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Identity And Pharmacological Classification — Field Notes

By Editorial Desk · published 2026-07-09 · last reviewed 2026-08-01 · News

If you have been reading about PPARδ 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.

Last reviewed on 2026-08-01. Where a claim depends on a specific study, the study is described rather than over-claimed.

Identity and Pharmacological Classification

PPARδ is a nuclear receptor that influences transcription of genes involved in fatty acid oxidation, lipid transport, and energy homeostasis. GW501516 binds and activates this receptor with high selectivity relative to PPARα and PPARγ in laboratory assays. Activation alters expression of target genes in skeletal muscle, liver, and adipose tissue in animal models. The exact clinical consequences of these changes in humans remain incompletely characterized, and observed effects in animals do not establish therapeutic benefit or safety.

Published studies have examined GW501516 in animal models of obesity, insulin resistance, and exercise endurance. Early human trials reportedly ended, and development was discontinued after preclinical findings raised concerns about cancer in some rodent studies. Regulatory agencies have not approved cardarine for any medical use. Its availability through non-pharmaceutical channels raises questions about identity, purity, and legal status that are separate from its laboratory pharmacology. Those questions are often addressed through analytical testing rather than assumptions about product labels.

Cardarine is a common name for GW501516, also GW-1516, a synthetic compound developed as a peroxisome proliferator-activated receptor delta (PPARδ) agonist. It belongs to a class of agents that modulate gene transcription related to lipid and energy metabolism. The compound was studied in preclinical and early clinical research for metabolic and cardiovascular conditions, but it did not progress to approved therapeutic use. Its name appears in fitness and sports contexts despite not being approved as a drug.

Detection and Regulatory Landscape

A common misconception is that cardarine has been proven safe for human use. In reality, human clinical data are limited, and long-term animal studies have raised concerns about cancer. Another misconception is that it is a supplement or vitamin-like compound. It is a synthetic research chemical with no approved medical indication. Scientific discussion often focuses on its mechanism and detection rather than therapeutic use. Regulatory and anti-doping literature treats it primarily as a prohibited substance.

Cardarine is explicitly prohibited by the World Anti-Doping Agency under the class of PPARδ agonists. Its presence in urine or blood samples can be detected using mass spectrometry-based methods, often liquid chromatography-tandem mass spectrometry. Athletes who test positive may face sanctions, including bans from competition. The compound is also regulated as a prescription-only or unapproved drug in many countries. Enforcement varies by jurisdiction, and some regions treat it as a controlled substance. Online sales may occur despite these restrictions, creating quality and legal risks.

Laboratory detection of cardarine typically involves sample preparation followed by chromatographic separation and mass spectrometric identification. Urine is the most common matrix for anti-doping tests, though blood and hair have also been explored. Methods can target the parent compound or its metabolites, depending on the expected window of detection. Reference standards are required for accurate quantification. Matrix effects and dilution can influence results, so laboratories use internal standards and validation protocols. The exact detection window varies with dose, route, and individual metabolism.

Cardarine at a glance

PropertyValueNotes
Chemical classPPARδ agonistNot an anabolic steroid.
Common synonymsGW501516, GW-1516Cardarine is an informal name.
AppearanceWhite to off-white powderTypical for research-grade solid.
Solubility classPoorly soluble in water; soluble in some organic solventsSuch as DMSO or ethanol in laboratory settings.
Typical storage temperatureCool, dry, protected from lightSpecific conditions vary by supplier and form.

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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Regulatory Status and Detection Context

Cardarine is not approved for human therapeutic use in any major jurisdiction. It appears on the World Anti-Doping Agency Prohibited List as a PPARδ agonist within the hormone and metabolic modulators category. Sports organizations test for it because it has been detected in athlete samples and seized products. Regulatory actions against marketed research chemical versions have occurred in several countries, though enforcement varies. Availability through unregulated channels complicates oversight.

Analytical laboratories typically identify cardarine and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is a common matrix in anti-doping testing, while blood and tissue may be used in research settings. Detection windows depend on the assay, the sample matrix, and the compound's metabolism. Because cardarine is extensively metabolized, laboratories often target specific metabolites to improve sensitivity and confirmation. Reference standards are required for reliable quantification. Method validation includes checks for selectivity, linearity, and carryover.

Regulation and Analytical Detection

Anti-doping laboratories detect GW501516 and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is the most common matrix, though blood and dried blood spots may also be used in some programs. Detection depends on factors such as dose, timing, metabolism, and the sensitivity of the assay. Published methods describe limits of detection in the low nanogram per milliliter range for related compounds. Exact detection windows are not fixed for all situations and remain an area of ongoing study.

