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Cardarine As Investigational Pparδ Agonist — Field Notes

By Editorial Desk · published 2025-12-14 · last reviewed 2026-02-02 · Blog

If you have been reading about GW501516 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 2026-02-02. Where a claim depends on a specific study, the study is described rather than over-claimed.

Cardarine as Investigational PPARδ Agonist

Safety discussions about cardarine frequently cite rodent carcinogenicity findings reported in the 2000s. In those studies, treated animals developed tumors at multiple sites, leading sponsors to discontinue clinical development. The relevance of these findings to humans has not been resolved, but they are a major reason the compound is not approved. Current literature emphasizes uncertainty about long-term effects and the risks of unregulated use. Regulators and health agencies have not established a safe human exposure level.

Cardarine is a synthetic compound also known as GW501516, GW-501516, and sometimes endurobol. It was developed as a selective agonist of peroxisome proliferator-activated receptor delta, a nuclear receptor involved in fatty acid oxidation and energy metabolism. The compound was studied in preclinical models for metabolic and cardiovascular conditions, but it did not become a marketed human medicine. In regulatory and anti-doping contexts, it is treated as a prohibited substance rather than a licensed medicine.

Identity and Pharmacological Mechanism

The compound is typically described as a laboratory compound rather than a therapeutic product. Published reports have explored its role in lipid disorders, insulin sensitivity, and exercise metabolism, yet no major drug regulator has approved it for medical use. Commercial samples sold under the cardarine name may vary in purity and identity. Analytical confirmation is therefore necessary when the material is discussed in scientific or regulatory contexts. Its classification as a prohibited substance in sport further shapes how it is studied and reported.

Cardarine is a common name for GW501516, a synthetic compound studied for its effects on lipid and glucose metabolism. It functions as an agonist at peroxisome proliferator-activated receptor delta, or PPARδ, a nuclear receptor that influences gene expression. The molecule is not a steroid, nor is it a selective androgen receptor modulator. It is also known in research and sports literature as GW-501516 and endurobol. Early laboratory work examined its metabolic activity in cell cultures and animal models.

Cardarine at a glance

PropertyValueNotes
Common synonymsGW501516, GW-501516, GW 501516, endurobolNames vary in research and anti-doping documents.
Chemical classSynthetic PPARδ agonistSmall-molecule nuclear receptor ligand.
CAS Registry Number317318-70-0Identifier commonly associated with GW501516.
AppearanceWhite to off-white powderTypical for purified research material.
SolubilityLow in water; soluble in DMSO and ethanolOrganic solvents are common for laboratory stock solutions.

Mechanism and Detection

Preclinical research reported that GW501516 increased running endurance in mice and improved lipid profiles in some animal species. Early human trials explored effects on high-density lipoprotein cholesterol, triglycerides, and glucose handling, but the program was discontinued. Published human data are sparse and do not establish efficacy for any condition. Studies also examined PPAR delta in cancer biology, with conflicting findings across models. The relationship between receptor activation, tissue context, and disease risk remains an active area of investigation.

Anti-doping laboratories identify GW501516 and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is the usual matrix, and detection can occur after the parent compound has cleared from blood. The exact detection window depends on dose, formulation, individual metabolism, and assay sensitivity. Because the compound is prohibited at all times, athletes are subject to testing in and out of competition. Analytical methods continue to improve as new metabolites and designer analogs are characterized.

GW501516 acts as a ligand for PPAR delta, a nuclear receptor that regulates transcription of genes involved in fatty acid oxidation and energy use. Activation of this receptor in skeletal muscle shifts metabolism toward fat burning in animal models. The compound does not burn fat directly; it changes gene expression over hours to days. Researchers study it to understand metabolic flexibility and exercise adaptation. Effects observed in rodents are not automatically expected in humans.

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Identity and Regulatory Status

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.

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.

Mechanism and Safety Research

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.

