Description
PrymaLab · Research use only
GW-501516 (Cardarine) (10mg/capsule) 60 Capsules
Cardarine, a selective PPAR-delta agonist dropped by GSK, 10 mg in each of 60 capsules
GW501516, sold as cardarine, is a selective agonist of PPAR-delta, one of the nuclear receptors that sense dietary lipids. It is a small molecule of about 453 Da, not a peptide and not a SARM. This listing is a bottle of 60 hard gelatin capsules, each holding 10 mg in a microcrystalline cellulose fill. GSK developed it as a lipid drug and stopped in 2007 after rodent carcinogenicity findings; the research on it covers cholesterol transport in cells and monkeys and muscle gene expression in mice.
Specifications
| Property | Value |
|---|---|
| Compound | GW-501516 (GW501516 (Cardarine), PPAR-delta agonist) |
| CAS number | 317318-70-0 |
| Molecular formula | C21H18F3NO3S2 |
| Contents | GW-501516: 10 mg per capsule |
| Form | Hard gelatin capsules containing the active substance blended with microcrystalline cellulose, packed in a sealed bottle |
| Storage, sealed | Store at room temperature (15–25 °C) in the tightly closed original container, dry and protected from light |
| Safety data sheet | PL-SDS-076 |
What is in each capsule
Each capsule contains 10 mg of GW501516, about 2.5% of the capsule contents by weight, blended with microcrystalline cellulose inside a gelatin shell, with 60 capsules to a bottle. The safety data sheet classifies GW501516 as suspected of causing cancer (Carc. 2, H351) and asks for the bottle to be stored locked up. The filler and the shell are not classified. Keep the bottle tightly closed in its original container at 15 to 25 °C, dry and protected from light, and handle opened capsules and spills under the laboratory’s rules for suspected carcinogens.
Why development stopped
Glaxo and Ligand Pharmaceuticals began the collaboration that produced GW501516 in 1992, and GSK took the compound into human studies for abnormal blood lipids from 2000. Development stopped in 2007. In 2009 GSK scientists presented rat and mouse carcinogenicity studies of GW501516 as posters at the Society of Toxicology meeting; they were never published as full papers, and they are the reason given for abandoning the compound. The receptor survived as a target. Seladelpar, a different selective PPAR-delta agonist, received accelerated FDA approval in 2024 for a cholestatic liver disease. WADA added PPAR-delta agonists to its Prohibited List in 2009, and the current list names GW501516 among the metabolic modulators, prohibited at all times.
What the research covers
Discovery and the lipid work
GW501516 came out of combinatorial chemistry and structure-based design aimed at the delta subtype, the one PPAR for which no selective ligand then existed; the alpha and gamma subtypes were already the targets of the fibrates and the glitazones1. In macrophages, fibroblasts and intestinal cells it raised expression of the cholesterol transporter ABCA1 and increased cholesterol efflux to apolipoprotein A11. In insulin-resistant, obese middle-aged rhesus monkeys it raised HDL cholesterol and lowered small dense LDL, fasting triglycerides and fasting insulin1. Those results set the course of its development as a lipid drug.
Muscle fibre studies in mice
Wang and colleagues built mice that expressed an activated form of PPAR-delta in skeletal muscle; the animals formed more type I fibres and could run up to twice as far as their littermates2. Treating ordinary mice with a PPAR-delta agonist produced a similar type I gene expression profile, a transcriptional signature and not a measured change in fibre composition2. In 2008 Narkar and colleagues found that a PPAR-delta agonist and exercise training together increased oxidative fibres and running endurance in mice3. The often repeated endurance gain in sedentary, untrained mice in that paper belonged to a different compound, the AMPK activator AICAR3, which is covered in the AICAR (acadesine) guide.
What is not established
The human record is a handful of small, short studies of blood lipids, insulin and liver fat, and none of them tested endurance or performance. Because the carcinogenicity studies were never published in full, the margin between the exposures that caused tumours in rodents and anything in people is unknown. None of this work used capsules. The cardarine (GW501516) guide sets out the human studies, the carcinogenicity record and the legal position in detail.
How each lot is tested
Every lot is tested in PrymaLab’s own laboratory in Ashland, Kentucky before release. Published certificates are listed on the results page and can be checked by number and key on the verify page. These are in-house results from PrymaLab Analytical, not an independent test, and the lab is not accredited to ISO 17025. The third-party testing guarantee on this page still applies: if any independent laboratory finds the wrong compound, or less than the stated purity or amount, the order is refunded and the cost of the test is reimbursed.
Frequently asked questions
Is GW501516 a SARM?
No. It binds PPAR-delta, a nuclear receptor in the family that regulates fatty acid and carbohydrate metabolism, and it has no action at the androgen receptor. It is sold beside SARMs and often listed as one, but its pharmacology, development history and safety record are separate.
Why does the safety data sheet carry a cancer hazard?
It classifies GW501516 as suspected of causing cancer (H351). Its developer stopped work on the compound in 2007, and rodent carcinogenicity studies presented by company scientists in 2009 described the findings behind that decision. The sheet asks for the bottle to be stored locked up.
Did GW501516 increase endurance on its own in the mouse studies?
Not in the 2008 study usually quoted. There the endurance increase came from the agonist combined with exercise training, and the gain in untrained mice belonged to AICAR. The earlier doubling of running distance was in genetically engineered mice, not mice given the drug.
Has GW501516 been tested in people?
Only in a few small, short studies run during its development, which measured blood lipids, insulin and liver fat. It was never approved, and no human study tested endurance. These capsules are for laboratory research only and must not be given to people or animals.
References
- Oliver WR Jr, Shenk JL, Snaith MR, et al. A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport. Proc Natl Acad Sci U S A. 2001;98(9):5306-11. DOI · PubMed
- Wang YX, Zhang CL, Yu RT, et al. Regulation of muscle fiber type and running endurance by PPARdelta. PLoS Biol. 2004;2(10):e294. DOI · PubMed
- Narkar VA, Downes M, Yu RT, et al. AMPK and PPARdelta agonists are exercise mimetics. Cell. 2008;134(3):405-15. DOI · PubMed
Research use only
For laboratory research use only. GW-501516 (Cardarine) (10mg/capsule) 60 Capsules is not a drug, food, cosmetic or dietary supplement, is not approved by the FDA or any comparable authority for human or veterinary use, and must not be given to people or animals. It is sold to qualified researchers and institutions, and the buyer is responsible for lawful handling and disposal.
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