A practical reference on Cardarine: what it is, how it behaves, what the literature reports, and where the honest uncertainties sit.
This page was last updated on 2026-05-27 and is reviewed periodically as new material appears.
GW501516 acts as a ligand for PPAR delta, a nuclear receptor that regulates transcription of genes involved in fatty acid oxidation and energy use. Activation of this receptor in skeletal muscle shifts metabolism toward fat burning in animal models. The compound does not burn fat directly; it changes gene expression over hours to days. Researchers study it to understand metabolic flexibility and exercise adaptation. Effects observed in rodents are not automatically expected in humans.
Preclinical research reported that GW501516 increased running endurance in mice and improved lipid profiles in some animal species. Early human trials explored effects on high-density lipoprotein cholesterol, triglycerides, and glucose handling, but the program was discontinued. Published human data are sparse and do not establish efficacy for any condition. Studies also examined PPAR delta in cancer biology, with conflicting findings across models. The relationship between receptor activation, tissue context, and disease risk remains an active area of investigation.
Anti-doping laboratories identify GW501516 and its metabolites using liquid chromatography-tandem mass spectrometry. Urine is the usual matrix, and detection can occur after the parent compound has cleared from blood. The exact detection window depends on dose, formulation, individual metabolism, and assay sensitivity. Because the compound is prohibited at all times, athletes are subject to testing in and out of competition. Analytical methods continue to improve as new metabolites and designer analogs are characterized.
GW501516 acts as an agonist at the peroxisome proliferator-activated receptor delta, a nuclear receptor that regulates gene expression. Activation shifts transcription toward genes involved in fatty acid uptake, oxidation, and energy expenditure. The compound does not bind the androgen receptor and therefore differs from anabolic steroids and SARMs. In rodent models, this metabolic shift has been linked to increased running endurance and reduced fat accumulation. The exact downstream pathways in humans remain incompletely characterized.
Early clinical research explored GW501516 for lipid disorders, obesity, and diabetes. Some short-term human studies reported changes in HDL cholesterol, LDL cholesterol, and triglycerides. The development program was discontinued after rodent studies showed dose-dependent tumor formation in multiple tissues, including liver, bladder, stomach, and skin. These findings raised concerns about long-term cancer risk in humans. Because human exposure data are limited, the clinical significance of the rodent tumors remains uncertain.
| Property | Value | Notes |
|---|---|---|
| Molecular target | PPAR delta (NR1C2) | Ligand-activated nuclear receptor. |
| Primary tissues studied | Skeletal muscle, liver, adipose | Effects on fatty acid oxidation and energy use. |
| Typical detection matrix | Urine | Used in anti-doping analysis. |
| Common analytical method | LC-MS/MS | Detects parent compound and metabolites. |
| Sport regulatory class | Prohibited at all times | Listed as a metabolic modulator by WADA. |
Cardarine is a common name for GW501516, also GW-1516, a synthetic compound developed as a peroxisome proliferator-activated receptor delta (PPARδ) agonist. It belongs to a class of agents that modulate gene transcription related to lipid and energy metabolism. The compound was studied in preclinical and early clinical research for metabolic and cardiovascular conditions, but it did not progress to approved therapeutic use. Its name appears in fitness and sports contexts despite not being approved as a drug.
PPARδ is a nuclear receptor that influences transcription of genes involved in fatty acid oxidation, lipid transport, and energy homeostasis. GW501516 binds and activates this receptor with high selectivity relative to PPARα and PPARγ in laboratory assays. Activation alters expression of target genes in skeletal muscle, liver, and adipose tissue in animal models. The exact clinical consequences of these changes in humans remain incompletely characterized, and observed effects in animals do not establish therapeutic benefit or safety.
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.
Published human data are sparse and mostly come from early-phase trials. Those studies examined short-term changes in lipids, glucose, and exercise capacity, but they were not large enough to establish efficacy or long-term safety. Some animal experiments reported increased running endurance, yet such findings do not prove a performance benefit in people. Anti-doping laboratories detect GW501516 and its metabolites in urine or blood using liquid chromatography-tandem mass spectrometry. Detection windows depend on dose, sample type, and individual metabolism. The method is sensitive enough to identify trace residues in tested samples.
