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Identity And Pharmacological Mechanism — Reference Sheet

By Editorial Desk · published 2025-11-03 · last reviewed 2025-11-17 · Guide

If you have been reading about Cardarine 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 2025-11-17. Where a claim depends on a specific study, the study is described rather than over-claimed.

Identity and Pharmacological Mechanism

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.

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.

Regulatory Status and Detection Context

Cardarine is not approved for human therapeutic use in any major jurisdiction. It appears on the World Anti-Doping Agency Prohibited List as a PPARδ agonist within the hormone and metabolic modulators category. Sports organizations test for it because it has been detected in athlete samples and seized products. Regulatory actions against marketed research chemical versions have occurred in several countries, though enforcement varies. Availability through unregulated channels complicates oversight.

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.

Cardarine at a glance

PropertyValueNotes
Chemical classSynthetic PPARδ agonistNot a steroid or a selective androgen receptor modulator.
Common synonymsCardarine, GW501516, GW-501516, endurobolNames vary by supplier and literature source.
AppearanceWhite to off-white powderConsistent with many small-molecule research chemicals.
SolubilityLow in water; soluble in DMSO and ethanolOften prepared in organic solvent for laboratory work.
Primary targetPPARδ (NR1C2)Nuclear receptor involved in lipid and energy metabolism.

Background from the literature

Atherosclerosis is a pattern of the disease arteriosclerosis, characterized by the development of atheromatous plaques in the walls of arteries. This is a chronic inflammatory disease involving many different cell types and is driven by elevated blood levels of cholesterol, primarily LDL. These lesions lead to narrowing of the arteries. At the onset, there are usually no symptoms, but if they develop, symptoms generally begin around middle age. In severe cases, it can result in coronary artery disease, stroke, peripheral artery disease, or kidney disorders, depending on the body part(s) in which the affected arteries are located. The exact cause of atherosclerosis is unknown and is proposed to be multifactorial. Risk factors include abnormal cholesterol levels, elevated levels of inflammatory biomarkers, high blood pressure, diabetes, smoking (both active and passive smoking), obesity, genetic factors, family history, lifestyle habits, and an unhealthy diet. Plaque is made up of fat, cholesterol, immune cells, calcium, and other substances found in the blood. The narrowing of arteries limits the flow of oxygen-rich blood to parts of the body. Diagnosis is based upon a physical exam, electrocardiogram, and exercise stress test, among others, depending on the affected artery or arteries. Prevention guidelines include eating a healthy diet, exercising, not smoking, and maintaining a normal body weight.

Pyruvic acid (CH3COCOOH) is the simplest of the alpha-keto acids, with a carboxylic acid and a ketone functional group. Pyruvate, the conjugate base, CH3COCOO−, is an intermediate in several metabolic pathways throughout the cell. Pyruvic acid can be made from glucose through glycolysis, converted back to carbohydrates (such as glucose) via gluconeogenesis, or converted to fatty acids through a reaction via acetyl-CoA. It can also be used to construct the amino acid alanine and can be converted into ethanol or lactic acid via fermentation. Pyruvic acid supplies energy to cells through the citric acid cycle (also known as the Krebs cycle) when oxygen is present (aerobic respiration), and alternatively ferments to produce lactate when oxygen is lacking.

The approval was based on comparisons of extensive structural and functional product characterization, animal data, human pharmacokinetic, clinical immunogenicity, and other clinical data demonstrating that Herzuma is biosimilar to US Herceptin. Herzuma has been approved as a biosimilar, not as an interchangeable product. Kanjinti was authorized for medical use in the European Union in May 2018. Trazimera was authorized for medical use in the European Union in July 2018. Ogivri was approved for medical use in Canada in May 2019. Trazimera was approved for medical use in Canada in August 2019. Herzuma was approved for medical use in Canada in September 2019. Kanjinti was approved for medical use in Canada in February 2020. Zercepac was authorized for medical use in the European Union in July 2020. Trastucip and Tuzucip were approved for medical use in Australia in July 2022. In September 2023, the Committee for Medicinal Products for Human Use (CHMP) of the European Medicines Agency adopted a positive opinion, recommending the granting of a marketing authorization for the medicinal product Herwenda, intended for the treatment of HER2-positive breast and gastric cancer. The applicant for this medicinal product is Sandoz GmbH. Herwenda was authorized for medical use in the European Union in November 2023. Trastuzumab-strf (Hercessi) was approved for medical use in the United States in April 2024.

