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Cardarine Identity And Mechanism — Hands-On Walkthrough

By Editorial Desk · published 2026-07-17 · last reviewed 2026-08-01 · Wiki

Nuclear receptor 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 2026-08-01. Numbers and descriptions here follow the published literature rather than marketing material.

Cardarine Identity and Mechanism

At the molecular level, GW501516 binds and activates PPARδ, a nuclear receptor that regulates transcription. Activation shifts expression of genes involved in fatty acid oxidation, energy expenditure, and lipid transport in skeletal muscle and liver. Animal studies report increased endurance and altered lipid profiles after exposure. Human data are limited to small trials and do not establish long-term safety or efficacy. PPARδ also has roles in cell proliferation, so the relationship between activation and cancer risk remains an open question.

Published literature on cardarine includes in vitro assays, rodent experiments, and a small number of human studies. Reports describe effects on exercise capacity and lipid metabolism in animals, while human evidence is sparse. Many online descriptions present the compound as a proven endurance aid, a claim not supported by regulatory approval or large clinical trials. Analytical studies focus on identifying the parent compound and its metabolites in biological samples. Important uncertainties include species differences, dose-response relationships, and the relevance of rodent tumor findings to humans.

Identity and Pharmacological Classification

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.

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.

Cardarine at a glance

PropertyValueNotes
Common nameCardarineAlso called GW501516 and endurobol.
Chemical formulaC21H18F3NO3S2Molecular weight about 453.5 g/mol.
AppearanceWhite to off-white solidForm depends on synthesis and purity.
SolubilitySoluble in DMSO and ethanolLow solubility in water.
Typical storage-20 °C, desiccated, protected from lightCommon for research chemicals.

Identity and Regulatory Status

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.

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.

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Background and Research Context

In laboratory settings, cardarine is studied as a tool compound for probing PPARδ biology. Published experiments often use cell cultures, rodent models, or isolated tissues. Some investigations focus on metabolic effects, while others assess potential risks such as carcinogenicity observed in long-term animal studies. Because human trials are sparse, most knowledge comes from preclinical work and adverse event reports. Scientific literature frequently notes the gap between animal findings and human outcomes. The compound is not a dietary supplement and is not intended for human consumption.

Cardarine is a common name for GW501516, a synthetic compound developed in the 1990s through research collaborations involving GlaxoSmithKline. It belongs to a class of molecules known as peroxisome proliferator-activated receptor delta agonists. Early studies explored its effects on lipid metabolism and energy expenditure in animal models. The compound was never approved as a human medicine, and clinical development was discontinued. In the years since, it has appeared in fitness and bodybuilding communities as a performance-enhancing substance. Regulatory agencies classify it as an unapproved drug.

PPARδ is a nuclear receptor that regulates gene expression related to fatty acid oxidation, glucose homeostasis, and mitochondrial function. GW501516 binds to this receptor with high affinity and activates downstream signaling in skeletal muscle and other tissues. Animal studies reported increased endurance and altered fuel preference, but human data remain limited and inconsistent. The precise relationship between receptor activation and observed physiological changes is still an area of active investigation. Researchers have also examined whether the compound affects inflammation or cell proliferation. No approved therapeutic indication exists for cardarine.

Background from the literature

== Contribution in modern medicine == Quinine, which is found naturally in the bark of the cinchona tree, is known to be used by Quechuas people for malaria-like symptoms. When chewed, coca acts as a mild stimulant and suppresses hunger, thirst, pain, and fatigue; it is also used to alleviate altitude sickness. Coca leaves are chewed during work in the fields as well as during breaks in construction projects in Quechua provinces. Coca leaves are the raw material from which cocaine, one of Peru's most historically important exports, is chemically extracted.

