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Identity And Regulatory Status — Hands-On Walkthrough

By Editorial Desk · published 2026-02-15 · last reviewed 2026-03-22 · Faq

PPARδ 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 2026-03-22. Numbers and descriptions here follow the published literature rather than marketing material.

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.

Regulatory treatment varies, but cardarine is not approved as a medicine. Sports authorities list GW501516 as a prohibited substance, and it is banned at all times under the World Anti-Doping Agency code. Many countries restrict sales for human consumption, while online vendors market it as a research chemical. Such products may lack purity data, and their actual contents can differ from the label. Purchasing or possessing cardarine may carry legal consequences depending on jurisdiction. The compound is not a dietary supplement ingredient in regulated markets.

Mechanism and Laboratory Detection

Laboratory handling focuses on identity, purity, and stability. Reference standards are typically stored cold and dry, protected from light, because solutions can degrade over time. Analytical checks may use high-performance liquid chromatography with ultraviolet detection or mass spectrometry. Impurities and related substances can be separated chromatographically and compared with a known standard. Because cardarine is not an approved drug, compendial monographs are absent, and laboratories often rely on in-house methods. Reported purity varies among unregulated products and should not be assumed from a label.

GW501516 binds and activates PPARδ, a nuclear receptor that influences transcription of genes involved in fatty acid oxidation and energy use. Activation shifts some metabolic pathways in preclinical models, which is why the compound has been studied for lipid disorders and exercise-related endpoints. The exact downstream effects in humans are incompletely mapped. PPARδ is expressed in many tissues, including skeletal muscle, liver, and adipose tissue, so broad activation may have varied consequences. Researchers continue to examine how selective or partial activation might alter the balance between benefits and risks.

Cardarine at a glance

PropertyValueNotes
Common synonymsGW501516; GW-1516; endurobolGW501516 is the research code
Drug classPPARδ agonistNot a selective androgen receptor modulator
Molecular formulaC21H18F3NO3S2Established chemical formula
Molar mass453.5 g/molCalculated from the formula
Regulatory statusProhibited in sport; not approved as medicineStatus varies by country

Mechanism and Safety Research

Literature on cardarine often separates receptor pharmacology from toxicology. Mechanistic papers describe PPARδ activation and gene expression changes, while safety assessments focus on carcinogenicity and species differences. Questions remain about whether rodent tumors arise through PPARδ-dependent or off-target mechanisms. Another open area is how human metabolism and exposure compare with those in animal studies. Analytical methods such as liquid chromatography–mass spectrometry are used to confirm identity in biological and product samples.

GW501516 acts as an agonist at the peroxisome proliferator-activated receptor delta, a nuclear receptor that regulates gene expression. Activation shifts transcription toward genes involved in fatty acid uptake, oxidation, and energy expenditure. The compound does not bind the androgen receptor and therefore differs from anabolic steroids and SARMs. In rodent models, this metabolic shift has been linked to increased running endurance and reduced fat accumulation. The exact downstream pathways in humans remain incompletely characterized.

Early clinical research explored GW501516 for lipid disorders, obesity, and diabetes. Some short-term human studies reported changes in HDL cholesterol, LDL cholesterol, and triglycerides. The development program was discontinued after rodent studies showed dose-dependent tumor formation in multiple tissues, including liver, bladder, stomach, and skin. These findings raised concerns about long-term cancer risk in humans. Because human exposure data are limited, the clinical significance of the rodent tumors remains uncertain.

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Background and Regulatory History

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.

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.

Background from the literature

== Biosynthesis == In Glycyrrhiza echinata, the enzyme 6'-deoxychalcone synthase catalyzes the synthesis of isoliquiritigenin from one unit of coumaroyl-CoA and three of malonyl-CoA. It requires reduced nicotinamide adenine dinucleotide phosphate (NADPH) to activate the substrate.

== Medical uses == Trifluridine eye drops are used for the treatment of keratitis and keratoconjunctivitis caused by the herpes simplex virus types 1 and 2, as well as for prevention and treatment of vaccinia virus infections of the eye. A Cochrane Systematic Review showed that trifluridine and aciclovir were a more effective treatment than idoxuridine or vidarabine, significantly increasing the relative number of successfully healed eyes in one to two weeks.

== Three phases of sea surface temperature == The El Niño–Southern Oscillation is a single climate phenomenon that quasi-periodically fluctuates between three phases: Neutral, La Niña or El Niño. La Niña and El Niño are opposite phases, which require certain changes to take place in both the ocean and the atmosphere before an event is declared. The cool phase of ENSO is La Niña, with SST in the eastern Pacific below average, and air pressure high in the eastern Pacific and low in the western Pacific. The ENSO cycle, including both El Niño and La Niña, causes global changes in temperature and rainfall.

