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Identity And Regulatory Status — Deep Dive

By Editorial Desk · published 2025-07-08 · last reviewed 2025-08-13 · Data

This is a working overview of PPARδ agonist, written for readers who want more than a one-paragraph summary but less than a textbook.

This page was last updated on 2025-08-13 and is reviewed periodically as new material appears.

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.

Identity and Pharmacological Classification

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.

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 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

Cardarine Identity and Mechanism

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.

Cardarine is the common name for GW501516, a synthetic compound studied as a peroxisome proliferator-activated receptor delta agonist. Researchers developed it to explore treatments for lipid disorders and metabolic conditions. It is not an approved medicine in any country. Early clinical work examined changes in HDL cholesterol and triglycerides, but development was discontinued after animal studies raised concerns about cancer. The compound remains available as a research chemical and appears in discussions of performance enhancement.

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.

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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.

Further detail

== Career == Working first in the Physical Chemistry Laboratory, he moved to the Dunn Nutritional Laboratory, and in 1938 moved to Wool Industries Research Institution in Leeds. He was head of the biochemistry division of Boots Pure Drug Company from 1946 to 1948, when he joined the Medical Research Council. There, he was appointed head of the physical chemistry division of the National Institute for Medical Research in 1952, and was chemical consultant from 1956 to 1959. He specialised in biochemistry, in some aspects of vitamins E and B2, and in techniques that laid the foundation for several new types of chromatography. He developed partition chromatography whilst working on the separation of amino acids, and later developed gas-liquid chromatography with Anthony T. James. Amongst many honours, he received his Nobel Prize in 1952. After his retirement from the University of Sussex, he was visiting professor at both the University of Houston in Texas and the EPFL (École Polytechnique Fédérale de Lausanne) in Switzerland. He published far fewer papers than the typical Nobel winners—only 70 in all—but his ninth paper contained the work that would eventually win him the Nobel Prize. The University of Houston dropped him from its chemistry faculty in 1979 (when he was 69 years old) because he was not publishing enough.

== History == The introduction of the baking of processed cereals, including the creation of flour, provided a more reliable source of food. Egyptian sailors carried a flat brittle loaf of millet bread called dhourra cake. A cracker called bucellatum is known from Ancient Rome. King Richard I of England left for the Third Crusade (1189–1192) with "biskit of muslin", which was a mixed grain compound of barley, bean flour, and rye. The more refined captain's biscuit was made with finer flour. Some 5th century BCE physicians, such as Hippocrates, associated most medical problems with digestion. For sustenance and health, eating a biscuit daily was considered good for one's constitution. Because hardtack biscuits were baked hard, they would stay intact for years if kept dry. For long voyages, hardtack was baked four times, rather than the more common two, and prepared six months before sailing. Because it is dry and hard, hardtack, when properly stored and transported, will survive rough handling and temperature extremes. Dry hardtack is dense and virtually inedible; troops issued it usually made it edible by dampening or crushing the biscuits. When James VI and I set sail for Norway in October 1589, his provisions included 15,000 "bisquit baiks". In 1665, Samuel Pepys first regularized naval victualling in the Royal Navy with varied and nutritious rations, to include "one pound daily of good, clean, sweet, sound, well-baked and well-conditioned wheaten biscuit".

== Symptoms and signs == Abdominal obesity, often assessed using the waist-to-hip ratio, is associated with hyperinsulinemia. Direct measurement of serum insulin levels can identify elevated insulin, which may precede the onset of impaired glucose tolerance or hyperglycemia by 10 to 20 years. Consequently, normal fasting blood glucose levels alone do not rule out early-stage hyperinsulinemia. Some patients may experience a variety of symptoms when hypoglycemia is present, including:

=== Contrast agents === Chelate complexes of gadolinium are often used as contrast agents in MRI scans, although iron particle and manganese chelate complexes have also been explored. Bifunctional chelate complexes of zirconium, gallium, fluorine, copper, yttrium, bromine, or iodine are often used for conjugation to monoclonal antibodies for use in antibody-based PET imaging. These chelate complexes often employ the usage of hexadentate ligands such as desferrioxamine B (DFO), according to Meijs et al., and the gadolinium complexes often employ the usage of octadentate ligands such as DTPA, according to Desreux et al. Auranofin, a chelate complex of gold, is used in the treatment of rheumatoid arthritis, and penicillamine, which forms chelate complexes of copper, is used in the treatment of Wilson's disease and cystinuria, as well as refractory rheumatoid arthritis.

