Cardarine comes up often in conversation and rarely with the context attached. Here we lay out the basics in order, then work through the practical considerations.
Last reviewed on 2025-12-18. Where a claim depends on a specific study, the study is described rather than over-claimed.
GW501516 acts as a selective agonist at PPARδ, a nuclear receptor that regulates transcription of genes involved in lipid handling and energy metabolism. Activation of PPARδ in preclinical models increases fatty acid oxidation, mitochondrial biogenesis, and exercise endurance in rodents. These effects have made the compound a subject of metabolic research and also a target for sport anti-doping rules. In humans, however, controlled studies are limited, and whether similar endurance or metabolic changes occur at tolerated exposures remains an open question. The receptor’s broad tissue distribution also means downstream effects may vary by organ and condition.
Detection of GW501516 in biological samples generally relies on liquid chromatography coupled with tandem mass spectrometry. Urine is a common matrix in anti-doping analysis, while blood or plasma may be used in research settings. Sample preparation can involve enzymatic hydrolysis, protein precipitation, or solid-phase extraction before instrumental analysis. Because the compound undergoes metabolism, assays may target the parent molecule, one or more metabolites, or both. Detection windows are not fixed; they depend on factors such as dose, route, individual metabolism, and assay sensitivity. Reference standards are required for accurate identification and quantification.
Handling and quality assessment of cardarine reference material follow general laboratory practices for poorly characterized compounds. It typically appears as a white to off-white powder and is sparingly soluble in water but soluble in organic solvents such as dimethyl sulfoxide and ethanol. Storage recommendations usually specify a cool, dry, dark place, with long-term storage at low temperature and desiccation. Purity may be checked by high-performance liquid chromatography with ultraviolet detection, while identity is confirmed by mass spectrometry and nuclear magnetic resonance. No pharmacopeial monograph exists, so reported purity and stability depend on the supplier’s methods.
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.
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.
| Property | Value | Notes |
|---|---|---|
| Appearance | White to off-white powder | Visual description for typical solid reference material. |
| Solubility | Poorly soluble in water; soluble in DMSO | Solubility depends on solvent, purity, and form. |
| Storage | Cool, dry, protected from light | Long-term storage often uses low temperature and desiccant. |
| Common analytical method | LC-MS/MS | Used for detection and quantification in biological matrices. |
| Common synonyms | GW-501516; GW501516; endurobol | Naming varies among literature, vendors, and databases. |
Cardarine is prohibited in competitive sport under the World Anti-Doping Agency code, where it is classified as a metabolic modulator. It is not approved as a prescription medicine in the United States, European Union, or other major markets. Regulatory action has focused on its presence in sports and in products marketed as research chemicals. Because it has no accepted medical indication, supply is often unregulated. This status creates legal and safety uncertainties for anyone who encounters the substance.
Anti-doping laboratories detect GW501516 and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is the most common matrix, though blood and dried blood spots may also be used in some programs. Detection depends on factors such as dose, timing, metabolism, and the sensitivity of the assay. Published methods describe limits of detection in the low nanogram per milliliter range for related compounds. Exact detection windows are not fixed for all situations and remain an area of ongoing study.
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 reading == The American Food Journal. American Food Journal, Incorporated. 1921. pp. 11–12. Retrieved May 23, 2017. Peter, K.V. (2004). Handbook of Herbs and Spices. Handbook of Herbs and Spices. CRC Press. p. 280. ISBN 978-1-85573-721-1. Retrieved May 24, 2017. Lovegren, S. (2005). Fashionable Food: Seven Decades of Food Fads. University of Chicago Press. p. 228. ISBN 978-0-226-49407-4. Retrieved May 23, 2017. Davis, E.L. (2009). Encyclopedia of Contemporary Chinese Culture. Encyclopedias of Contemporary Culture Series. Routledge. p. 385. ISBN 978-0-415-77716-2. Retrieved May 24, 2017. Solt, G. (2014). The Untold History of Ramen: How Political Crisis in Japan Spawned a Global Food Craze. California Studies in Food and Culture. University of California Press. p. 113. ISBN 978-0-520-27756-4. Retrieved May 24, 2017. Mehta, Foram (August 12, 2016). "New Research Shows Instant Noodles are Especially Harmful for Women". India.com. Retrieved May 24, 2017.
=== Luna Diabetes === Former founders of Timesulin, Welldoc, Companion Medical and Bigfoot Biomedical have joined together to create the world's first automated insulin delivery system for those that want to continue to use insulin pens. The team is calling it Episodic AID. The working product name is Luna.