Products sold as cardarine have been found to contain incorrect compounds, variable amounts, or no active ingredient at all. Independent testing is required to verify identity and purity. Common analytical approaches include high-performance liquid chromatography, mass spectrometry, and nuclear magnetic resonance for structural confirmation. These methods can distinguish GW501516 from related PPAR agonists and from unrelated steroids. For regulators and researchers, such verification is central to interpreting both biological results and adverse event reports.

Cardarine is prohibited in competitive sport under the World Anti-Doping Agency code, where it is classified as a metabolic modulator. It is not approved as a prescription medicine in the United States, European Union, or other major markets. Regulatory action has focused on its presence in sports and in products marketed as research chemicals. Because it has no accepted medical indication, supply is often unregulated. This status creates legal and safety uncertainties for anyone who encounters the substance.

Notes from published material

Photoinduction takes place with a brief exposure to light (wavelength is tetrazole-dependent) to minimize photodamage to cells. The reaction is enhanced in aqueous conditions and generates a single regioisomer. The transient nitrile imine is highly reactive for 1,3-dipolar cycloaddition due to a bent structure which reduces distortion energy. Substitution with electron-donating groups on phenyl rings increases the HOMO energy, when placed on the 1,3 nitrile imine and increases the rate of reaction. Advantages of this approach include the ability to spatially or temporally control reaction and the ability to incorporate both alkenes and tetrazoles into biomolecules using simple biological methods such as genetic encoding. Additionally, the tetrazole can be designed to be fluorogenic in order to monitor progress of the reaction.

Firehouse Restaurant Group, Inc., doing business as Firehouse Subs, is an American multinational fast casual restaurant chain based in Jacksonville, Florida, that specializes in submarine sandwiches. It was founded in 1994 in Jacksonville, Florida by former firefighter brothers Chris and Robin Sorensen. It is a subsidiary of Restaurant Brands International, which also owns the chains Burger King, Popeyes, and Tim Hortons. Firehouse Subs has over 1,200 restaurants in 46 states, Puerto Rico, Switzerland, Mexico, Albania, Kosovo, Canada, Middle East and soon the United Kingdom and Australia by 2025 and in Brazil by 2026.

Some brewers add one or more clarifying agents to beer, which typically precipitate (collect as a solid) out of the beer along with protein solids and are found only in trace amounts in the finished product. This process makes the beer appear bright and clean, rather than the cloudy appearance of ethnic and older styles of beer such as wheat beers. Examples of clarifying agents include isinglass, obtained from swim bladders of fish; Irish moss, a seaweed; kappa carrageenan, from the seaweed kappaphycus; polyclar (a commercial brand of clarifier); and gelatin. If a beer is marked "suitable for Vegans", it was generally clarified either with seaweed or with artificial agents, although the "Fast Cask" method invented by Marston's in 2009 may provide another method.

Hear Music began as a music catalog company in 1990, adding a few retail locations in the San Francisco Bay Area. Hear Music was purchased by Starbucks in 1999. In 2002, it produced a Starbucks opera album, featuring artists such as Luciano Pavarotti, followed in March 2007 by the hit CD Memory Almost Full by Paul McCartney, making McCartney the first artist signed to the new Hear Music label sold in Starbucks outlets. In 2006, the company created Starbucks Entertainment, one of the producers of the 2006 film Akeelah and the Bee. Starbucks stores advertised the film before its release and sold the DVD. Starbucks has become the subject of a protest song, "A Rock Star Bucks a Coffee Shop" by Neil Young and his band, Promise of the Real. This single from the album The Monsanto Years criticized both Starbucks's alleged use of genetically modified food and the GMO company Monsanto.

=== Mechanism of action === When it is administered intravenously, adenosine causes transient heart block in the atrioventricular (AV) node. This is mediated via the A1 receptor, inhibiting adenylyl cyclase, reducing cAMP and so causing cell hyperpolarization by increasing K+ efflux via inward rectifier K+ channels, subsequently inhibiting Ca2+ current. It also causes endothelial-dependent relaxation of smooth muscle as is found inside the artery walls. This causes dilation of the "normal" segments of arteries, i.e. where the endothelium is not separated from the tunica media by atherosclerotic plaque. This feature allows physicians to use adenosine to test for blockages in the coronary arteries, by exaggerating the difference between the normal and abnormal segments. The administration of adenosine also reduces blood flow to coronary arteries past the occlusion. Other coronary arteries dilate when adenosine is administered while the segment past the occlusion is already maximally dilated, which is a process called coronary steal. This leads to less blood reaching the ischemic tissue, which in turn produces the characteristic chest pain.

