If you have been reading about Metabolite and want a single page that covers the useful parts, this is it: definitions, context, how it is studied, and the questions that come up repeatedly.
Last reviewed on 2025-08-19. Where a claim depends on a specific study, the study is described rather than over-claimed.
Safety concerns emerged from long-term animal studies. In rodents given the compound for extended periods, researchers found an increased incidence of certain cancers, including liver and bladder tumors. These findings contributed to the discontinuation of clinical development. Whether similar risks apply to short-term or low-level exposure in humans is not established, and controlled human safety data are limited. The relevance of high-dose rodent carcinogenicity findings to human use remains a subject of debate.
Human trials of GW501516 were small and short in duration. They examined lipid levels, glucose handling, and other metabolic markers, but the programs were halted after the animal cancer findings. No approved therapeutic product exists, and published human data are insufficient for establishing long-term safety. Reports of use for athletic performance come mainly from non-clinical settings and cannot be verified through controlled trials. Independent testing of products sold as cardarine has found inconsistent purity and labeling.
A common misconception is that cardarine has been proven safe for human use. In reality, human clinical data are limited, and long-term animal studies have raised concerns about cancer. Another misconception is that it is a supplement or vitamin-like compound. It is a synthetic research chemical with no approved medical indication. Scientific discussion often focuses on its mechanism and detection rather than therapeutic use. Regulatory and anti-doping literature treats it primarily as a prohibited substance.
Cardarine is explicitly prohibited by the World Anti-Doping Agency under the class of PPARδ agonists. Its presence in urine or blood samples can be detected using mass spectrometry-based methods, often liquid chromatography-tandem mass spectrometry. Athletes who test positive may face sanctions, including bans from competition. The compound is also regulated as a prescription-only or unapproved drug in many countries. Enforcement varies by jurisdiction, and some regions treat it as a controlled substance. Online sales may occur despite these restrictions, creating quality and legal risks.
Laboratory detection of cardarine typically involves sample preparation followed by chromatographic separation and mass spectrometric identification. Urine is the most common matrix for anti-doping tests, though blood and hair have also been explored. Methods can target the parent compound or its metabolites, depending on the expected window of detection. Reference standards are required for accurate quantification. Matrix effects and dilution can influence results, so laboratories use internal standards and validation protocols. The exact detection window varies with dose, route, and individual metabolism.
| Property | Value | Notes |
|---|---|---|
| Primary target | PPARδ (NR1C2) | Nuclear receptor involved in lipid metabolism |
| Preclinical effect | Increased fatty acid oxidation | Observed in rodent studies |
| Key safety signal | Tumors in rodents after long-term exposure | Contributed to halted clinical development |
| Human trial status | No approved product; development stopped | Limited short-term metabolic data |
| Sport regulatory status | Prohibited at all times | WADA hormone and metabolic modulators class |
Clinical development stopped after rodent studies showed tumors at multiple sites. Whether those findings predict human cancer risk remains an open question, but they led sponsors to discontinue programs. Human safety data are limited to small, short-term studies that were not designed to assess cancer risk. Reported effects in those studies included changes in blood lipids, but the evidence is insufficient for medical use. Long-term consequences of nonmedical use are not well characterized. Questions about dose, duration, and individual susceptibility remain unresolved.
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.
In the fitness and bodybuilding literature, cardarine is frequently discussed as an endurance agent or fat-loss compound, although such claims are not supported by robust clinical evidence. Online descriptions often mix animal data, user anecdotes, and marketing language. Researchers who study PPARδ agonists distinguish between receptor activation in controlled experiments and unsupervised use of unverified products. The latter introduces unknown purity, dose, and interactions, making reported experiences difficult to interpret scientifically.
GW501516 acts as an agonist at peroxisome proliferator-activated receptor delta, a nuclear receptor involved in transcription of genes related to lipid handling and energy use. Activation of PPARδ can shift skeletal muscle toward greater fatty acid oxidation in animal models, which is one reason it drew interest for metabolic disease and exercise research. The exact downstream effects depend on tissue, species, dose, and duration. Human data are sparse, so many proposed benefits remain hypotheses rather than established clinical outcomes.
Laboratory studies have examined GW501516 in cell cultures and rodents for conditions such as dyslipidemia, insulin resistance, and obesity. Some trials in humans were initiated, but development was discontinued after preclinical findings raised concerns about cancer in certain models. Those findings do not prove that the compound causes cancer in people, but they contributed to regulatory caution. Later reviews often describe the evidence as preliminary and insufficient for assessing long-term safety.
