Cardarine (GW-501516): Scientific Profile
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Cardarine (GW-501516) is a selective agonist of the PPAR-δ receptors investigated for its capacity to metabolically reprogram the cellular energy substrate toward lipid oxidation.
GW-501516, commonly termed Cardarine, is a synthetic ligand that acts as a high-affinity selective agonist of the peroxisome proliferator-activated receptor delta (PPAR-δ). In research settings, this non-steroidal compound has demonstrated the ability to modulate gene expression involved in energy expenditure and lipid homeostasis, facilitating a metabolic transition that favors the use of fatty acids over glucose in skeletal muscle tissue.
Administration in animal models has demonstrated a significant improvement in the oxidative capacity of muscle fibers, promoting mitochondrial biogenesis and the expression of fatty acid transport proteins. These findings suggest considerable academic potential for the study of metabolic disorders and the improvement of physical endurance in test subjects, without altering endogenous hormone levels or possessing androgenic activity.
Additionally, the scientific literature highlights the influence of Cardarine on experimental cardiovascular health, with improvements observed in lipid profiles, with increases in high-density lipoproteins (HDL) and reductions in triglycerides. Its use is strictly limited to in vitro and in vivo scientific research applications to understand the mechanisms of PPAR-δ cell signaling.
Mechanism of action
The compound works by selectively binding to the PPAR-δ receptor, activating the recruitment of the coactivator PGC-1α. This process induces the transcription of genes responsible for the beta-oxidation of fatty acids and lipid transport. Unlike other ligands, GW-501516 promotes the remodeling of fast-twitch muscle fibers toward slow-twitch (Type I) fibers, increasing mitochondrial density and aerobic metabolic efficiency.
Mechanism summary
Action as a PPAR-δ receptor agonist that induces the expression of key genes in lipid oxidation and muscle mitochondrial biogenesis.
Clinical Studies (7)
- Testing for GW501516 (cardarine) in human hair using LC/MS-MS and confirmation by LC/HRMS (Kintz P et al. · Drug testing and analysis · 2020) PMID 32298044.
- PPARdelta activator GW-501516 has no acute effect on glucose transport in skeletal muscle (Terada S et al. · American journal of physiology. Endocrinology and metabolism · 2006) PMID 16278250.
- GW-501516 GlaxoSmithKline/Ligand (Pelton P · Current opinion in investigational drugs (London, England: 2000) · 2006) PMID 16625823.
- Activation of Nuclear Hormone Receptor Peroxisome Proliferator-Activated Receptor-Delta Accelerates Intestinal Adenoma Growth (Gupta, et al. · Nature Medicine · 2004) PMID 14758356.
- The PPARdelta Agonist, GW501516, Promotes Fatty Acid Oxidation but Has No Direct Effect on Glucose Utilisation or Insulin Sensitivity in Rat L6 Skeletal Muscle Cells (Dimopoulos, et al. · FEBS Letters · 2007) PMID 17869249.
- Lipid Effects of Peroxisome Proliferator-Activated Receptor-Delta Agonist GW501516 in Subjects with Low High-Density Lipoprotein Cholesterol: Characteristics of Metabolic Syndrome (Olson, et al. · Arteriosclerosis, Thrombosis, and Vascular Biology · 2012) PMID 22814748.
- Effects of the Peroxisome Proliferator-Activated Receptor (PPAR)-delta Agonist GW501516 on Bone and Muscle in Ovariectomized Rats (Mosti, et al. · Endocrinology · 2014) PMID 24708238.
Warnings
Cardarine (GW-501516) is a research-use-only (RUO) compound; the following warnings and handling considerations apply to its laboratory use:
- Product exclusively for laboratory studies
- Handle with adequate personal protective equipment
- Keep out of reach of untrained personnel
- Presence of neoplasms in research subjects
- Pre-existing hepatic dysfunction in experimental models
- Pregnancy or lactation in animal specimens
Technical data
- CAS
- 317318-70-0
- Molecular formula
- C21H18F3NO3S2
- Molecular weight
- 453.5 Da
- Compound type
- metabolic
- Storage
- 15-30°C ambient, avoid direct light
- Shelf life (lyophilized)
- 24 months
- Shelf life (reconstituted)
- Not applicable (Solid presentation)
- Light-sensitive
- Sí
Available for research
Cardarine (GW-501516) is available as a research reagent (RUO):
Frequently asked questions about Cardarine (GW-501516)
What is Cardarine (GW-501516)?
Cardarine (GW-501516) is a selective agonist of the PPAR-δ receptors investigated for its capacity to metabolically reprogram the cellular energy substrate toward lipid oxidation.
What is the mechanism of action of Cardarine (GW-501516)?
Action as a PPAR-δ receptor agonist that induces the expression of key genes in lipid oxidation and muscle mitochondrial biogenesis.
What is Cardarine (GW-501516) researched for?
In preclinical research, Cardarine (GW-501516) is studied mainly in: Modulation of experimental oxidative metabolism; Research on systemic weight reduction; Stimulation of mitochondrial biogenesis in myocytes. Material exclusively for scientific research.
What are the chemical properties of Cardarine (GW-501516)?
Molecular formula C21H18F3NO3S2; molecular weight 453.5 Da; CAS number 317318-70-0.
How is Cardarine (GW-501516) stored?
Storage conditions: 15-30°C ambient, avoid direct light; lyophilized stability: 24 months; once reconstituted: Not applicable (solid presentation); protect from light.
What routes of administration are studied for Cardarine (GW-501516)?
In the research models the following are described: Oral (Research), Nasogastric tube (Animal models). Use is exclusively for scientific research.