"You Hurled Me Into the Depths, Into the Very Heart of the Seas" is the second episode of the fourth season of the American dark comedy crime television series The Righteous Gemstones. It is the 29th overall episode of the series and was written by executive producer John Carcieri, executive producer Jeff Fradley, and series creator Danny McBride, and directed by executive producer Jody Hill. It was released on HBO on March 16, 2025, and also was available on Max on the same date. The series follows a family of televangelists and megachurch pastors led by widowed patriarch Eli Gemstone. The main focus is Eli and his immature children, Jesse, Kelvin and Judy, all of whom face challenges in their lives. The series depicts the family's past and scandals, which unleash consequences. In the episode, the Gemstones try to locate a missing Elijah for a telethon. According to Nielsen Media Research, the episode was seen by an estimated 0.264 million household viewers and gained a 0.05 ratings share among adults aged 18–49. The episode received mostly positive reviews from critics, who praised its humor, performances and character development.

Sources: en.wikipedia.org

Supporting material

A member state of the United Nations since 1955, Portugal is a member of almost all major international organisations, and is among the countries that founded NATO in 1949, the OECD in 1961, EFTA in 1960, and the Community of Portuguese Language Countries (CPLP) in 1996, an international organisation of countries with Portuguese as an official language. Portugal has a stable foreign policy that is the result of its history, geography, and specific foreign policy choices. It is structured around six principal regional and policy priorities: Europe, NATO and relations with the United Kingdom and with the United States, the Portuguese-speaking world, the importance of and support for Portuguese communities abroad, the internationalisation of the national economy, and the strengthening of multilateralism. Portugal regards the success of European integration as paramount and is prepared, where a consensus exists among European Union member states, to endorse policies that go against with the country's national interests; it also supports general disarmament, the dismantling of political-military blocs, and the creation of a collective security system aimed at establishing an international order grounded in peace and justice among peoples. Portugal has two territorial disputes, both of which are with Spain: the Spanish town of Olivenza which has been claimed by Portugal since the 19th century, and the surrounding waters of the Portuguese Savage Islands which have been claimed by Spain since the 15th century.

=== Protein === As a GRX family protein, Grx2 has an N-terminal thioredoxin domain, possessing a 37CSYC40 active site motif with a serine residue replacing the conserved proline residue. This amino acid substitution allows the main chain of Grx2 to be more flexible, promoting coordination of the iron-sulfur cluster and facilitating deglutathionylation by enhanced glutathione-binding. The cysteine pair (Cys28, Cys113) falls outside of the active site, and it is completely conserved in Grx2 proteins but not found in some other GRX family proteins (i.e. Grx1 and Grx5). A disulfide bond between this cysteine pair increases structural stability and provides resistance to over-oxidation induced enzymatic inactivation.

Wherever Marvel Studios plans to take the MCU in the future, it's refreshing to know that its past is expansive and filled with infinite possibilities. Likewise, in his review of Avengers: Endgame, Joe Morgenstern of The Wall Street Journal acknowledged the unique achievement that the Marvel Cinematic Universe had accomplished:

From Greek βίος (bíos) 'life', (from Proto-Indo-European root *gwei-, to live) and λογία (logia) 'study of'. The compound appears in the title of Volume 3 of Michael Christoph Hanow's Philosophiae naturalis sive physicae dogmaticae: Geologia, biologia, phytologia generalis et dendrologia, published in 1766. The term biology in its modern sense appears to have been introduced independently by Thomas Beddoes (in 1799), Karl Friedrich Burdach (in 1800), Gottfried Reinhold Treviranus (Biologie oder Philosophie der lebenden Natur, 1802) and Jean-Baptiste Lamarck (Hydrogéologie, 1802).

A NAD⁺-II class riboswitch, termed mini-NAD⁺-II, was first identified through iterative covariance model (CM) searches against representative bacterial genomes in the Genome Taxonomy Database. Mini-NAD⁺-II riboswitches lack the P1a stem and instead fold into a simple H-type pseudoknot, a compact RNA tertiary structure. The conserved nucleotides essential for tertiary contacts and specific recognition of the NMN moiety are retained, as is an A-rich tract following the P1 stem that likely forms a minor groove triplex. Mini-NAD⁺-II riboswitches lack the P1a stem and instead fold into a simple H-type pseudoknot, a compact RNA tertiary structure. The conserved nucleotides essential for tertiary contacts and specific recognition of the NMN moiety are retained, as is an A-rich tract following the P1 stem that likely forms a minor groove triplex. The potential for base pairing with the adjacent Shine–Dalgarno sequence is also retained, suggesting a conserved mechanism of translational regulation.

Sources: en.wikipedia.org

Supporting material

Although lemborexant has a longer terminal elimination half-life than suvorexant, it appears to be more rapidly cleared than suvorexant in the earlier phases of elimination. In addition, lemborexant dissociates from the orexin receptors more rapidly than does suvorexant. These differences may allow for comparatively reduced next-day effects such as daytime somnolence with lemborexant.

