GW-501516 (Cardarine)

Description

What is Cardarine?

GW501516, commonly known as Cardarine, is a small-molecule compound that functions as a high-affinity agonist of the peroxisome proliferator-activated receptor delta (PPAR-δ). Unlike selective androgen receptor modulators (SARMs), GW501516 does not interact with androgen receptors and is therefore classified as a PPAR-δ agonist rather than a SARM. It has been extensively studied in investigating energy metabolism, lipid utilization, skeletal muscle physiology, and metabolic regulation.

Activation of PPAR-δ influences the transcription of genes involved in fatty acid transport, mitochondrial metabolism, oxidative energy production, and glucose homeostasis. Through modulation of these pathways, GW501516 has been investigated for its potential effects on endurance-related physiology, substrate utilization, and metabolic adaptation during prolonged exercise. The precise contribution of individual downstream pathways continues to be investigated.

GW501516 remains an important research compound for studying nuclear receptor biology, mitochondrial metabolism, lipid oxidation, and skeletal muscle adaptation. It is also prohibited in competitive sport by major anti-doping organizations due to its potential performance-enhancing properties.

Product Specifications

• Compound / Peptide name: GW501516 (Cardarine)
• Classification: PPAR-δ agonist (non-hormonal small molecule)
• Sequence (if applicable): Not applicable
• Molecular Formula: C21H18F3NO3S2
• Form: Tablet
• Strength: 10 mg per tablet
• Purity: 98%
• Appearance: Tablet form; physical characteristics depend on formulation
• Storage: Store in a cool, dry place away from direct sunlight; keep container tightly sealed
• Solubility: Research-dependent
• Regulatory Status: Investigational research compound; not approved for human therapeutic use

What Is It Used For and Its Purpose 

GW501516 is primarily used as a research compound to investigate PPAR-δ signaling and its role in metabolic physiology. Scientists employ this compound to study mechanisms involved in lipid metabolism, mitochondrial function, glucose utilization, and skeletal muscle energy production. Research has explored how activation of PPAR-δ influences fatty acid oxidation, oxidative muscle fiber metabolism, endurance adaptation, and regulation of genes associated with cellular energy homeostasis.

These investigations provide insights into nuclear receptor signaling and metabolic regulation rather than established therapeutic applications. Researchers also study GW501516 to better understand interactions between lipid metabolism, mitochondrial biogenesis, cardiovascular physiology, and exercise-associated metabolic adaptation.

Research Application

• Metabolism research
• Endocrinology
• Mitochondrial function
• Lipid metabolism
• Glucose metabolism
• Nuclear receptor signaling
• Cardiovascular physiology
• Skeletal muscle physiology
• Exercise metabolism
• Energy homeostasis

Potential Scientific Benefits 

Studies have demonstrated that GW501516 activates PPAR-δ, resulting in altered expression of genes involved in fatty acid transport, β-oxidation, mitochondrial metabolism, and oxidative energy production. These biological effects have been investigated extensively in cell culture systems and animal models. Studies have reported increased fatty acid oxidation, improved oxidative capacity of skeletal muscle, and enhanced endurance performance in experimental animals. These findings are believed to result from increased expression of metabolic enzymes and enhanced mitochondrial function following activation of PPAR-δ-responsive transcriptional pathways.

Laboratory investigations have also explored the effects of GW501516 on lipid metabolism, glucose utilization, and inflammatory signaling. Experimental evidence suggests that PPAR-δ activation may influence lipid homeostasis and insulin sensitivity in certain models.

Observed biological activities in research

• Activation of PPAR-δ-mediated transcription
• Increased fatty acid oxidation in experimental models
• Investigation of mitochondrial metabolic pathways
• Modulation of lipid metabolism
• Effects on glucose utilization and metabolic flexibility
• Investigation of endurance-related physiological adaptation

Molecular mechanisms reported

• PPAR-δ agonism
• Regulation of genes involved in β-oxidation
• Modulation of mitochondrial oxidative metabolism
• Activation of lipid transport and energy metabolism pathways

Physiological pathways involved

• Fatty acid metabolism
• Mitochondrial energy production
• Skeletal muscle oxidative metabolism
• Lipid homeostasis
• Glucose metabolic regulation

Experimental outcomes in models

• Increased endurance capacity in animal studies
• Enhanced oxidative muscle metabolism
• Altered lipid utilization
• Changes in metabolic gene expression

Current evidence remains limited, and further well-controlled clinical studies are required to establish long-term efficacy and safety in humans.

Research Data Sheet 

• Compound / Peptide name: GW501516 (Cardarine)
• Sequence (if applicable): Not applicable
• Classification: PPAR-δ agonist
• Molecular Formula: C21H18F3NO3S2
• Form: Tablet
• Appearance: Tablet form
• Purity: 99%
• Solubility: Research-dependent
• Storage: Store in a cool, dry place away from direct sunlight; keep container tightly sealed
• Research Categories: Metabolism, mitochondrial function, lipid metabolism, cardiovascular physiology, exercise physiology, nuclear receptor signaling

Safety Precautions 

GW501516 is supplied exclusively for laboratory research and should only be handled by qualified personnel following established laboratory safety protocols. Appropriate laboratory handling, documentation, storage, and disposal procedures should be followed at all times.

• Research use only
• Not for human consumption
• Not intended to diagnose, treat, or prevent disease
• Wear appropriate personal protective equipment, including gloves, laboratory coat, and eye protection
• Follow aseptic laboratory handling procedures where appropriate
• Store under recommended storage conditions
• Avoid unnecessary freeze–thaw cycles where applicable
• Maintain accurate labeling and documentation
• Dispose of waste according to institutional and regulatory laboratory requirements
• Limited human safety data available
• Potential unknown long-term biological effects

Conclusion 

GW501516 (Cardarine) is an investigational PPAR-δ agonist that has contributed significantly to research examining energy metabolism, lipid oxidation, mitochondrial biology, and skeletal muscle physiology. Its mechanism of action differs fundamentally from androgen receptor modulators by targeting nuclear receptors involved in metabolic gene regulation rather than hormonal signaling.

GW501516 continues to serve as a valuable research tool for studying nuclear receptor pharmacology, metabolic adaptation, and cellular energy regulation. Ongoing investigations may further clarify the complex role of PPAR-δ signaling in physiology and disease biology.