PPARδ is one of those subjects where the details matter more than the headlines. This page pulls together the background, the mechanisms, and the practical points readers ask about most.
Last reviewed on 2025-09-23. Where a claim depends on a specific study, the study is described rather than over-claimed.
Safety discussions about cardarine frequently cite rodent carcinogenicity findings reported in the 2000s. In those studies, treated animals developed tumors at multiple sites, leading sponsors to discontinue clinical development. The relevance of these findings to humans has not been resolved, but they are a major reason the compound is not approved. Current literature emphasizes uncertainty about long-term effects and the risks of unregulated use. Regulators and health agencies have not established a safe human exposure level.
Cardarine is a synthetic compound also known as GW501516, GW-501516, and sometimes endurobol. It was developed as a selective agonist of peroxisome proliferator-activated receptor delta, a nuclear receptor involved in fatty acid oxidation and energy metabolism. The compound was studied in preclinical models for metabolic and cardiovascular conditions, but it did not become a marketed human medicine. In regulatory and anti-doping contexts, it is treated as a prohibited substance rather than a licensed medicine.
The pharmacological interest in cardarine centers on PPARδ activation and its downstream effects on lipid handling and mitochondrial function. In animal studies, PPARδ agonists have been associated with changes in exercise endurance and fatty acid utilization, though results vary by model and protocol. Human data remain sparse, and the absence of large controlled trials limits conclusions about efficacy. Researchers often describe the compound as a tool for probing PPARδ biology rather than a proven therapeutic agent.
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.
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.
| Property | Value | Notes |
|---|---|---|
| Common synonyms | GW501516, GW-501516, GW 501516, endurobol | Names vary in research and anti-doping documents. |
| Chemical class | Synthetic PPARδ agonist | Small-molecule nuclear receptor ligand. |
| CAS Registry Number | 317318-70-0 | Identifier commonly associated with GW501516. |
| Appearance | White to off-white powder | Typical for purified research material. |
| Solubility | Low in water; soluble in DMSO and ethanol | Organic solvents are common for laboratory stock solutions. |
==== Distribution ==== Following a 600 mg oral dose, peak plasma concentrations (Cmax) are achieved in approximately 2 hours under fasting conditions and 4 hours under non-fasting conditions. The presence of food alters absorption; the bioavailability of the tablet formulation decreases by 21–23% under moderate to high-fat conditions relative to fasting conditions. Ritonavir is highly bound (98–99%) to human serum proteins, primarily binding to serum albumin and α1-acid glycoprotein over a concentration range of 0.01 to 30 µg/mL. This extensive protein binding attenuates its free antiviral activity in vitro by approximately 20-fold. The drug exhibits a volume of distribution (Vd) of 0.41 ± 0.25 L/kg.
As of July 2024, lisdexamfetamine is the only pharmacotherapy approved by the US Food and Drug Administration (FDA) and the Therapeutic Goods Administration for BED. Evidence indicates that its effectiveness in treating BED may be partially due to a psychopathological overlap with attention deficit hyperactivity disorder, a cognitive-control disorder that also benefits from treatment with lisdexamfetamine. Medical reviews of randomized controlled trials have established that lisdexamfetamine, administered at doses between 50 and 70 mg, is safe and effective for treating BED. These reviews consistently report fewer weekly binge eating episodes. Furthermore, a meta-analytic systematic review included a 12-month study showing the medication was effective for a long period of time. Two reviews have found lisdexamfetamine to be superior to placebo in several secondary outcomes, including persistent binge eating cessation and reductions in obsessive-compulsive binge eating symptoms, body weight, and triglycerides. Lisdexamfetamine is a pharmacologically inert prodrug that confers its therapeutic effects for BED after conversion to its active metabolite, dextroamphetamine, which acts in the central nervous system. Dextroamphetamine increases the availability of dopamine and norepinephrine in the prefrontal cortex, which makes major decision-making for the body. Lisdexamfetamine, like all pharmaceutical amphetamines, possesses direct appetite suppressant effects, which may be therapeutically beneficial for BED and its associated comorbidities.
Activity-based proteomics, or activity-based protein profiling (ABPP) is a chemoproteomic strategy that employs modular probes to directly assess the functional state of enzymes within complex proteomes. Unlike expression-based proteomics, which measures protein abundance, ABPP provides information about catalytic activity, thereby enabling researchers to distinguish between active and inactive forms of enzymes. This functional perspective has proven valuable for identifying drug targets, mapping ligandable sites, and understanding enzyme regulation in physiological and pathological contexts. By covalently modifying active sites, activity-based probes (ABPs) allow selective tagging, enrichment, and isolation of proteins, reducing the complexity of proteomic samples and facilitating downstream analysis. ABPP has been applied across diverse biological systems, including cells, tissues, and whole organisms, and has contributed to advances in biomarker discovery, drug development, and in vivo imaging.
