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Background And Regulatory Status — Deep Dive

By Editorial Desk · published 2025-09-02 · last reviewed 2025-09-16 · Blog

The short version of research chemical fits in a sentence. The long version — which is the one that helps — is below.

Reviewed 2025-09-16. Anything still debated is marked as such rather than presented as settled.

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.

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.

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

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.

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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.

Further detail

=== Collectors' Mug and free floats === The first time A&W Restaurants offered a day of free root beer floats was in 2004; under the old management, it was held on June 20, the date of A&W's anniversary, though it is unknown if it donated the proceeds, unlike the current administration. Mid-year, A&W announces the following year's Collectors' Mug, which has a single design for each year. In 2005, it had a full-color image of The Great Root Bear printed on it. By 2010, the event had changed to August 6. It was the chain's first attempt at a digital promotion, where users who liked its Facebook page would receive a digital coupon to redeem a free float. A&W supports Disabled American Veterans and, since 2013, collects funds for it on National Root Beer Float Day, which is observed on August 6. Donation figures for 2019 were of a record $175,000. In the 2000s it was held in June and was known as National Float Day.

For service members with strict religious dietary requirements, the military offers the specialized Meal, Religious, Kosher/Halal. These are tailored to provide the same nutritional content, but will not contain offending ingredients. The entrees come in distinct stylized packaging with a color picture of the prepared entree on it (like civilian pre-made meals) and the food accessories come in commercial packaging. Kosher entrees are marked "Glatt Kosher" in Hebrew and English, while halal entrees are marked "Dhabiha Halal" in Arabic and English. The meals come in cases of 12 that weigh 18 lb (8.2 kg) and have a volume of 1.4 cubic feet (40 L). To keep with dietary laws, the entree and accessory packets are packed in two separate inner boxes in an outer case and come in kosher or halal only (the two special ration types are never mixed in a shipping case). The original meals were kosher only and came in 4 Beef, 4 Chicken, 2 Salmon, and 2 Gefilte Fish menus. The meals now come in Beef, Lamb, Chicken, Vegetarian, and Pasta dishes. The entrees are a mixture of traditional Middle-Eastern and South Asian dishes (like Lamb & Vegetable Jalfrezi or Curried Chicken with Basmati Rice, Lentils, and Vegetables) and Western dishes (like Vegetable Ratatouille, Florentine-style Vegetable Lasagna, or New Orleans Gumbo with Chicken). Each menu contains an average of 1200 kilocalories and has a shelf life of 3 to 10 months. There is also a special kosher meal certified for Passover requirements.

Interface to personal computers: Since the late 1990s, most pumps can interface with personal computers for managing and documenting pump programming and/or to upload data from the pump. This simplifies record keeping and can be interfaced with diabetes management software. Integration with blood glucose meters: Blood glucose data can be manually entered into the pump to support the bolus wizard for calculation of the next insulin bolus. Some pumps support an interface between the insulin pump and a blood glucose meter, with either wired or radio frequency (RF) communication. Integration with continuous glucose monitoring systems: Some insulin pumps can be used as a display for interstitial glucose values obtained from a continuous glucose monitoring system or sensor.

Sources: en.wikipedia.org

Supporting material

Re2O7 + 17 CO → Re2(CO)10 + 7 CO2 If metal oxides are used carbon dioxide is formed as a reaction product. In the reduction of metal chlorides with carbon monoxide phosgene is formed, as in the preparation of osmium carbonyl chloride from the chloride salts. Carbon monoxide is also suitable for the reduction of sulfides, where carbonyl sulfide is the byproduct.

== Honours and awards == He received honorary degrees from University of Poitiers, France (D.Sc.1981), Uppsala University, Sweden (FarmDhc, 1989), and Athens University, Greece ( D.Sc., 2011). He was made Fellow, Academy of Medical Sciences (2001), Fellow, British Pharmacological Society (2012), and Honorary Fellow, American College of Clinical Pharmacology (2003). He received the Scheele Award (Swedish Academy of Pharmaceutical Sciences, 1984), the Distinguished Investigator Award (American College of Clinical Pharmacology, 2007), the New Safe Medicines Faster Award (EUFEPS, 2009), Research Achievement Award in Pharmacokinetics (American Association of Pharmaceutical Scientists, 1994), the Sheiner-Beal Award in Pharmacometrics (American Society of Clinical Pharmacology and Therapeutics, 2012) and the Ariens Award (Dutch Pharmacological Society, 2020)., as well as the Harrison Memorial Medal (Royal Pharmaceutical Society of Great Britain, 1992) and Host Madsen Medal (International Pharmaceutical Federation, 2011).

=== Silage === Lactiplantibacillus plantarum is the most common bacterium used in silage inoculants. During the anaerobic conditions of ensilage, these organisms quickly dominate the microbial population, and, within 48 hours, they begin to produce lactic and acetic acids via the Embden-Meyerhof Pathway, further diminishing their competition. Under these conditions, L. plantarum strains producing high levels of heterologous proteins have been found to remain highly competitive. This quality could allow this species to be utilized as an effective biological pretreatment for lignocellulosic biomass.

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 the main molecular target of cardarine?

It targets PPARδ, a nuclear receptor involved in lipid and energy metabolism. It does not act primarily on androgen receptors. This distinction separates it from SARMs.

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