=== No development reported === AB-101 (RJ-101) – topical – alopecia – undefined mechanism of action BRM-421 (GPN-00136, PDSP) – topical – alopecia – cell proliferation stimulant Dimethylcurcumin (ASC-J9, AJ-101) – topical – male pattern baldness – androgen receptor degradation enhancer Lepzacitinib (ATI-1777) – topical – alopecia areata – Janus kinase 1 inhibitor, Janus kinase 3 inhibitor PF-277343 – unspecified – alopecia – undefined mechanism of action Research programme: janus kinase inhibitors - Aclaris Therapeutics/ JAKPharm – unknown – alopecia areata – Janus kinase 3 inhibitors Research programme: skin diseases therapeutics - Quark Pharmaceuticals (QP-AL1; QP-AL2) – unknown – alopecia (chemotherapy-induced) – RNA interference Research programme: stem cell therapeutics - Histostem (Cirrhosis HMScs) – unknown – alopecia – cell replacement Synephrine (AB-102) – topical – alopecia – α1-adrenergic receptor agonist Valproic acid (VPA spray) – topical – male pattern baldness – glycogen synthase kinase 3β inhibitor, Wnt signalling pathway stimulant
Sources: en.wikipedia.org
The Golgi matrix is a protein scaffold around the Golgi apparatus made up of Golgins, GRASP's and miscellaneous other proteins on the cytoplasmic side of the Golgi apparatus involved in keeping its shape and membrane stacking.
=== Otospondylomegaepiphyseal dysplasia === Approximately 10 mutations identified in the COL11A2 gene are responsible for otospondylomegaepiphyseal dysplasia (OSMED). Most of these mutations result in a complete lack of pro-alpha2(XI) chains, which leads to a loss of function of type XI collagen. Some mutations affect the production of the pro-alpha2(XI) chain and disrupt normal collagen assembly. Because this type of collagen is an important component of cartilage and other connective tissues, these mutations result in the characteristic signs and symptoms of OSMED.
In bovine corneas, the length of the CS/DS proteoglycans is about 70 nm, while the KS proteoglycans are about 40 nm long. Proteoglycan protein cores attach to the surface of the collagen fibrils with the GAG chains projecting outwards. The GAG chains are able to form antiparallel links with other GAG chains from adjacent fibrils, perhaps through the mediation of positively charged ions. In such a way, bridges are formed between adjacent collagen fibrils. These bridges are subject to thermal motion which prevents them from assuming a fully extended conformation. This results in forces that tend to move adjacent fibrils close to each other. At the same time the charges on the GAG chains attract ions and water molecules by the Donnan effect. The increased water volume between the fibrils results in forces that tend to push the fibrils apart. A balance between attractive and repulsive forces is reached for specific inter-fibrillar distances, which depends on the type of proteoglycans present. Locally, the separations between adjacent collagen fibrils are very uniform. Stromal transparency is mainly a consequence of the remarkable degree of order in the arrangement of the collagen fibrils in the lamellae and of fibril diameter uniformity. Light entering the cornea is scattered by each fibril. The arrangement and the diameter of the fibrils is such that scattered light interferes constructively only in the forward direction, allowing the light through to the retina.
Sources: en.wikipedia.org
=== Pre-discovery === In the late 1940s to early 1960s, the early days of making heavier and heavier transuranic elements, it was predicted that since such elements did not occur naturally, they would have shorter and shorter spontaneous fission half-lives, until they stopped existing altogether around element 108 (now called hassium). Initial work in synthesizing the heavier actinides seemed to confirm this. But the nuclear shell model, introduced in 1949 and extensively developed in the late 1960s by William Myers and Władysław Świątecki, stated that protons and neutrons form shells within a nucleus, analogous to electron shells. Noble gases are unreactive due to a full electron shell; similarly, it was theorized that elements with full nuclear shells – those having "magic" numbers of protons or neutrons – would be stabilized against decay. A doubly magic isotope, with magic numbers of both protons and neutrons, would be especially stabilized. Heiner Meldner calculated in 1965 that the next doubly magic isotope after 208Pb was 298Fl with 114 protons and 184 neutrons, which would be the centre of an "island of stability". This island of stability, supposedly from copernicium (Z = 112) to oganesson (Z = 118), would come after a long "sea of instability" from mendelevium (Z = 101) to roentgenium (Z = 111), and the flerovium isotopes in it were speculated in 1966 to have half-lives over 108 years. These early predictions fascinated researchers, and led to the first attempt to make flerovium, in 1968 with the reaction 248Cm(40Ar,xn).
=== Use in pregnancy and lactation === Pioglitazone/metformin should not be used during pregnancy unless the potential benefit justifies the potential risk to the fetus. There are no adequate and well-controlled studies in pregnant women with combination of pioglitazone and metformin or its individual components. It is not known whether pioglitazone and/or metformin are secreted in human milk. Because many drugs are excreted in human milk, pioglitazone/metformin should not be administered to a breastfeeding woman.
=== Abuse of migrants === According to Human Rights Watch, Houthi militias have "beaten, raped, and tortured detained migrants and asylum seekers from the Horn of Africa." UN experts have warned that female migrants face sexual violence, forced labor, and forced drug trafficking by smugglers who collaborate with the Houthi-controlled Yemen Immigration, Passport and Nationality Authority (IPNA).
Sources: en.wikipedia.org
Cardarine targets PPARδ, a nuclear receptor involved in lipid and energy metabolism. It does not bind the androgen receptor in the way SARMs do.
Most methods use liquid chromatography with tandem mass spectrometry. Urine is common in anti-doping testing, and blood or plasma may be used in research.
Typical guidance is cool, dry, dark storage, often at low temperature and with desiccant. Stability data are limited, so storage conditions should be verified for each batch or supplier.
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.