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Background And Regulatory Status — Questions and Answers

By Editorial Desk · published 2026-06-23 · last reviewed 2026-07-11 · Data

Everything below concerns anti-doping. We keep the language plain, cite what the science says, and separate well-supported claims from open questions.

Last reviewed on 2026-07-11. Where a claim depends on a specific study, the study is described rather than over-claimed.

Background and Regulatory Status

Legal status varies by country. In some places, cardarine is controlled under medicines or psychoactive substances laws; in others, it may be sold with minimal oversight as a research chemical. Customs agencies have intercepted shipments, and several national health agencies have issued warnings about products marketed for bodybuilding or performance enhancement. The lack of a standardized pharmaceutical supply means identity, purity, and contamination levels can differ widely between samples. These factors make cardarine a regulatory and public health concern rather than a conventional prescription drug.

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.

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.

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

Further detail

Butyrylcholinesterase deficiency (also known as pseudocholinesterase deficiency, and Succinylcholine Sensitivity is an autosomal recessive inherited blood plasma enzyme abnormality in which the body's production of butyrylcholinesterase (BChE) is impaired. People who have this abnormality may be sensitive to certain anesthetic drugs, including the muscle relaxants succinylcholine and mivacurium as well as other ester local anesthetics. It is classed as an inborn error of metabolism in ICD11.

The ACAM2000 vaccine is produced from the vaccinia virus, which is sufficiently closely related to smallpox to provide immunity, but the ACAM2000 vaccine cannot cause smallpox because it does not contain the smallpox virus. Other vaccines containing live viruses include measles, mumps, rubella, polio and chickenpox. The vaccine is administered using a bifurcated stainless steel needle. The needle is dipped into the vaccine solution and used to prick the skin several times in the upper arm. The vaccinia virus will begin to grow at the injection site. It will cause a localized infection, with a red itchy sore produced at the vaccination site within three to four days. If the infection occurs, that is an indication that the vaccine was successful. Ultimately, the sore turns into a blister and then dries up. A scab forms and then falls off in the third week, leaving a small scar behind.

In patients with familial hyperaldosteronism type 1, there is a genetic crossover between specific regions of the CYP11B1 and CYP11B2 genes. This crossover results in the expression of an additional gene in the zona fasciculata, which is regulated by ACTH. The additional gene plays a role in synthesizing 18-hydroxycortisol by 18-hydroxylation of cortisol. This gene also plays a role in the biosynthesis of aldosterone and 18-oxocortisol. Cortisol 18-Hydroxycorticosterone 18-Oxocortisol Aldosterone synthase Steroid 11β-hydroxylase 6β-Hydroxycortisol

Subfamily ABCC contains thirteen members and nine of these transporters are referred to as the Multidrug Resistance Proteins (MRPs). The MRP proteins are found throughout nature and they mediate many important functions. They are known to be involved in ion transport, toxin secretion, and signal transduction. Of the nine MRP proteins, four of them, MRP4, 5, 8, 9, (ABCC4, 5, 11, and 12), have a typical ABC structure with four domains, comprising two membrane spanning domains, with each spanning domain followed by a nucleotide binding domain. These are referred to as short MRPs. The remaining 5 MRP's (MRP1, 2, 6, 7) (ABCC1, 2, 3, 6 and 10) are known as long MRPs and feature an additional fifth domain at their N terminus. CFTR, the transporter involved in the disease cystic fibrosis, is also considered part of this subfamily. Cystic fibrosis occurs upon mutation and loss of function of CFTR. The sulfonylurea receptors (SUR), involved in insulin secretion, neuronal function, and muscle function, are also part of this family of proteins. Mutations in SUR proteins are a potential cause of Neonatal diabetes mellitus. SUR is also the binding site for drugs such as sulfonylureas and potassium-channel openers activators such as diazoxide.

NETA metabolizes into ethinylestradiol at a rate of 0.20 to 0.33% across a dose range of 10 to 40 mg. Peak levels of ethinylestradiol with a 10, 20, or 40 mg dose of NETA were 58, 178, and 231 pg/mL, respectively. For comparison, a 30 to 40 μg dose of oral ethinylestradiol typically results in a peak ethinylestradiol level of 100 to 135 pg/mL. As such, in terms of ethinylestradiol exposure, 10 to 20 mg NETA may be equivalent to 20 to 30 μg ethinylestradiol and 40 mg NETA may be similar to 50 μg ethinylestradiol. In another study however, 5 mg NETA produced an equivalent of 28 μg ethinylestradiol (0.7% conversion rate) and 10 mg NETA produced an equivalent of 62 μg ethinylestradiol (1.0% conversion rate). Due to its estrogenic activity via ethinylestradiol, high doses of NETA have been proposed for add-back in the treatment of endometriosis without estrogen supplementation. Generation of ethinylestradiol with high doses of NETA may increase the risk of venous thromboembolism but may also decrease menstrual bleeding relative to progestogen exposure alone.

Sources: en.wikipedia.org

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Supporting material

Automated iterative homologation enables stepwise construction of carbon chains through repeated one-carbon extensions of boronic esters. Two reactions adapted to automation are the Matteson homologation, which inserts a methylene unit via chloromethyllithium, and chiral carbenoid homologation, which uses lithiated benzoate esters. Both methods have been implemented on robotic platforms under low-temperature, inert conditions. Using these techniques, up to six consecutive C(sp³)–C(sp³) bond-forming homologations have been performed without manual intervention, representing the highest number reported in an automated synthesis. The approach has also been applied to the synthesis of intermediates of the natural product (+)-kalkitoxin.

