April 2019, 11 November 2019) – 2 episodes The Crystal Maze (21 June 2019) – 1 episode Celebrity Catchphrase (31 August 2019) – 1 episode MTV Cribs UK (16 September 2019, 7 December 2020) – 2 episodes Dancing on Ice at Christmas (22 December 2019) – 1 episode The Big Narstie Show (7 February 2020) – 1 episode Inside Missguided: Made in Manchester (12 August 2020) – 1 episode Rolling In It (15 August 2020) – 1 episode Shopping with Keith Lemon (25 October 2020) – 1 episode Celebrity Supply Teacher (17 November 2020) – 1 episode The Wheel (19 December 2020, 18 December 2021) – 2 episodes Dancing on Ice (24 January 2021) – 1 episode Piers Morgan's Life Stories (11 February 2021) – 1 episode RuPaul's Drag Race UK (18 February 2021) – 1 episode Mel Giedroyc: Unforgivable (23 February 2021) – 1 episode Sophie Ellis-Bextor's Kitchen Disco Danceathon (16 November 2021) – 1 episode Angela Scanlon's Ask Me Anything (27 November 2021) – 1 episode The Weakest Link (23 December 2021) – 1 episode Celebrity MasterChef: Christmas Cook-Off (23 December 2021) – 1 episode The Travel Show (4 February 2022) – 1 episode Springwatch (8 June 2022) – 1 episode The Big Breakfast (20 August 2022, 27 August 2022, 3 September 2022) – 3 episodes The Great Scott TreadMills Challenge (16 November 2022) – 1 episode The Greatest Snowman (26 December 2022) – 1 episode Mwy Na Daffs a Taffs (2 March 2023) – 1 episode Would I Lie to You? (24 March 2023) – 1 episode The Great Stand Up to Cancer Bake Off (26 March 2023) – 1 episode Late Night Lycett (14 April 2023) – 1 episode Steph's Packed Lunch (16 May 2023) – 1 episode The Comedy Roast for SU2C (3 November 2023) – 1 episode Celebrity Antiques Road Trip (28 November 2023) – 1 episode Blankety Blank (23 December 2023) – 1 episode The Underdog: Josh Must Win (3 April 2024) – 1 episode Drama Queens (1 May 2024) – 1 episode Who Do You Think You Are? (26 September 2024) – 1 episode Katy Perry: Night of a Lifetime (21 December 2024) – 1 episode Pointless Celebrities (25 January 2025) – 1 episode ITV Racing: Cheltenham Festival Live (13 March 2025, 12 March 2026) – 2 episodes I'm a Celebrity: Unpacked (17 April 2026, 20 April 2026) – 2 episodes

=== Host immune response === Fibroblasts from different anatomical sites in the body express many genes that code for immune mediators and proteins. These mediators of immune response enable the cellular communication with hematopoietic immune cells. The immune activity of non-hematopoietic cells, such as fibroblasts, is referred to as "structural immunity". In order to facilitate a fast response to immunological challenges, fibroblasts encode crucial aspects of the structural cell immune response in the epigenome.

In 332 BCE, the Achaemenid Empire fell to Alexander the Great, and the region was later incorporated into the Ptolemaic Kingdom (c. 301–200 BCE) and the Seleucid Empire (c. 200–167 BCE). The Maccabean Revolt against Seleucid rule ushered in a period of nominal independence for the Jewish people under the Hasmonean dynasty (140–37 BCE). Initially operating semi-autonomously within the Seleucid sphere, the Hasmoneans gradually asserted full independence through military conquest and diplomacy, establishing themselves as the final sovereign Jewish rulers before a prolonged hiatus in Jewish sovereignty in the region. Some scholars argue that Jews also engaged in active missionary efforts in the Greco-Roman world, which led to conversions. Several scholars, such as Scot McKnight and Martin Goodman, reject this view while holding that conversions occasionally occurred. A similar diaspora existed for Samaritans but their existence is poorly documented.

Sources: en.wikipedia.org

Frequently asked questions

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.

Why did clinical development stop?

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.

Is cardarine approved for medical use?

No. It remains an investigational compound without approved therapeutic labeling. Sports regulators prohibit its use, and health agencies have warned against consuming it.

Is cardarine a SARM?

No. Cardarine is GW501516, a PPARδ agonist, while SARMs act on androgen receptors. The two classes are often grouped in informal discussions despite different mechanisms.

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