=== Assumed correlation between impact factor and quality === The journal impact factor was originally designed by Eugene Garfield as a metric to help librarians make decisions about which journals were worth indexing, as the JIF aggregates the number of citations to articles published in each journal. Since then, the JIF has become associated as a mark of journal "quality", and gained widespread use for evaluation of research and researchers instead, even at the institutional level. It thus has significant impact on steering research practices and behaviors. By 2010, national and international research funding institutions were already starting to point out that numerical indicators such as the JIF should not be considered as a measure of quality. In fact, research was indicating that the JIF is a highly manipulated metric, and the justification for its continued widespread use beyond its original narrow purpose seems due to its simplicity (easily calculable and comparable number), rather than any actual relationship to research quality. Empirical evidence shows that the misuse of the JIF—and journal ranking metrics in general—has a number of negative consequences for the scholarly communication system. These include gaps between the reach of a journal and the quality of its individual papers and insufficient coverage of social sciences and humanities as well as research outputs from across Latin America, Africa, and South-East Asia.
Nonsteroidal antiandrogens are antiandrogens which are nonsteroidal and hence unrelated to steroid hormones in terms of chemical structure. These medications are primarily used in the treatment of prostate cancer, but are also used for other purposes such as the treatment of acne, excessive facial/body hair growth, and high androgen levels in women. Unlike steroidal antiandrogens, nonsteroidal antiandrogens are highly selective for the androgen receptor and act as pure androgen receptor antagonists. Similarly to spironolactone however, they do not lower androgen levels, and instead work exclusively by preventing androgens from activating the androgen receptor. Nonsteroidal antiandrogens are more efficacious androgen receptor antagonists than are steroidal antiandrogens, and for this reason, in conjunction with GnRH modulators, have largely replaced steroidal antiandrogens in the treatment of prostate cancer. The nonsteroidal antiandrogens that have been used in transgender women include the first-generation medications flutamide (Eulexin), nilutamide (Anandron, Nilandron), and bicalutamide (Casodex). Newer and even more efficacious second-generation nonsteroidal antiandrogens like enzalutamide (Xtandi), apalutamide (Erleada), and darolutamide (Nubeqa) also exist, but are very expensive due to generics being unavailable and have not been used in transgender women. Flutamide and nilutamide have relatively high toxicity, including considerable risks of liver damage and lung disease.
== In literature == The literary lich developed from monsters found in earlier classic sword and sorcery fiction, which is filled with powerful sorcerers who use their magic to triumph over death. Many of Clark Ashton Smith's short stories feature powerful wizards whose magic enables them to return from the dead. Several stories by Robert E. Howard, such as the novella Skull-Face (1929) and the short story "Scarlet Tears", feature undying sorcerers who retain a semblance of life through mystical means, their bodies reduced to shriveled husks with which they manage to maintain inhuman mobility and active thought. The term lich, used as an archaic word for corpse (or body), is commonly used in these stories. Ambrose Bierce's tale of possession "The Death of Halpin Frayser" features the word in its introduction, referring to a corpse. H. P. Lovecraft also used the word in "The Thing on the Doorstep" (published 1937) where the narrator refers to the corpse of his friend possessed by a sorcerer. Liches are sometimes depicted using a magical device called a phylactery to anchor their souls to the physical world so that if their body is destroyed they can rise again over and over, as long as the phylactery remains intact. Other imagery surrounding demiliches, in particular that of a jeweled skull, is drawn from the early Fritz Leiber story "Thieves' House". Gary Gygax, one of the co-creators of Dungeons & Dragons, said that he based the description of a lich included in the game on the short story "The Sword of the Sorcerer" (1969) by Gardner Fox.
=== Acidification === Potassium hydrogen sulfate (also known as potassium bisulfate), KHSO4, is readily produced by reacting K2SO4 with sulfuric acid. It forms rhombic pyramids, which melt at 197 °C (387 °F). It dissolves in three parts of water at 0 °C (32 °F). The solution behaves much as if its two congeners, K2SO4 and H2SO4, were present side by side of each other uncombined; an excess of ethanol the precipitates normal sulfate (with little bisulfate) with excess acid remaining. The behavior of the fused dry salt is similar when heated to several hundred degrees; it acts on silicates, titanates, etc., the same way as sulfuric acid that is heated beyond its natural boiling point does. Hence it is frequently used in analytical chemistry as a disintegrating agent. For information about other salts that contain sulfate, see sulfate.