Laboratory handling focuses on identity, purity, and stability. Reference standards are typically stored cold and dry, protected from light, because solutions can degrade over time. Analytical checks may use high-performance liquid chromatography with ultraviolet detection or mass spectrometry. Impurities and related substances can be separated chromatographically and compared with a known standard. Because cardarine is not an approved drug, compendial monographs are absent, and laboratories often rely on in-house methods. Reported purity varies among unregulated products and should not be assumed from a label.
Isotope masses from: M. Wang; G. Audi; A. H. Wapstra; F. G. Kondev; M. MacCormick; X. Xu; et al. (2012). "The AME2012 atomic mass evaluation (II). Tables, graphs and references" (PDF). Chinese Physics C. 36 (12): 1603–2014. Bibcode:2012ChPhC..36....3M. doi:10.1088/1674-1137/36/12/003. hdl:11858/00-001M-0000-0010-23E8-5. S2CID 250839471. Archived from the original (PDF) on 2013-09-28. Retrieved 2013-07-03. Audi, Georges; Bersillon, Olivier; Blachot, Jean; Wapstra, Aaldert Hendrik (2003), "The NUBASE evaluation of nuclear and decay properties", Nuclear Physics A, 729: 3–128, Bibcode:2003NuPhA.729....3A, doi:10.1016/j.nuclphysa.2003.11.001 Half-life, spin, and isomer data selected from the following sources. Audi, Georges; Bersillon, Olivier; Blachot, Jean; Wapstra, Aaldert Hendrik (2003), "The NUBASE evaluation of nuclear and decay properties", Nuclear Physics A, 729: 3–128, Bibcode:2003NuPhA.729....3A, doi:10.1016/j.nuclphysa.2003.11.001 National Nuclear Data Center. "NuDat 3.0 database". Brookhaven National Laboratory. Holden, Norman E. (2004). "11. Table of the Isotopes". In Lide, David R. (ed.). CRC Handbook of Chemistry and Physics (85th ed.). Boca Raton, Florida: CRC Press. ISBN 978-0-8493-0485-9.
== Antivenom == Antivenom, or antivenin, is commonly used to treat the effects of local and systemic pit viper envenomations. The first step in the production of crotaline antivenom is collecting ("milking") the venom of a live rattlesnake—usually from the western diamondback (Crotalus atrox), eastern diamondback (Crotalus adamanteus), South American rattlesnake (Crotalus durissis terrificus), or fer-de-lance (Bothrops atrox). The extracted venom is then diluted and injected into horses, goats, or sheep, whose immune systems produce antibodies that protect from the toxic effects of the venom. These antibodies accumulate in the blood, which is then extracted and centrifuged to separate the red blood cells. The resulting serum is purified into a lyophilized powder, which is packaged for distribution and later use by human patients. Because antivenom is derived from animal antibodies, people generally display an allergic response during infusion, known as serum sickness.
=== Ontologies and data integration === Biological ontologies are directed acyclic graphs of controlled vocabularies. They create categories for biological concepts and descriptions so they can be easily analyzed with computers. When categorised in this way, it is possible to gain added value from holistic and integrated analysis. The OBO Foundry was an effort to standardise certain ontologies. One of the most widespread is the Gene ontology which describes gene function. There are also ontologies which describe phenotypes.
Sources: en.wikipedia.org
=== Worms === Levamisole was originally used as an anthelmintic to treat worm infestations in both humans and animals. Levamisole works as a nicotinic acetylcholine receptor agonist that causes continued stimulation of the parasitic worm muscles, leading to paralysis. Levamisole has gained prominence among aquarists as an effective treatment for Camallanus roundworm infestations in freshwater tropical fish. Levamisole has been used to treat small ruminant animals since the late 1960s. Levamisole-resistant parasitic worms are common in sheep farms in New Zealand, Uruguay, Paraguay, and Brazil.
Hypophosphatemia is an electrolyte disorder in which there is a low level of phosphate in the blood. Symptoms may include weakness, trouble breathing, and loss of appetite. Complications may include seizures, coma, rhabdomyolysis, or softening of the bones. Nutritional phosphate deficiency is exceedingly rare as phosphate is abundant in most types of foods and is readily passively absorbed from the gastrointestinal tract; hypophosphatemia is thus typically a result of diseases or an adverse effect of medical treatments. Causes include alcohol use disorder, refeeding in those with malnutrition, recovery from diabetic ketoacidosis, burns, hyperventilation, and certain medications. It may also occur in the setting of hyperparathyroidism, hypothyroidism, and Cushing syndrome. It is diagnosed based on a blood phosphate concentration of less than 0.81 mmol/L (2.5 mg/dL). When levels are below 0.32 mmol/L (1.0 mg/dL), it is deemed to be severe. Treatment depends on the underlying cause. Phosphate may be given by mouth or by injection into a vein. Hypophosphatemia occurs in about 2% of people within hospital and 70% of people in the intensive care unit (ICU).