Sources: en.wikipedia.org

Background from the literature

==== Europe ==== In 1998, Starbucks entered the United Kingdom market with the US$83 million acquisition of the then 56-outlet, UK-based Seattle Coffee Company, re-branding all those stores as Starbucks. In October 2002, Starbucks established a coffee trading company in Lausanne, Switzerland, to handle purchases of green coffee. All other coffee-related business continued to be managed from Seattle. In September 2007, the company opened its first store in Russia, ten years after first registering a trademark there. After the Russian invasion of Ukraine, on May 21, 2022, Starbucks announced closure of all outlets in Russia, and in July it was revealed that a local restaurant manager, Anton Pinsky, is going to acquire Starbucks' Russian operating company OOO Starbucks and all its 130 stores. In 2008, Starbucks opened in Belgium, Bulgaria, the Czech Republic, and Portugal.

=== Receptor Genetics === Four RXFPs in humans are located in different linkage groups. Additionally there are two RXFP pseudogenes ("RXFP3-3" and "RXFP2-like") which have functional counterparts in other species.

=== Chemo preventative therapy === It has been noted that ornithine decarboxylase (ODC) exhibits high activity in tumor cells, promoting cell growth and division, while absence of ODC activity leads to depletion of putrescine, causing impairment of RNA and DNA synthesis. Typically, drugs that inhibit cell growth are considered candidates for cancer therapy, so eflornithine was naturally believed to have potential utility as an anti-cancer agent. By inhibiting ODC, eflornithine inhibits cell growth and division of both cancerous and noncancerous cells. However, several clinical trials demonstrated minor results. It was found that inhibition of ODC by eflornithine does not kill proliferating cells, making eflornithine ineffective as a chemotherapeutic agent. The inhibition of the formation of polyamines by ODC activity can be ameliorated by dietary and bacterial means because high concentrations are found in cheese, red meat, and some intestinal bacteria, providing reserves if ODC is inhibited. Although the role of polyamines in carcinogenesis is still unclear, polyamine synthesis has been supported to be more of a causative agent rather than an associative effect in cancer. Other studies have suggested that eflornithine can still aid in some chemoprevention by lowering polyamine levels in colorectal mucosa, with additional strong preclinical evidence available for application of eflornithine in colorectal and skin carcinogenesis. This has made eflornithine a supported chemopreventive therapy specifically for colon cancer in combination with other medications.

In its wild-type form, the IDH1 enzyme is active in the cytoplasm and peroxisomes, where it catalyzes the conversion of isocitrate into α-ketoglutarate (α-KG) as part of the citric acid cycle. This process generates NADPH, a vital molecule that supports antioxidant defenses and biosynthetic processes. When mutated, IDH1 undergoes a neomorphic transformation, shifting its function. The altered enzyme converts α-KG into D-2-hydroxyglutarate (D-2HG), an oncometabolite. Elevated D-2HG levels disrupt normal cellular processes by inhibiting α-KG–dependent dioxygenases, leading to epigenetic changes, DNA hypermethylation, and impaired differentiation. Moreover, the mutation redirects NADPH consumption, increasing oxidative stress, which further drives tumor development. The accumulation of D-2HG and elevated oxidative stress play a critical role in reshaping the tumor microenvironment, positioning the R132H mutation as a prime target for IDH inhibitors. These therapies aim to restore regular metabolic functions and reduce tumor aggressiveness, offering a promising avenue for glioma treatment. In addition to being mutated in diffuse gliomas, IDH1 has also been shown to harbor mutations in human acute myeloid leukemia. The IDH1 mutation is considered a driver alteration and occurs early during tumorigenesis, in specific in glioma and glioblastoma multiforme, its possible use as a new tumour-specific antigen to induce antitumor immunity for the cancer treatment has recently been prompted.

Sources: en.wikipedia.org

Frequently asked questions

What is cardarine also known as?

Cardarine is commonly known as GW501516 or GW-1516. These names refer to the same synthetic compound. It is not a brand-name approved medicine.

Is cardarine a steroid?

No, cardarine is not a steroid. It is classified as a PPARδ agonist. Its structure and receptor target differ from anabolic steroids.

Has cardarine been approved for human use?

No regulatory agency has approved cardarine as a medicine. It was investigated in early research but development was discontinued. It is not available as a prescription drug.

Is cardarine banned in sports?

Yes, WADA prohibits cardarine as a PPARδ agonist. It appears on the prohibited list and can be detected in urine or blood. Athletes using it risk sanctions.

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