Ontario: Banting and Best Public School, Toronto Ontario: Banting Memorial High School, Alliston Ontario: Sir Frederick Banting Secondary School, London British Columbia: École Banting Middle School, Coquitlam

Consequently, some of the equivalent salts have the same crystal structure, and in other circumstances where ionic radius is a determining factor, the chemistry of zinc has much in common with that of magnesium. Compared to the transition metals, zinc tends to form bonds with a greater degree of covalency. Complexes with N- and S- donors are much more stable. Complexes of zinc are mostly 4- or 6- coordinate, although 5-coordinate complexes are known. Other oxidation states require unusual physical conditions, and the only positive oxidation states demonstrated are +1 or +2. The volatilization of zinc in combination with zinc chloride at temperatures above 285 °C indicates the formation of Zn2Cl2, a zinc compound with a +1 oxidation state. Calculations indicate that a zinc compound with the oxidation state of +4 is unlikely to exist. Zn(III) is predicted to exist in the presence of strongly electronegative trianions; however, there exists some doubt around this possibility.

Sources: en.wikipedia.org

Reference notes

In the tropics and sub-tropics, relatively more species are expanding due to human activities, particularly due to the spread of crops such as rice whose expansion in south Asia has benefitted at least 64 bird species, though may have harmed many more species.

Molecular evidence of RNA editing in Bombyx chemosensory protein family. PLoS ONE 2014; 9: e86932. 10. Xuan N, Rajashekar B, Kasvandik S, Picimbon JF. Structural components of chemosensory protein mutations in the silkworm moth, Bombyx mori. Agri Gene 2016; 2: 53-58. 11. Xuan N, Rajashekar B, Picimbon JF. DNA and RNA-dependent polymerization in editing of Bombyx chemosensory protein (CSP) gene family. Agri Gene 2019; 12: 100087. 12. Picimbon JF. Mutations in the insect transcriptome. J Clin Exp Pathol. 2016; 6: 3. 13. Picimbon JF. A new view of genetic mutations. Australas Med J. 2017; 10: 701-715. 14. Picimbon JF. Evolution of protein physical structures in insect chemosensory systems. In: Picimbon JF (Ed.), Olfactory Concepts of Insect Control-Alternative to Insecticides. vol. 2 Springer Nature, Switzerland, 2019, pp. 231–263. 15. Campanacci V, Lartigue A, Hällberg BM, Jones TA, Giuici-Orticoni MT, Tegoni M, et al. Moth chemosensory protein exhibits drastic conformational changes and cooperativity on ligand binding. Proc Natl Acad Sci. USA 2003; 100: 5069-5074. 16. Picimbon JF, Dietrich K, Angeli S, Scaloni A, Krieger J, Breer H et al. Purification and molecular cloning of chemosensory proteins from Bombyx mori. Arch Insect Biochem Physiol. 2000b; 44: 120-129. 17. Picimbon JF, Dietrich K, Krieger J, Breer H. Identity and expression pattern of chemosensory proteins in Heliothis virescens (Lepidoptera, Noctuidae). Insect Biochem Mol Biol. 2001; 31: 1173-1181. 18. Wanner KW, Isman MB, Feng Q, Plettner E, Theilmann DA.

suspension A heterogeneous mixture that contains solid particles which are sufficiently large for sedimentation to occur, by which such particles separate from and settle out of the fluid over time if left undisturbed. In a suspension, the solute does not dissolve but remains dispersed or suspended throughout the fluid solvent only transiently and with mechanical agitation. Contrast colloid and solution.

In 2010, President Barack Obama signed the Patient Protection and Affordable Care Act into law. Since the 2022 U.S. Supreme Court decision Dobbs v. Jackson Women's Health Organization, which effectively overruled Roe v. Wade (1973), abortion in the United States is no longer federally protected but is subject to the laws of each state or territory.