Affimers are recombinant proteins. As they are manufactured using recombinant bacterial production processes, the batch-to-batch consistency for Affimers is improved compared to polyclonal antibodies, overcoming some of the issues of reproducibility and security of supply. These synthetic antibodies were engineered to be stable, non-toxic, biologically neutral and contain no post-translational modifications or disulfide bridges. Two separate loop sequences, incorporating a total of 12 to 36 amino acids, form the target interaction surface so interaction surfaces can range form 650–1000 Å. The large interaction surface results allows binding to target proteins. Affimer technology has been commercialised and developed by Avacta, which is developing these affinity reagents as tools for diagnostics and as biotherapeutics.

== Decay == Uranium-235 is an alpha emitter, producing thorium-231. Uranium-235 is the main progenitor of the actinium series, one of the principal actinide decay chains, as it is the longest-lived and sole primordial nuclide (aside from the final end product, lead-207). Beginning with naturally occurring uranium-235, this series includes isotopes of astatine, bismuth, francium, lead, polonium, protactinium, radium, radon, thallium, and thorium, all of which are present in natural uranium sources. The decay proceeds as (only main decay branches shown):

Sources: en.wikipedia.org

Reference notes

=== Simplifications === In case of conservative body forces, ∇ × B = 0. For a barotropic fluid, ∇ρ × ∇p = 0. This is also true for a constant density fluid (including incompressible fluid) where ∇ρ = 0. Note that this is not the same as an incompressible flow, for which the barotropic term cannot be neglected. This note seems to be talking about the fact that conservation of momentum says

Milanese resumed football activity only at a regional level, only to officially end it at the end of the 1945-1946 season. In 2021, after 75 years, a new project is initiated: from the union of three clubs from the south of Milan (Accademia Sandonatese and ACD Metanopoli Calcio) Football Club Milanese 1902 is born, whose first team plays in the fifth division of the Italian championship, with a regional youth sector. F.C. Milanese 1902 was recreated with the intention of giving continuity in the football field to its ancestor U.S. Milanese, taking up its history, logo, traditions and club colours. Right now, F.C. Milanese 1902 is playing at the non-professional level with a youth sector of regional level.

=== Uniforms === Battledress - Used until the 1960s Boots, General Service Khaki drill Denison smock - Used in airborne units until the 1970s 1950 Pattern Jungle Green Dress Boots, Tropical Jungle 1960 Pattern Combat Dress - Produced in olive green and then in Disruptive Pattern Material. Boots, Directly Moulded Sole 1968 Pattern No. 8 Combat Dress - Produced in Disruptive Pattern Material. Smock Parachutist DPM Lightweight Trousers - Produced in olive green No. 9 Tropical Dress 1984 Pattern Combat Dress Boots, Combat, High

Two black spots (ocelli) can be found on each side of the white or orangish nape. The function of these spots is debated, but the most commonly accepted theory is that they act as "false eyes", and help to protect the bird from potential attackers.

Across several benchmarks, AlphaFold3 has demonstrated, on average, superior performance to conventional search-based docking algorithms in predicting small-molecule–protein binding modes. AlphaFold 3 version can predict structures of protein complexes with a very limited set of selected cofactors and co- and post-translational modifications. Between 50% and 70% of the structures of the human proteome are incomplete without covalently-attached glycans. Studies have shown that although AlphaFold3 can jointly model protein–ligand co-folding, its accuracy drops markedly on test cases with low similarity to its training data—an area of particular importance for drug discovery. Other work has found that AlphaFold is insensitive to adversarial decoys generated by altering the physicochemical properties of binding pockets, suggesting potential reliance on training-set memorization rather than genuine chemical awareness.

Sources: en.wikipedia.org

Frequently asked questions

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.

Is cardarine approved for human use?

No. It has no approved medical indication in any country. Regulatory agencies have not cleared it for treatment or prevention of any condition.

Why was its development discontinued?

Early clinical work stopped after rodent carcinogenicity findings. Those animal results raised concerns about long-term human risk, although direct human evidence is lacking. The human relevance of the tumors remains an open scientific question.

How is cardarine detected in samples?

Anti-doping and clinical laboratories commonly use liquid chromatography-tandem mass spectrometry. The method can identify GW501516 and its metabolites in urine or blood. Detection depends on sample timing and the amount present.

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