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Background And Regulatory Status — Beginner to Advanced

By Editorial Desk · published 2025-12-16 · last reviewed 2026-01-02 · Topic

The short version of GW501516 fits in a sentence. The long version — which is the one that helps — is below.

This page was last updated on 2026-01-02 and is reviewed periodically as new material appears.

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.

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.

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.

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.

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

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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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.

Notes from published material

RANKL is a member of the TNF superfamily of ligands. Through binding to the RANK receptor it activates various molecules, like NF-kappa B, MAPK, NFAT and PI3K52. The RANKL/RANK signaling pathway regulates osteoclastogenesis, as well as, the survival and activation of osteoclasts. Adenosine is very relevant in bone metabolism, as it plays a role in formation and activation of both osteoclasts and osteoblasts. Adenosine acts by binding to purinergic receptors and influencing adenylyl cyclase activity and the formation of cAMP and PKA 54. Adenosine may have opposite effects on bone metabolism, because while certain purinergic receptors stimulate adenylyl cyclase activity, others have the opposite effect. Under certain circumstances adenosine stimulates bone destruction and in other situations it promotes bone formation, depending on the purinergic receptor that is being activated.

In response to a stimulus, GPCRs activate heterotrimeric G proteins. In order to turn off this response, or adapt to a persistent stimulus, active receptors need to be desensitized. The first step in desensitization is phosphorylation of the receptor by a class of serine/threonine kinases called G protein coupled receptor kinases (GRKs). GRK phosphorylation specifically prepares the activated receptor for arrestin binding. Arrestin binding to the receptor blocks further G protein-mediated signaling and targets receptors for internalization, and redirects signaling to alternative G protein-independent pathways, such as β-arrestin signaling. In addition to GPCRs, arrestins bind to other classes of cell surface receptors and a variety of other signaling proteins. Mammals express four arrestin subtypes and each arrestin subtype is known by multiple aliases. The systematic arrestin name (1–4) plus the most widely used aliases for each arrestin subtype are listed in bold below:

While AM could be an important biomarker for bacterial infections like sepsis, AM has diminished value in its utility for cardiovascular diseases (CVD), attributable to its minimal increase in these conditions and reduced half-life. AM is associated with controlling vascular integrity, blood pressure, and general cardiovascular function. Since AM has been noted for its exacerbated levels in intense diseases with an elevated concern for mortality, AM could still have some value as a predictive biomarker of harmful clinical consequences for an array of cardiovascular illnesses. AM has conservatory effects against arteriosclerosis and vascular harm. Extended AM administration or hyper-expression of its target gene in rodent model organisms diminishes vascular hyperplasia, fatty streak construction, and intimal expansion. AM also has angiogenic characteristics, leading to organ and tissue maintenance by reducing the risk of ischemic diseases. AM binds to particular receptors like calcitonin gene-related peptide (CGRP) receptors, which affects the cardiovascular system by contributing to vasodilation as well as elevated heart rate and blood pressure.

Sources: en.wikipedia.org

Further detail

Unlike anandamide, formation of 2-AG is calcium-dependent and is mediated by the activities of phospholipase C (PLC) and diacylglycerol lipase (DAGL). 2-AG acts as a full agonist at the CB1 receptor. At a concentration of 0.3 nM, 2-AG induces a rapid, transient increase in intracellular free calcium in NG108-15 neuroblastoma X glioma cells through a CB1 receptor-dependent mechanism. 2-AG is hydrolyzed in vitro by monoacylglycerol lipase (MAGL), fatty acid amide hydrolase (FAAH), and the uncharacterized serine hydrolase enzymes ABHD2, ABHD6 and ABHD12. The exact contribution of each of these enzymes to the termination of 2-AG signaling in vivo is unknown, though it is estimated that MAGL is responsible for ~85% of this activity in the brain. There have been identified transport proteins for 2-arachidonoylglycerol and anandamide. These include the heat shock proteins (Hsp70s) and fatty acid binding proteins (FABPs).