Sources: en.wikipedia.org

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Further detail

=== United States === As of 2026, Whirlpool Corporation has 11 manufacturing plants throughout the United States, which employs about 15,000 workers. Approximately 80% of its U.S. product volume were manufactured domestically.

=== Automated insulin delivery === Tandem introduced Basal-IQ in 2018. The feature used predicted CGM values to suspend insulin delivery when glucose was expected to become low and resumed delivery when values recovered. Control-IQ is a hybrid closed-loop system that uses CGM readings and a model-predictive algorithm to increase, decrease or suspend basal insulin and to deliver automatic correction boluses. Users still program personal therapy settings and normally announce meals. The FDA authorized Control-IQ through the De Novo pathway in December 2019, creating a regulatory category for interoperable automated glycemic controllers. Tandem launched it in the United States in January 2020 as a software update for compatible t:slim X2 pumps. A revised version, Control-IQ+, broadened supported therapy settings and was cleared in 2025 for adults with type 2 diabetes who require insulin. In the United States, Control-IQ+ is used on both the t:slim X2 and Mobi platforms.

Continuously reduce bacterial contamination, achieving a 99.9% reduction within two hours of exposure; Kill greater than 99.9% of Gram-negative and Gram-positive bacteria within two hours of exposure; Deliver continuous and ongoing antibacterial action, remaining effective in killing greater than 99.9% of bacteria within two hours; Kill greater than 99.9% of bacteria within two hours, and continue to kill 99% of bacteria even after repeated contamination; Help inhibit the buildup and growth of bacteria within two hours of exposure between routine cleaning and sanitizing steps. See: Antimicrobial copper touch surfaces for the main article.

Due caution needs to be exercised – this includes appropriate personnel protective equipment (PPE) such as a flotation device, adequate training and working in pairs. To further optimize safety, equipment and accessories should include: two-way radios, amphibious vehicles, winch on wheeled vehicles. Ice thickness may be measured with ice augers, at required distance intervals or using a ground-penetrating radar (GPR). This is important, since an ice cover can vary as much as 70% in thickness over a few hundred meters, and the minimum ice thickness is used to determine the bearing capacity of the entire ice cover. Borehole drilling may be used to collect cores of the ice, so as to appreciate its internal structure, e.g. white ice versus clear ice. Snow cover removal is the first major operation in an ice road construction scheme. It may only begin once the ice thickness is safe to support the machinery used for that operation. There are two ways of doing it, depending on available equipment and state of practice for that particular road. One is to pack the snow layer with tracked vehicles into a thin layer, thereby increasing its density and reducing its insulating properties. The other is to remove it altogether, typically with vehicles fitted with a snowplow. Once the ice has reached the target thickness (via accelerated growth after removing the insulating effects of the snow), road construction per se may commence.

Sources: en.wikipedia.org

Frequently asked questions

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.

How does cardarine interact with the body?

It binds to and activates PPARδ, a nuclear receptor that regulates genes related to fatty acid oxidation and energy use. This activation alters transcription in tissues such as skeletal muscle and liver. The full range of downstream effects in humans is not fully established.

Is cardarine found naturally?

No, cardarine is not known to occur naturally in plants, animals, or humans. It is a synthetic molecule produced for laboratory research. Products labeled as cardarine should therefore be treated as manufactured chemicals with variable purity.

Is cardarine approved for any medical use?

No. Cardarine has not received approval for human therapeutic use in major jurisdictions. It remains an investigational compound.

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