Reference notes

== Hyperfibrinogenemia == Levels of functionally normal fibrinogen increase in pregnancy to an average of 4.5 gram/liter (g/L) compared to an average of 3 g/L in non-pregnant people. They may also increase in various forms of cancer, particularly gastric, lung, prostate, and ovarian cancers. In these cases, the hyperfibrinogenemia may contribute to the development of pathological thrombosis. A particular pattern of migratory superficial vein thrombosis, termed trousseau's syndrome, occurs in, and may precede all other signs and symptoms of, these cancers. Hyperfibrinogenemia has also been linked as a cause of persistent pulmonary hypertension of the newborn and post-operative thrombosis. High fibrinogen levels had been proposed as a predictor of hemorrhagic complications during catheter-directed thrombolysis for acute or subacute peripheral native artery and arterial bypass occlusions. However, a systematic review of the available literature until January 2016 found that the predictive value of plasma fibrinogen level for predicting hemorrhagic complications after catheter-directed thrombolysis is unproven.

== MTRR gene == The Methionine Synthase Reductase (MTRR) gene primarily acts in the reductive regeneration of cob(I)alamin (vitamin B12). Cob(I)alamin is a cofactor that maintains activation of the methionine synthase enzyme (MTR) methionine synthase, linking folate and methionine metabolism. Donation of methyl groups from folate are utilized for cellular and DNA methylation, influencing epigenetic inheritance.

The oldest and most widely used expression systems are cell-based and may be defined as the "combination of an expression vector, its cloned DNA, and the host for the vector that provide a context to allow foreign gene function in a host cell, that is, produce proteins at a high level". Overexpression is an abnormally and excessively high level of gene expression which produces a pronounced gene-related phenotype. There are many ways to introduce foreign DNA to a cell for expression, and many different host cells may be used for expression — each expression system has distinct advantages and liabilities. Expression systems are normally referred to by the host and the DNA source or the delivery mechanism for the genetic material. For example, common hosts are bacteria (such as E. coli, B. subtilis), yeast (such as S. cerevisiae) or eukaryotic cell lines. Common DNA sources and delivery mechanisms are viruses (such as baculovirus, retrovirus, adenovirus), plasmids, artificial chromosomes and bacteriophage (such as lambda). The best expression system depends on the gene involved, for example the Saccharomyces cerevisiae is often preferred for proteins that require significant posttranslational modification. Insect or mammal cell lines are used when human-like splicing of mRNA is required. Nonetheless, bacterial expression has the advantage of easily producing large amounts of protein, which is required for X-ray crystallography or nuclear magnetic resonance experiments for structure determination.

== Function == The primary protein encoded by HTN3 is histatin 3. Histatins are a family of small, histidine-rich, salivary proteins, encoded by at least two loci (HTN3 and HTN1). Post-translational proteolytic processing results in many histatins: e.g., histatins 4-6 are derived from histatin 3 by proteolysis. Histatins 1 and 3 are primary products of HIS1(1) and HIS2(1) alleles, respectively. Histatins are believed to have important non-immunological, anti-microbial function in the oral cavity. Histatin 1 and histatin 2 are major wound-closing factors in human saliva.

In April 2010, the library announced plans to archive all public communication on Twitter, including all communication since Twitter's launch in March 2006. As of 2015, the Twitter archive remains unfinished. Before retiring in 2015, after 28 years of service, Billington had come "under pressure" as librarian of Congress. This followed a GAO report that described a "work environment lacking central oversight" and faulted Billington for "ignoring repeated calls to hire a chief information officer, as required by law." When Billington announced his plans to retire in 2015, commentator George Weigel described the Library of Congress as "one of the last refuges in Washington of serious bipartisanship and calm, considered conversation", and "one of the world's greatest cultural centers".

Sources: en.wikipedia.org

Notes from published material

Oxygenated blood then returns to the left atrium, passes through the left ventricle and is pumped out through the aorta into systemic circulation, traveling through arteries, arterioles, and capillaries—where nutrients and other substances are exchanged between blood vessels and cells, losing oxygen and gaining carbon dioxide—before being returned to the heart through venules and veins. The adult heart beats at a resting rate close to 72 beats per minute. Cardiovascular diseases are the most common cause of death globally; an estimated 19.8 million people died from them in 2022, representing about 32% of all deaths worldwide. Of these, 85% were due to heart attack and stroke. Risk factors include: smoking, being overweight, little exercise, high cholesterol, high blood pressure, and poorly controlled diabetes, among others. Cardiovascular diseases do not frequently have symptoms but may cause chest pain or shortness of breath. Diagnosis of heart disease is often done by the taking of a medical history, listening to the heart-sounds with a stethoscope, as well as with ECG, and echocardiogram which uses ultrasound. Specialists who focus on diseases of the heart are called cardiologists, although many specialties of medicine may be involved in treatment.