Protein folding must be thermodynamically favorable within a cell in order for it to be a spontaneous reaction. Since it is known that protein folding is a spontaneous reaction, then it must assume a negative Gibbs free energy value. Gibbs free energy in protein folding is directly related to enthalpy and entropy. For a negative delta G to arise and for protein folding to become thermodynamically favorable, then either enthalpy, entropy, or both terms must be favorable.
Sources: en.wikipedia.org
In the United States, it also operates under the Speedway brand (predominantly in the Midwest and on the East Coast) and as Stripes Convenience Stores within the West South Central states. Both Speedway and Stripes operate alongside 7-Eleven's namesake stores in several American markets. 7-Eleven also operates A-Plus locations, licensing the name from its owner, Energy Transfer Partners, a fellow company based in the Dallas–Fort Worth metroplex. However, most of these stores have since been rebranded as standard 7-Eleven stores.
=== Scientific analyses === Cultural considerations can sometimes interfere with the conservation of human remains, particularly when it comes to physical and chemical analyses, which play an important role in their care. Testing conducted on human remains, especially ancient ones, can include DNA testing, isotope analyses, and carbon-14 dating. The benefits of such testing is sometimes outweighed by the cultural or sacred importance of the remains as well as the risk of damaging them too greatly. According to the Deutscher Museumsbund, there are only three circumstances in which scientific research should be conducted on human remains:
Elevated waist circumference (population- and country-specific) Triglycerides ≥150 mg/dL (1.7 mmol/L) Reduced HDL-C (≤40 mg/dL (1.0 mmol/L) men; ≤50 mg/dL (1.3 mmol/L) women) Elevated blood pressure (systolic ≥130 and/or diastolic ≥85 mmHg) Fasting glucose ≥100 mg/dL (5.55 mmol/L) This statement recognises population differences in waist risk thresholds and encourages common criteria with agreed cut points for international comparisons. The prior IDF and revised NCEP definitions are similar, but differ on assumptions when body mass index ≥30 kg/m2 and on geography-specific waist cut points.
The major metabolite of progesterone in the urine is the 3α,5β,20α isomer of pregnanediol glucuronide, which has been found to constitute 15–30% of an injection of progesterone. Other metabolites of progesterone formed by the enzymes in this pathway include 3α-dihydroprogesterone, 3β-dihydroprogesterone, 20α-dihydroprogesterone, and 20β-dihydroprogesterone, as well as various combination products of the enzymes aside from those already mentioned. Progesterone can also first be hydroxylated (see below) and then reduced. Endogenous progesterone is metabolized approximately 50% into 5α-dihydroprogesterone in the corpus luteum, 35% into 3β-dihydroprogesterone in the liver, and 10% into 20α-dihydroprogesterone. Relatively small portions of progesterone are hydroxylated via 17α-hydroxylase (CYP17A1) and 21-hydroxylase (CYP21A2), into 17α-hydroxyprogesterone and 11-deoxycorticosterone (21-hydroxyprogesterone), respectively, and pregnanetriols are formed secondarily to 17α-hydroxylation. Even smaller amounts of progesterone may also be hydroxylated via 11β-hydroxylase (CYP11B1) and, to a lesser extent, via aldosterone synthase (CYP11B2) into 11β-hydroxyprogesterone. In addition, progesterone can be hydroxylated in the liver by other cytochrome P450 enzymes that are not steroid-specific. Catalyzed mainly by CYP3A4, 6β-Hydroxylation is the major transformation and is responsible for approximately 70% of cytochrome P450-mediated progesterone metabolism. Other routes include 6α-, 16α-, and 16β-hydroxylation.
=== DCVJ, rigidity sensitive dyes === 4-(dicyanovinyl)julolidine (DCVJ) is a molecular rotor probe with fluorescence that is strongly dependent on the rigidity of its environment. When protein denatures, DCVJ increases in fluorescence. It has been reported to work with 40 mg/ml of antibody.
Sources: en.wikipedia.org
Rodent studies reported increased endurance and fat oxidation after GW501516 exposure. Long-term studies also found higher rates of some tumors, which led to halted development.
Small short-term human trials examined metabolic markers such as lipids and glucose. The trials did not continue after rodent cancer findings, so long-term human safety is unknown.
Controlled human trials have not established a performance benefit. Anecdotal reports exist, but they are not reliable evidence.
Yes, WADA prohibits cardarine as a PPARδ agonist. It appears on the prohibited list and can be detected in urine or blood. Athletes using it risk sanctions.