In the 1060s the Normans, under the leadership of Robert Guiscard's brother, Roger I of Sicily, established a presence, and organized a government modeled on the Eastern Roman Empire that was run by the local magnates of Calabria. Of note is that the Normans established their presence there, in Calabria, 6 years prior to their conquest of England. The purpose of this presence in Calabria was to lay the foundations for the Crusades 30 years later, and for the creation of the Kingdom of Jerusalem, and the Kingdom of Sicily. Ships sailed from Calabria to the Holy Land. This made Calabria one of Europe's richest regions as princes from England, France and other regions constructed secondary residences and palaces there, on their way to the Holy Land. Guiscard's son Bohemond, who was born in San Marco Argentano, was one of the leaders of the first crusade. The Via Francigena was an ancient pilgrim route that goes from Canterbury to Rome and southern Italy, reaching Calabria, Basilicata and Apulia, where the crusaders lived, prayed and trained, respectively. In 1098, Roger I of Sicily was named the equivalent of an apostolic legate by Pope Urban II. His son Roger II later became the first King of Sicily and formed what became the Kingdom of Sicily, which lasted nearly 700 years. Under the Normans southern Italy was united as one region and started a feudal system of land ownership in which the Normans were made lords while peasants performed all the work.

=== Partnerships === In 2017, the company announced partnerships with major pharmaceutical companies to negotiate lowering prescription drug costs. GoodRx has deep relationships with major pharmacy chains, including Walgreens, Walmart, CVS Caremark, and Publix, to allow customers to use GoodRx discounts and Gold benefits. GoodRx began its partnership with CVS Caremark in July 2023 to automatically apply coupons to insured CVS customers purchasing generic prescriptions at certain locations. In April 2024, GoodRx added Publix into its network, allowing GoodRx Gold members to use their cards at Publix Pharmacies. GoodRx partners with Pharmacy Benefit Management like Caremark, Express Scripts, and MedImpact to apply their savings directly to eligible insurance plans and members. GoodRx partners with companies like Affirm, Benefitfocus, and DoorDash to integrate their services that offer members discounts and financial flexibility for prescriptions. GoodRx also partners with organizations like the American Academy of Family Physicians Foundation to support broader access to care. In October 2022, GoodRx launched Provider Mode, which allows healthcare providers to use the app to compare costs of drugs for patients based on different payment methods and drug alternatives. In 2025, GoodRx partnered with Novo Nordisk to offer discounted cash-pay access to semaglutide products like Ozempic and Wegovy through its platform and participating pharmacies.

Many catabolic biochemical processes, such as glycolysis, the citric acid cycle, and beta oxidation, produce the reduced coenzyme NADH. This coenzyme contains electrons that have a high transfer potential; in other words, they will release a large amount of energy upon oxidation. However, the cell does not release this energy all at once, as this would be an uncontrollable reaction. Instead, the electrons are removed from NADH and passed to oxygen through a series of enzymes that each release a small amount of the energy. This set of enzymes, consisting of complexes I through IV, is called the electron transport chain and is found in the inner membrane of the mitochondrion. In eukaryotes, the enzymes in this electron transport system use the energy released from O2 by NADH to pump protons across the inner membrane of the mitochondrion. This causes protons to build up in the intermembrane space, and generates an electrochemical gradient across the membrane. The energy stored in this potential is then used by ATP synthase to produce ATP. Oxidative phosphorylation in the eukaryotic mitochondrion is the best-understood example of this process. The mitochondrion is present in almost all eukaryotes, with the exception of anaerobic protozoa such as Trichomonas vaginalis that instead reduce protons to hydrogen in a remnant mitochondrion called a hydrogenosome.

=== Human health === When CEC bypass water filtration systems and contaminate drinking water or accumulate in the food chain, they can also cause risks to human health. Chronic exposure to low doses of CEC has been linked to various health issues. For example, certain pharmaceutical CEC and EDCs have been associated with hormonal imbalances, increased risks of certain cancers, and developmental problems. The antibiotics present in the environment can also contribute to the development of antibiotic-resistant bacteria, which poses a serious threat to human health by reducing the effectiveness of antibiotic treatments. Studies have shown that even at low concentrations, the presence of CEC in drinking water can correlate with neurological disorders and can decrease cognitive function over time. Certain perfluoroalkyl substances (PFAS), which are a type of CEC, have been linked to different adverse health outcomes like increased cholesterol levels, changes in liver enzymes, and reduced vaccine efficacy, which raises concerns about widespread exposure to these chemicals. The CDC also identifies exposure to high levels of CEC with negative effects on the immune system, by compromising the body's ability to fight infections and increasing the risk of rheumatological diseases. Exposure to a combination of various CEC, which can occur through contaminated drinking water or food chains, may lead to cumulative on human health that are not yet fully understood.

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.

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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