== Career == After the break-up of the Beat in 1983 (known as the English Beat in North America), vocalists Dave Wakeling and Ranking Roger decided to continue working together in a new venture. They joined up with keyboardist Mickey Billingham (Dexys Midnight Runners), guitarist Mick Jones (the Clash), bassist Horace Panter (the Specials) and drummer Stoker (Dexys Midnight Runners/the Bureau) to form a supergroup of the UK punk and ska scene. They named the band General Public and were rapidly signed to Virgin Records in the UK and I.R.S. Records in North America. The band recorded and released the album All the Rage in 1984. Jones left General Public part way through the recording process, but he is listed in the album's inner sleeve credits as a group member (although he did not appear in any of the band photographs for the album cover). Jones' replacement, guitarist Kevin White, also played on the album and was also listed as an official group member. White's picture also appeared on the album's back cover. In the UK, General Public had a minor hit with the track "General Public", which reached No. 60 in the UK singles chart in 1984. The single's B-side "Dishwasher" (an instrumental mix of "Burning Bright" from All The Rage) became a surprise Top 40 hit in the Netherlands, after its use as a closing theme tune to the pop radio show Avondspits. Later in the year, the band fared even better in North America, where their second single "Tenderness" was a Top 30 hit in Canada (No. 11) and the US (No. 27).
Sources: en.wikipedia.org
== Medical uses == Ciprofol is used for the intravenous induction of general anesthesia. Studies published in 2022 and 2023 found it was efficacious as a general anesthetic in people undergoing gynecological surgery and kidney transplantation, as well as for endoscopic procedures such as bronchoscopy, esophagogastroduodenoscopy and colonoscopy. Ciprofol has also been used for sedation of critically ill people undergoing mechanical ventilation in the intensive care unit, as well as for the treatment of agitation and delirium in that patient population. When combined with mild therapeutic hypothermia, ciprofol may also be useful as a cerebral protective agent in the setting of cerebral ischemia-reperfusion injury.
Substantial cephalopelvic disproportion Unfavorable fetal position or presentation (e.g., transverse lies) undeliverable without conversion before delivery Obstetric emergencies where maternal or fetal risk-to-benefit ratio favors surgery Fetal distress when delivery is not imminent Umbilical cord prolapse Uterine activity fails to progress adequately Hyperactive or hypertonic uterus Vaginal delivery is contraindicated (e.g., invasive cervical carcinoma, active genital herpes infection, total placenta previa, vasa previa, cord presentation or prolapse) Uterine or cervical scarring from previous cesarean section or major cervical or uterine (e.g., transfundal) surgery Unengaged fetal head History of hypersensitivity to oxytocin or any ingredient in the formulation
inosine (I, Ino) A naturally occurring, non-canonical nucleoside consisting of a hypoxanthine base with its N9 nitrogen bonded to the C1 carbon of a ribose sugar. Inosine may be incorporated into certain RNA molecules such as the anticodons of some transfer RNAs, and occurs as an intermediate in the breakdown of adenosine to uric acid and in the recycling of adenosine by salvage pathways.
Sources: en.wikipedia.org
It binds to and activates PPAR delta, a nuclear receptor that controls expression of genes related to fatty acid oxidation. This mechanism can alter energy metabolism in animal models. It is not a direct stimulant or fat-burning enzyme.
Early-stage trials examined lipid and glucose markers, but the development program was discontinued. Published human results are limited and do not support approved use for any indication. Claims of performance or health benefits remain unproven.
Yes. Laboratories use LC-MS/MS to detect GW501516 and its metabolites in urine. Detection depends on timing and sensitivity, but the substance is banned at all times.
It targets PPARδ, a nuclear receptor involved in lipid and energy metabolism. It does not act primarily on androgen receptors. This distinction separates it from SARMs.