Instead, they stretch to compensate for dead cells which reduces the overall cell density of the endothelium, which affects fluid regulation. If the endothelium can no longer maintain a proper fluid balance, stromal swelling due to excess fluids and subsequent loss of transparency will occur and this may cause corneal edema and interference with the transparency of the cornea and thus impairing the image formed. Iris pigment cells deposited on the corneal endothelium can sometimes be washed into a distinct vertical pattern by the aqueous currents - this is known as Krukenberg's Spindle.

== Tissue distribution == Type III collagen is found as a major structural component in hollow organs such as large blood vessels, uterus and bowel. It is also found in many other tissues together with type I collagen.

Much of the genetic manipulation done in CHO cells is done in cells lacking DHFR enzyme. This genetic selection scheme remains one of the standard methods to establish transfected CHO cell lines for the production of recombinant therapeutic proteins. The process begins with the molecular cloning of the gene of interest and the DHFR gene into a single mammalian expression system. The plasmid DNA carrying the two genes is then transfected into cells, and the cells are grown under selective conditions in a thymidine-lacking medium. Surviving cells will have the exogenous DHFR gene along with the gene of interest integrated in its genome. The growth rate and the level of recombinant protein production of each cell line varies widely. To obtain a few stably transfected cell lines with the desired phenotypic characteristics, evaluating several hundred candidate cell lines may be necessary. The CHO and CHO-K1 cell lines can be obtained from a number of biological resource centres such as the European Collection of Cell Cultures, which is part of the Health Protection Agency Culture Collections. These organizations also maintain data, such as growth curves, timelapse videos of growth, images, and subculture routine information.

Sources: en.wikipedia.org

Notes from published material

{\displaystyle \langle \Psi _{nlm_{l}m_{s}}|\mu |\Psi _{n'l'm_{l}'m_{s}'}\rangle } For example in the E1 transition, unless Δ l = ± 1, Δ ml = 0 or ± 1, Δ ms = 0, and Δ n = any integer, the equation above will yield a value equal to zero and the transition would be known as a “forbidden transition”. For example, this would occur for certain cases like when Δ l = 2. In this case, the transition would not be allowed and therefore would be much weaker than an allowed transition. These specific values for the changes in quantum numbers are known as the selection rules for the allowed transitions and are shown for common transitions in the table below: Cold vapour atomic fluorescence spectroscopy Atomic spectral line Prospects in Analytical Atomic Spectrometry – tendencies in five main branches of atomic spectrometry (absorption, emission, mass, fluorescence and ionization spectrometry) Learning by Simulations – various atomic absorption and emission spectra Atomic Spectroscopy: A Compendium of Basic Ideas, Notation, Data, and Formulas

The molecular weight of c7orf26 is 50 kilodaltons. The isoelectric point is 7.61. The protein sequence is uniquely rich for leucine at 15.8% of its composition, this may indicate a leucine-zipper. Further analysis from PSORT indicates that a leucine-zipper region is found at amino acid 318 and lasts until position 340 (22 amino acids long). There are no extremes with regards to acidity and alkalinity. c7orf26 has a positive charge cluster from amino acid 245 – 275 and does not have any negative, or mixed charge clusters. An even distribution of amino acids compose c7orf26. The percent composition of each amino acid is fairly consistent throughout the orthologs of the protein. The most distant ortholog displays the most variance in amino acid composition. There is a higher percent composition of tyrosine, histidine and leucine and a lower composition of valine and alanine.

1-Ethyl-3-(3-dimethylaminopropyl)carbodiimide (EDC, EDAC or EDCI) is a water-soluble carbodiimide usually handled as the hydrochloride, which is a white solid. It is typically employed in the 4.0-6.0 pH range. It is generally used as a carboxyl activating agent for the coupling of primary amines to yield amide bonds. While other carbodiimides like dicyclohexylcarbodiimide (DCC) or diisopropylcarbodiimide (DIC) are also employed for this purpose, EDC has the advantage that the urea byproduct formed (often challenging to remove in the case of DCC or DIC) can be washed away from the amide product using dilute acid. Additionally, EDC can also be used to activate phosphate groups in order to form phosphomonoesters and phosphodiesters. Common uses for this carbodiimide include peptide synthesis, protein crosslinking to nucleic acids, but also in the preparation of immunoconjugates. EDC is often used in combination with N-hydroxysuccinimide (NHS) for the immobilisation of large biomolecules. Recent work has also used EDC to assess the structure state of uracil nucleobases in RNA.

Luis Moroder (6 December 1940 – 18 May 2024) was an Italian peptide chemist, who pioneered research on the interactions between peptide hormones and cell membrane-bound hormone receptors. He later expanded this research to other biological systems of medical relevance such as protein inhibitors, collagens, and synthetic proteins. A hallmark of his research is interdisciplinarity as reflected in his use and development of methods in organic chemistry, biophysics and molecular biology. He was a co-editor of the five-volume Houben-Weyl, Methods of Organic Chemistry, Synthesis of Peptides and Peptidomimetics. From 2008 he was the editor-in-chief of the Journal of Peptide Science, the official journal of the European Peptide Society.

DT56a has been described in scientific literature as a selective estrogen receptor modulator (SERM)-like compound. Experimental studies have suggested that DT56a may exert agonistic effects on estrogen receptors in bone and brain tissues, while demonstrating limited activity in uterine and breast tissues. Several studies have investigated DT56a in relation to menopausal symptoms and bone health. In vitro studies have also reported stimulation of osteoblast activity in cultured human bone cells. Published studies have additionally suggested that DT56a does not significantly affect circulating hormone levels or blood coagulation parameters. Selective estrogen receptor modulator

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.

Is cardarine a selective androgen receptor modulator?

No. Cardarine is a PPARδ agonist, while selective androgen receptor modulators act on androgen receptors. The two classes differ in receptor target and downstream effects.

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