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Background And Regulatory Status — Quick Reference

By Editorial Desk · published 2026-04-22 · last reviewed 2026-05-12 · Topic

If you have been reading about Investigational drug 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 2026-05-12. Where a claim depends on a specific study, the study is described rather than over-claimed.

Background and Regulatory Status

Cardarine is a common name for GW501516, a synthetic compound first described in the 1990s as a selective agonist of the peroxisome proliferator-activated receptor delta. It was studied in preclinical models for metabolic and cardiovascular conditions, but it has not been approved as a medicine in the United States, Europe, or other major jurisdictions. Retail products labeled as cardarine are generally research chemicals or supplements, not pharmaceutical formulations. Because human safety and efficacy data remain limited, regulatory agencies treat it as an unapproved substance rather than a therapeutic product.

Sporting authorities added GW501516 to prohibited lists after it appeared in athlete samples and online markets. The World Anti-Doping Agency classifies it as a hormone and metabolic modulator, and its use can lead to an anti-doping rule violation. Some early laboratory work suggested effects on fatty acid oxidation and endurance-related metabolism in animals, but those findings do not establish safe or effective use in people. Reports of adverse events in humans are scarce and often anecdotal, which complicates risk assessment.

Identity and Pharmacological Mechanism

Activation of PPARδ changes transcription of genes involved in fatty acid transport, mitochondrial function, and skeletal muscle fuel preference. In rodent studies, pharmacological PPARδ activation was associated with increased endurance and altered body composition. These findings generated interest in performance enhancement, but species differences and study designs limit direct extrapolation to humans. Small human trials were conducted in the 2000s and later discontinued. The extent to which cardarine produces similar metabolic or performance effects in people remains an open question.

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
IUPAC name{4-[({4-methyl-2-[4-(trifluoromethyl)phenyl]-1,3-thiazol-5-yl}methyl)sulfanyl]phenoxy}acetic acidSystematic name for GW501516
CAS Registry Number317318-70-0Unique identifier for the parent compound
Molecular formulaC21H18F3NO3S2Includes carbon, hydrogen, fluorine, nitrogen, oxygen, and sulfur
Molecular weight453.5 g/molApproximate value for the neutral form
AppearanceWhite to off-white powderTypical description for purified laboratory material

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.

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Regulatory Status and Detection Context

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.

A persistent misconception is that cardarine is a fat-burning drug or a safe alternative to anabolic steroids. No approved therapeutic product exists, and human safety data are limited. The tumor findings in rodents remain a central concern in scientific reviews. Products sold online may contain inaccurate labels, impurities, or different compounds entirely, which complicates any assessment of effects. Independent testing of such products has reported frequent mislabeling. For these reasons, discussions in the literature emphasize risks and unknowns rather than benefits.

Notes from published material

=== Motivation, technique, and counselling === Kalra has led several original studies examining insulin usage practices in South Asia. Kalra has also led multiple manuscripts providing regional best practices and recommendations related to insulin delivery devices, injection techniques, monitoring, and complication management. He was also the lead author of expert recommendations for the use of insulin in India, published in 2017.

=== Interaction proteomics and protein networks === Interaction proteomics is the analysis of protein interactions from scales of binary interactions to proteome- or network-wide. Most proteins function via protein–protein interactions, and one goal of interaction proteomics is to identify binary protein interactions, protein complexes, and interactomes. Several methods are available to probe protein–protein interactions. While the most traditional method is yeast two-hybrid analysis, a powerful emerging method is affinity purification followed by protein mass spectrometry using tagged protein baits. Other methods include surface plasmon resonance (SPR), protein microarrays, dual polarisation interferometry, microscale thermophoresis, kinetic exclusion assay, and experimental methods such as phage display and in silico computational methods. Knowledge of protein-protein interactions is especially useful in regard to biological networks and systems biology, for example in cell signaling cascades and gene regulatory networks (GRNs, where knowledge of protein-DNA interactions is also informative). Proteome-wide analysis of protein interactions, and integration of these interaction patterns into larger biological networks, is crucial towards understanding systems-level biology.

Radar equipment is used at airports, in airplanes, at missile sites, on tanks, and on ships. The radar technology commonly used in the 20th century produced X-rays as a technically unavoidable by-product in the high-voltage electronics of the equipment. In the 1960s and 1970s, German soldiers and technicians were largely unaware of the dangers, as were those in the GDR's National People's Army. The problem had been known internationally since the 1950s, and to the German Armed Forces since at least 1958. However, no radiation protection measures were taken, such as the wearing of lead aprons. Until about the mid-1980s, radiation shielding was inadequate, especially for pulse switch tubes. Particularly affected were maintenance technicians (radar mechanics) who were exposed to the X-ray generating parts for hours without any protection. The permissible annual limit value could be exceeded after just 3 minutes. It was not until 1976 that warning notices were put up and protective measures taken in the German Navy, and not until the early 1980s in general. As late as the 1990s, the German Armed Forces denied any connection between radar equipment and cancer or genetic damage. The number of victims amounted to several thousand. The connection was later acknowledged by the German Armed Forces and in many cases a supplementary pension was paid. In 2012, a foundation was set up to provide unbureaucratic compensation for the victims.