Amylopectin-based fibers have been fabricated mainly by blending native or modified starches with polymers, plasticizers, cross-linkers, or other additives. Most amylopectin-based fibers are fabricated by electro-wet-spinning, however, the method is demonstrated to be suitable for starches with amylopectin content below 65% and sensitive to amylopectin content of starches. Electrospinning allows for amylopectin to coagulate and form a filament. Fibrous starches induce a more dense material, which can optimize the mechanical properties of starch. Fibers in biomaterials can be used for bone tissue engineering as suitable environment for bone tissue repair and regeneration. Natural bone is a complex composite material composed of an extracellular matrix of mineralized fibers containing living cells and bioactive molecules. Consequently, the use of fibers in biomaterial-based scaffolds offers a wide variety of opportunities to replicate the functional performance of bone. In the last decade, fiber-based techniques such as weaving, knitting, braiding, as well as electrospinning, and direct writing have emerged as promising platforms for making 3D tissue constructs.

The 2025 Cleveland Guardians season was the 125th season for the franchise, which competes in the American League of Major League Baseball (MLB). On July 6, they were 15.5 games back of the first place Detroit Tigers and were as many as 11 games back on September 4. However, the Guardians surged while the Tigers collapsed and took the American League Central lead on September 23 with a win over the Tigers. With the Guardians having trailed Detroit by 15.5 games in July, this ranked as the largest divisional comeback in MLB history. In addition to the historic division comeback, the Guardians also became the fifth team to make the playoffs while being sub-.500 on September 4 or later. On September 27, with a walk-off win over the Texas Rangers, the Guardians clinched a postseason berth, taking the sixth and final postseason spot in the American League. On September 28, with the Tigers' loss to the Red Sox, the Guardians clinched the American League Central division for the second consecutive time and the sixth time in ten years (2016–2018, 2022, 2024–2025). However, they lost to the Tigers in the Wild Card Series.

Sources: en.wikipedia.org

Supporting material

The characterization of the caspases allowed the development of caspase inhibitors, which can be used to determine whether a cellular process involves active caspases. Using these inhibitors, it was discovered that cells can die while displaying a morphology similar to apoptosis without caspase activation. Later studies linked this phenomenon to the release of AIF (apoptosis-inducing factor) from the mitochondria and its translocation into the nucleus mediated by its nuclear localization signal (NLS). Inside the mitochondria, AIF is anchored to the inner membrane. In order to be released, the protein is cleaved by a calcium-dependent calpain protease. Anoikis Apaf-1 Apo2.7 Apoptotic DNA fragmentation Atromentin induces apoptosis in human leukemia U937 cells. Autolysis Autophagy Cisplatin Cytotoxicity Entosis Ferroptosis Homeostasis Immunology Necrobiosis Necrosis Necrotaxis Nemosis Mitotic catastrophe p53 Paraptosis Pseudoapoptosis PI3K/AKT/mTOR pathway Ruptosis

In molecular biology, the BSD domain is an approximately 60-amino-acid-long protein domain named after the BTF2-like transcription factors, synapse-associated proteins and DOS2-like proteins in which it is found. It is also found in several hypothetical proteins. It occurs in one or two copies in a variety of species ranging from primal protozoan to human, and can be found associated with other domains such as the BTB domain or the U-box in multidomain proteins. Its function is as yet unknown. Secondary structure prediction indicates the presence of three predicted alpha helices, which probably form a three-helical bundle in small |domains. The third predicted helix contains neighbouring phenylalanine and tryptophan residues—less common amino acids that are invariant in all the BSD domains identified and that are the domain's most striking sequence features. Some proteins known to contain one or two BSD domains are:

A decreased renal function can be caused by many types of kidney disease. Upon presentation of decreased renal function, it is recommended to perform a history and physical examination, as well as performing a renal ultrasound and a urinalysis. The most relevant items in the history are medications, edema, nocturia, gross hematuria, family history of kidney disease, diabetes and polyuria. The most important items in a physical examination are signs of vasculitis, lupus erythematosus, diabetes, endocarditis and hypertension. A urinalysis is helpful even when not showing any pathology, as this finding suggests an extrarenal etiology. Proteinuria and/or urinary sediment usually indicates the presence of glomerular disease. Hematuria may be caused by glomerular disease or by a disease along the urinary tract. The most relevant assessments in a renal ultrasound are renal sizes, echogenicity and any signs of hydronephrosis. Renal enlargement usually indicates diabetic nephropathy, focal segmental glomerular sclerosis or myeloma. Renal atrophy suggests longstanding chronic renal disease.

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 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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