== Chemistry == Proteins constitute 90-95% of venom's dry weight and are responsible for almost all of its biological effects. The hundreds, even thousands, of proteins found in venom include toxins, neurotoxins in particular, as well as nontoxic proteins (which also have pharmacological properties), and many enzymes, especially hydrolytic ones. Enzymes (molecular weight 13-150 KDa) make up 80-90% of viperid and 25-70% of elapid venoms, including digestive hydrolases, L-amino-acid oxidase, phospholipases, thrombin-like pro-coagulant, and kallikrein-like serine proteases and metalloproteinases (hemorrhagins), which damage vascular endothelium. Polypeptide toxins (molecular weight 5-10 KDa) include cytotoxins, cardiotoxins, and postsynaptic neurotoxins (such as α-bungarotoxin and α-Cobratoxin), which bind to acetylcholine receptors at neuromuscular junctions. Compounds with low molecular weight (up to 1.5 KDa) include metals, peptides, lipids, nucleosides, carbohydrates, amines, and oligopeptides, which inhibit angiotensin-converting enzyme (ACE) and potentiate bradykinin (BPP). Inter- and intra-species variation in venom chemical composition is geographical and ontogenic. Phosphodiesterases interfere with the prey's cardiac system, mainly to lower the blood pressure. Phospholipase A2 causes hemolysis by lysing the phospholipid cell membranes of red blood cells. Amino acid oxidases and proteases are used for digestion. Amino acid oxidase also triggers some other enzymes and is responsible for the yellow colour of the venom of some species.

=== West Asia === Documentation of the use of saffron over the span of 3,500 years has been uncovered. Saffron -based pigments have indeed been found in 50,000-year-old depictions of prehistoric places in northwest Iran. The Sumerians later used wild-growing saffron in their remedies and magical potions. It was also known in ancient Egypt, as indicated by a 2000 BC papyrus. Saffron was an article of long-distance trade before the Minoan palace culture's 2nd millennium BC peak. Ancient Persians cultivated Persian saffron (Crocus sativus var. haussknechtii now called Crocus haussknechtii by botanists) in Derbent, Isfahan, and Khorasan by the 10th century BC. At such sites, saffron threads were woven into textiles, ritually offered to divinities, and used in dyes, perfumes, medicines, and body washes. Saffron threads would thus be scattered across beds and mixed into hot teas as a curative for bouts of melancholy. Non-Persians also feared the Persians' usage of saffron as a drugging agent and aphrodisiac. Saffron is featured in trade lists from Mari, Syria, is described in a 7th-century BC Assyrian botanical reference compiled under Ashurbanipal, and is listed among other aromatic plants in the Hebrew Bible, in Song of Songs 4:14. During his Asian campaigns, Alexander the Great used Persian saffron in his infusions, rice, and baths as a curative for battle wounds. Alexander's troops imitated the practice from the Persians and brought saffron-bathing to Greece.

== Dietary intake of PhIP == Determining dietary intake of PhIP can be obtained by more or one ways. One method used is a Food Frequency Questionaries (FFQ) which surveys a population on their estimated consumption of cooked meats. Another method directly measures the quantity of PhIP in a cooked meat sample. However, because the formation of PhIP in cooked meat items is dependent on temperature, cooking time, and cooking method, variations do occur in the direct measurement method. Direct measurement methods have determined dietary intake levels of PhIP to range from 0.07-4.3 ng/kg per day.

Sources: en.wikipedia.org

Frequently asked questions

What is cardarine?

Cardarine is an investigational synthetic compound that acts as a PPARδ agonist. It is also known as GW501516 and has been studied mainly in preclinical research. It is not an approved medicine.

Is cardarine a steroid?

No. Cardarine is not a steroid hormone; it targets the nuclear receptor PPARδ. Its classification in anti-doping rules differs from anabolic steroids, though it remains prohibited in sport.

Why was cardarine not developed further?

Early rodent studies reported tumor formation at multiple sites, which raised safety concerns. Sponsors stopped clinical development, and no approved human product exists.

What is cardarine?

Cardarine is a common name for GW501516, a synthetic PPARδ agonist. It is not a steroid or a selective androgen receptor modulator. It was developed and studied as a research compound for metabolic pathways.

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