=== Function === ACTH released from the corticotropes binds to G protein-coupled receptors in the adrenal cortex, where it stimulates the production of glucocorticoids (primarily cortisol). ACTH binds to the melanocortin 2 receptor and, through signal transduction, increases levels of cholesterol esterase, the transport of cholesterol across the mitochondrial membrane, cholesterol binding to P450SCC and, an increase in pregnenolone synthesis. It also serves as a secondary stimulus for the synthesis of mineralocorticoids such as aldosterone, which serve an important role in regulating the salt balance of the blood. Glucocorticoids released by the adrenal cortex inhibit production of CRH and ACTH, forming a negative feedback loop.

Sources: en.wikipedia.org

Background from the literature

Modern research suggests Jenner was trying to distinguish between effects caused by what would be recognised as a non-infectious vaccine, a different virus (e.g. paravaccinia/milker's nodes), or contaminating bacterial pathogens. This caused confusion at the time, but would become important criteria in vaccine development. A further source of confusion was Jenner's belief that fully effective vaccine obtained from cows originated in an equine disease, which he mistakenly referred to as grease. This was criticised at the time but vaccines derived from horsepox were soon introduced and later contributed to the complicated problem of the origin of vaccinia virus, the virus in present-day vaccine. The introduction of the vaccine to the New World took place in Trinity, Newfoundland, in 1798 by Dr. John Clinch, boyhood friend and medical colleague of Jenner. The first smallpox vaccine in the United States was administered in 1799. The physician Valentine Seaman gave his children a smallpox vaccination using a serum acquired from Jenner. By 1800, Jenner's work had been published in all the major European languages and had reached Benjamin Waterhouse in the United States – an indication of rapid spread and deep interest. Despite some concern about the safety of vaccination the mortality using carefully selected vaccine was close to zero, and it was soon in use all over Europe and the United States.

But it also does something no other game has done to date: It really makes you feel." The New York Times reviewer described it as: "intelligent, gorgeous, occasionally frightening" and added: "Anchored by its provocative, morality-based story line, sumptuous art direction and superb voice acting, BioShock can also hold its head high among the best games ever made." GameSpy praised BioShock's "inescapable atmosphere", and Official Xbox Magazine lauded its "inconceivably great plot" and "stunning soundtrack and audio effects". The gameplay and combat system have been praised for being smooth and open-ended, and elements of the graphics, such as the water, were commended for their quality. It has been noted that the combination of the game's elements "straddles so many entertainment art forms so expertly that it's the best demonstration yet how flexible this medium can be. It's no longer just another shooter wrapped up in a pretty game engine, but a story that exists and unfolds inside the most convincing and elaborate and artistic game world ever conceived." Reviewers did highlight a few negative issues in BioShock, however. The recovery system involving "Vita-Chambers", which revive a defeated player at half-health, but do not alter the enemies' health, makes it possible to wear down enemies through sheer perseverance, and was criticized as one of the most significant flaws in the gameplay.

==== Earl G. Graves School of Business and Management ==== The Earl G. Graves School of Business and Management (GSBM) is named in honor of alumnus Earl G. Graves, Sr. and is housed in the Graves School of Business and Management building, which was opened for the Fall Semester 2015 at the western edge of the campus. It contains classrooms, laboratories, and office buildings with rooms for hospitality management students to operate. The GSBM offers Bachelor of Science, Master of Science, Master of Business Administration, and PhD degree programs. These programs are accredited by The Association to Advance Collegiate Schools of Business (AACSB).

== Pharmacology == JDTic is a potent KOR antagonist, and is highly selective for KOR over μ- (MOR) and δ-opioid receptors (DOR), along with many non-opioid receptors. However, it shows modest affinity for the nociceptin receptor (NOP). In one study, JDTic showed little binding selectivity over the μ-opioid receptor, but it failed to block the effects of the selective μ-opioid receptor agonist sufentanil across a wide range of doses in animals. It has a very long duration of action, with effects in animals seen for up to several weeks after administration of a single dose, although its binding to the KOR is not irreversible; its long duration of action is instead caused by activation of a c-Jun N-terminal kinase. Animal studies suggest that JDTic may produce antidepressant, anxiolytic, and anti-stress effects, as well as having possible application in the treatment of addiction to cocaine and morphine. JDTic shows robust activity in animal models of depression, anxiety, stress-induced cocaine relapse, and nicotine withdrawal.

== Administration == Prajmaline can be administered orally, parenterally or intravenously. Three days after the last dose, a limited effect has been observed. Therefore, it has been suggested that treatment of arrhythmias with Prajmaline must be continuous to see acceptable results.

Sources: en.wikipedia.org

Frequently asked questions

Is cardarine approved for human use?

No. Major drug regulators have not approved GW501516 for treating any medical condition. Products sold as cardarine are typically unapproved research chemicals or supplements, so their contents and safety are not assured.

Why is cardarine banned in sport?

It is prohibited by the World Anti-Doping Agency as a hormone and metabolic modulator. Athletes who test positive for GW501516 can face sanctions, including suspensions and loss of results.

What is the difference between cardarine and GW501516?

Cardarine is a common or trade-style name, while GW501516 is the research code for the same chemical entity. Some sources also use Endurobol or GSK-516. The names refer to the same compound, not distinct drugs.

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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