The body of 18-year-old Hannah Lynch, daughter of Mike Lynch, is recovered from the Bayesian, making her the seventh and final victim of the sinking. Storm Lilian brings disruption to much of the UK, with gusts of up to 70 mph in some regions. The Energy Price Cap is set to rise by 10% in October, with the average household price for gas and electricity increasing by £149 per year. A report by the United Nations urges the UK to take measures to curb race hate speech, including by politicians. 24–26 August – Eight people are stabbed during the Notting Hill Carnival, with a total of 334 people being arrested during the event. 24 August Data from the Office for National Statistics shows the number of those aged 16–24 not in employment, education or training rose to 872,000 during the period of April to June 2024. British athletes Helene Raynsford and Gregor Ewan light the Paralympic Flame at Stoke Mandeville, ahead of its journey to Paris for the 2024 Summer Paralympics. 25 August EE, one of the UK's largest mobile phone networks, advises parents not to give primary school age children smartphones after receiving an increase in the number of requests for guidance from parents. A British Reuters employee named as Ryan Evans is confirmed as having been killed in a missile attack on a hotel in Ukraine the previous day. 26 August A major incident is declared as a fire engulfs a block of flats in Dagenham, east London, which had "known" safety issues. More than 100 people are evacuated, with two taken to hospital.
Ectopia lentis Systemic score* ≥ 7 Aortic root Z-score ≥ 2 Points for systemic score: Wrist AND thumb sign=3 (wrist OR thumb sign=1) Pectus carinatum deformity=2 (pectus excavatum or chest asymmetry=1) Hindfoot deformity=2 (plain pes planus=1) Dural ectasia=2 Protrusio acetabuli=2 pneumothorax=2 Reduced upper segment/lower segment ratio AND increased arm/height AND no severe scoliosis=1 Scoliosis or thoracolumbar kyphosis=1 Reduced elbow extension=1 Facial features (3/5)=1 (dolichocephaly, enophthalmos, downslanting palpebral fissures, malar hypoplasia, retrognathia) Skin striae (stretch marks)=1 Myopia > 3 diopters=1 Mitral valve prolapse=1 The thumb sign (Steinberg's sign) is elicited by asking the person to flex the thumb as far as possible and then close the fingers over it. A positive thumb sign is where the entire distal phalanx is visible beyond the ulnar border of the hand, caused by a combination of hypermobility of the thumb as well as a thumb which is longer than usual. The wrist sign (Walker-Murdoch sign) is elicited by asking the person to curl the thumb and fingers of one hand around the other wrist. A positive wrist sign is where the little finger and the thumb overlap, caused by a combination of thin wrists and long fingers.
Sources: en.wikipedia.org
== Sources == This article incorporates text from a free content work. Licensed under CC BY 4.0 (license statement/permission). Text taken from World Food and Agriculture – Statistical Yearbook 2025, Food and Agriculture Organization of the United Nations. This article incorporates text from a free content work. Licensed under CC BY 4.0 (license statement/permission). Text taken from The State of Food Security and Nutrition in the World 2026, Food and Agriculture Organization of the United Nations.
== Clinical effects == Kynurenine protects the eye by absorbing UV light, especially in the UVA region (315–400 nm). Kynurenine is present in the lens and retina as one of multiple tryptophan derivatives produced in the eye, including 3-hydroxykynurenine, that together provide UV protection and aid in enhancing visual acuity. The use of kynurenine as a UV filter is consistent with its photostability and low photosensitization, owing to its efficient relaxation from the UV-induced excited state. The concentration of this UV filter decreases with age, and this loss of free kynurenine and the concomitant formation of relatively more photosensitizing kynurenine derivatives and kynurenine-protein conjugates may contribute to the formation of cataracts. Evidence suggests that increased kynurenine production may precipitate depressive symptoms associated with interferon treatment for hepatitis C. Cognitive deficits in schizophrenia are associated with imbalances in the enzymes that break down kynurenine. Blood levels of kynurenine are reduced in people with bipolar disorder. Kynurenine production is increased in Alzheimer's disease and cardiovascular disease where its metabolites are associated with cognitive deficits and depressive symptoms. Kynurenine is also associated with tics. Myokines regulate its metabolism. Kynurenine has also been identified as one of two compounds that makes up the pigment that gives the goldenrod crab spider its yellow color.
== Neoplasms of uncertain behavior (235–238) == 235 Neoplasm of uncertain behavior of digestive and respiratory systems 236 Neoplasm of uncertain behavior of genitourinary organs 237 Neoplasm of uncertain behavior of endocrine glands and nervous system 237.0 Pituitary gland and craniopharyngeal duct Pituitary adenoma 237.7 Neurofibromatosis 238 Neoplasm of uncertain behavior of other and unspecified sites and tissues 238.4 Polycythemia vera
A myocardial infarction is usually clinically classified as an ST-elevation MI (STEMI) or a non-ST elevation MI (NSTEMI). These are based on ST elevation, a portion of a heartbeat graphically recorded on an ECG. STEMIs make up about 25–40% of myocardial infarctions. A more explicit classification system, based on international consensus in 2026, also exists. This classifies myocardial infarctions into three types:
Sources: en.wikipedia.org
Cardarine is an investigational synthetic compound that acts as a PPARδ agonist. It is also known as GW501516 and has been studied mainly in preclinical research. It is not an approved medicine.
No. Cardarine is not a steroid hormone; it targets the nuclear receptor PPARδ. Its classification in anti-doping rules differs from anabolic steroids, though it remains prohibited in sport.
Early rodent studies reported tumor formation at multiple sites, which raised safety concerns. Sponsors stopped clinical development, and no approved human product exists.
Cardarine targets PPARδ, a nuclear receptor involved in lipid and energy metabolism. It does not bind the androgen receptor in the way SARMs do.