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Identity And Pharmacological Mechanism — Practical Notes

By Editorial Desk · published 2025-09-19 · last reviewed 2025-10-08 · Faq

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

Reviewed 2025-10-08. Anything still debated is marked as such rather than presented as settled.

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.

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.

Supporting material

== External links == "Moxetumomab Pasudotox-tdfk". National Cancer Institute. 24 October 2018. Archived from the original on 19 October 2021. Retrieved 11 October 2020. "Moxetumomab Pasudotox-tdfk". NCI Drug Dictionary. National Cancer Institute.

=== HIV in transgender people === Transgender people are infected by HIV at disproportionately high rates worldwide. According to the U.S. Centers for Disease Control and Prevention (CDC), in the United States in 2019, 2% of patients newly diagnosed with HIV were transgender, a higher percentage than the 0.3% of the U.S. population which self-identified as transgender. HIV prevalence is higher in transgender women compared to transgender men. One systematic review and meta-analysis found that overall HIV prevalence around the world was 19.9% in transfeminine individuals and 2.56% in transmasculine individuals. Transgender sex work are at further enhanced HIV risk, and transgender populations in African and Latin American regions have higher HIV prevalence. Following CDC and USPSTF guidelines, UCSF recommends HIV screening for all transgender people at least once. Screening may be repeated on a case-by-case basis, depending on the person's risk for contracting HIV. The risk should be assessed based on the individual's sexual behavior. HIV risk assessment screening should account for the individual's specific anatomy and what type of sexual acts and behaviors the individual partakes in. For instance, HIV prevalence in transgender women is notably high, and a risk factor is that transgender women are frequently noted to partake in receptive anal sex with biologically male partners. There has been a tendency for these individuals to be grouped with "MSM" in research on HIV risk factors, due to a supposed shared mechanism of biological vulnerability to HIV transmission.

Although the preponderance of evidence is on the side of a multidimensional measure, the issue has not been fully resolved owing in part to limitations in the methodological knowledge available on distinguishing between substantive and method variance.

Sources: en.wikipedia.org

Related pages on this site

Notes from published material

=== Graphene === Layering graphene on top of gold has been shown to improve SPR sensor performance. Its high electrical conductivity increases the sensitivity of detection. The large surface area of graphene also facilitates the immobilization of biomolecules while its low refractive index minimizes its interference. Enhancing SPR sensitivity by incorporating graphene with other materials expands the potential of SPR sensors, making them practical in a broader range of applications. For instance, the enhanced sensitivity of graphene can be used in conjunction with a silver SPR sensor, providing a cost-effective alternative for measuring glucose levels in urine. Graphene has also been shown to improve the resistance of SPR sensors to high-temperature annealing up to 500 °C.

== Tissue distribution == Studies have detected FFAR2 protein and/or its messenger RNA (an indicator of FFAR2 protein expression) in the following cell types, cell lines, and tissues: 1) human and rodent enteroendocrine K cells, i.e., cells located in the epithelium of the small intestine; 2) human and rodent enteroendocrine L cells, i.e., cells located in the epithelium of the small intestine and colon; 3) human and rodent fat tissue and/or cultured fat cells; 4) cells in human and rodent pancreatic islets (these islets contain the beta cells and alpha cells that synthesize and secrete insulin and glucagon, respectively, into the blood); 5) cells in and/or derived from cells in the human or mouse spleen, lymph nodes, bone marrow, and blood (e.g., monocytes, lymphocytes, and neutrophils); 6) mouse and, based on indirect studies, human dendritic cells; 7) cells in or derived from cells in human and/or rodent kidneys, hearts, brains (e.g., hypothalamus), fetal membranes, and placentas; 8) cells in the taste buds' lingual papillae of human tongues; 9) mouse renal arteries, aortas, and iliac arteries; 10) various human cell lines including SW480, SW620, HT-29, and T84 colon cancer cells, NCI-H716 colon cancer cells that have a lymphoblast morphology, Caco-2 colorectal cancer cells, Hutu-80 duodenal cancer cells, SW872 liposarcoma cells, MDA-MB-231, MDA-MB-436, and MCF7 breast cancer cells, Huh7 and JHH-4 liver cancer cells, THP-1 acute myeloid leukemia cells, U937 acute promyelocytic leukemia cells, and K562 myelogenous leukemia cells; and 11) the various mouse and rat cell lines discussed below. FFAR2 is also expressed in a wide range of tissues in other animals such as cows, pigs, sheep, cats, and dogs.

== Clinical significance == Fascia itself becomes clinically important when it loses stiffness, becomes too stiff, or has decreased shearing ability. Fascial dysfunction has been implicated in a range of musculoskeletal pain syndromes, including myofascial pain and some cases of chronic low back pain, where altered fascial gliding or adhesions may contribute to symptoms. Surgical disruption of fascial planes can produce postoperative adhesions and functional limitations. Rehabilitation approaches such as targeted physical therapy and myofascial release aim to restore fascial mobility and reduce pain, though high-quality randomized trials assessing long-term efficacy are limited. When pathology causes fibrosis and adhesions, fascial tissue fails to differentiate the adjacent structures effectively. This can happen for a number of reasons, such as

=== Other forms === The anamorphic form of P. semilanceata is an asexual stage in the fungus's life cycle involved in the development of mitotic diaspores (conidia). In culture, grown in a petri dish, the fungus forms a white to pale orange cottony or felt-like mat of mycelia. The conidia formed are straight to curved, measuring 2.0–8.0 by 1.1–2.0 μm, and may contain one to several small intracellular droplets. Although little is known of the anamorphic stage of P. semilanceata beyond the confines of laboratory culture, in general, the morphology of the asexual structures may be used as classical characters in phylogenetic analyses to help understand the evolutionary relationships between related groups of fungi. Scottish mycologist Roy Watling described sequestrate (truffle-like) or secotioid versions of P. semilanceata he found growing in association with regular fruit bodies. These versions had elongated caps, 20–22 cm (7.9–8.7 in) long and 0.8–1 cm (0.3–0.4 in) wide at the base, with the inward curved margins closely hugging the stipe from the development of membranous flanges. Their gills were narrow, closely crowded together, and anastomosed (fused together in a vein-like network). The color of the gills was sepia with a brownish vinaceous (red wine-colored) cast, and a white margin. The stipes of the fruit bodies were 5–6 cm (2.0–2.4 in) long by 0.1–0.3 cm (0.04–0.12 in) thick, with about 2 cm (0.8 in) of stipe length covered by the extended cap. The thick-walled ellipsoid spores were 12.5–13.5 by 6.5–7 μm.

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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