Sources: en.wikipedia.org

Notes from published material

In 1972, the Dutch government divided drugs into more- and less-dangerous categories, with cannabis being in the lesser category. Accordingly, possession of 30 grams (1.1 oz) or less was made a misdemeanor. Cannabis has been available for recreational use in coffee shops since 1976. Cannabis products are only sold openly in certain local "coffeeshops" and possession of up to 5 grams (0.18 oz) for personal use is decriminalized, however: the police may still confiscate it, which often happens in car checks near the border. Other types of sales and transportation are not permitted, although the general approach toward cannabis was lenient even before official decriminalization. In Uruguay, President Jose Mujica signed legislation to legalize recreational cannabis in December 2013, making Uruguay the first country in the modern era to legalize cannabis. In August 2014, Uruguay legalized growing up to six plants at home, as well as the formation of growing clubs (Cannabis social club), and a state-controlled marijuana dispensary regime. As of 17 October 2018, when recreational use of cannabis was legalized in Canada, dietary supplements for human use and veterinary health products containing not more than 10 parts per million of THC extract were approved for marketing; Nabiximols (as Sativex) is used as a prescription drug in Canada. The United Nations' World Drug Report stated that cannabis "was the world's most widely produced, trafficked, and consumed drug in the world in 2010", and estimated between 128 million and 238 million users globally in 2015.

==== Increasing protein intake ==== A high protein diet relative to a low-fat or high-carbohydrate diet may increase thermogenesis and decrease appetite leading to weight reduction, particularly 3-6 months into a diet when rapid weight loss is observed. However, these advantages may be reduced later at 12–24 months into a diet during the slow weight loss phase.

Selectivity of a cyclodextrin phase is dependent on two key factors namely the size and structure of the analyte since it is based on a simple fit-unfit geometric criteria. An aromatic ring or cycloalkyl ring should be attached near the stereogenic center of the analyte. Substituents at or near the analyte chiral center must be able to interact with the hydroxyl groups at the entrance of the CD cavity through H-bonding. α-Cyclodextrin holds small aromatic molecules, whereas β-cyclodextrin incorporates both naphthyl groups and substituted phenyl groups. The aqueous compatibility of CD and its unique molecular structure make the CD- bonded phase highly suitable for use in chiral HPLC analysis of drugs. One further benefit of CD is that they are generally less expensive than the other CSPs. Some of the major shortcomings of CD CSPs is that it is limited to compounds that can enter into CD cavity, minor structural changes in analyte leads to unpredictable effect on resolution, often poor efficiency and cannot invert elution order.

==== Statistics ==== There have been 12 large scale, high-quality trials of rtPA in acute ischemic stroke. A meta-analysis of these trials concluded that rtPA given within 6 hours of a stroke significantly increased the odds of being alive and independent at final follow-up, particularly in patients treated within 3 hours. However a significant mortality rate was noted, mostly from intracranial haemorrhage at 7 days, but later mortality was not significant amongst treated and non-treated patients. It has been suggested that if tPA is effective in ischemic stroke, it must be administered as early as possible after the onset of stroke symptoms, given that patients present to an ED in a timely manner. Many national guidelines including the AHA have interpreted this cohort of studies as suggesting that there are specific subgroups who may benefit from tPA and thus recommend its use within a limited time window after the event. Protocol guidelines require its use intravenously within the first three hours of the event, after which its detriments may outweigh its benefits. For example, the Canadian Stroke Network guideline states "All patients with disabling acute ischemic stroke who can be treated within 4.5 hours of symptom onset should be evaluated without delay to determine their eligibility for treatment" with tPA. Delayed presentation to the ED leads to decreased eligibility; as few as 3% of people qualify for this treatment.

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Sources: en.wikipedia.org

Frequently asked questions

What is cardarine?

Cardarine is a common name for the investigational compound GW501516. It acts as a PPARδ agonist and is not approved for human use. It is prohibited in sport.

How does cardarine work?

It activates PPARδ, a nuclear receptor that influences gene expression related to lipid and energy metabolism. Animal studies show changes in endurance and lipid levels. Human effects and risks are not well established.

Is cardarine a steroid?

No, cardarine is not a steroid. It belongs to a different chemical class, the PPARδ agonists. It is also not a selective androgen receptor modulator.

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.

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