Cardarine (GW 501516)
What is Cardarine (GW 501516)?
Cardarine (GW-501516) is a selective PPARδ (peroxisome proliferator-activated receptor delta) agonist that fundamentally alters cellular metabolism by switching fuel preference from glucose to fatty acids. Originally developed by GlaxoSmithKline for treating metabolic syndrome and cardiovascular disease, it activates the PPARδ pathway which regulates genes involved in energy expenditure, lipid metabolism, and inflammation. Clinical studies demonstrated remarkable improvements in lipid markers: HDL cholesterol increased by 17%, LDL decreased, and triglycerides dropped significantly—all at very low doses (2.5-10mg daily). Cardarine enhances mitochondrial function, promotes fat oxidation, and improves insulin sensitivity without affecting blood sugar levels. It increases the expression of genes involved in fatty acid transport and oxidation, effectively making the body more efficient at burning fat for fuel. Unlike stimulants, it improves endurance through metabolic efficiency rather than CNS activation. IMPORTANT CONTEXT: Development was halted in 2007 after rodent studies showed cancer development, but this occurred at extremely high doses (equivalent to 40-200mg daily in humans for 2+ years) in rats specifically bred to develop cancer. Human clinical trials at therapeutic doses (2.5-10mg for 2-12 weeks) showed no safety signals. The cardiovascular and metabolic benefits at low doses are well-documented, making it valuable for lipid optimization and metabolic health when used responsibly.
Benefits
- Dramatic Improvement in Lipid Profile (↑HDL 17%, ↓LDL, ↓Triglycerides)
- Enhanced Endurance and Aerobic Capacity (↑VO2 Max)
- Potent Fat Oxidation and Metabolic Switching
- Improved Insulin Sensitivity and Glucose Metabolism
- Cardiovascular Protection and Reduced Inflammation
- Increased Fatty Acid Oxidation Without Stimulants
- Enhanced Mitochondrial Biogenesis
- Reduced Liver Fat and NAFLD Markers
Typical Dosage
- Low-dose (cardiovascular/lipid benefits): 2.5-5mg daily
- Standard: 10mg daily
- Performance: 10-20mg daily (higher risk)
- 8-12 week cycles maximum
- Take 30-45 minutes before training
Side Effects
- Excellent safety profile at low doses (2.5-10mg)
- Potential headaches (rare, usually first week)
- Mild muscle cramps (stay hydrated)
- Insomnia if taken late in day
- Theoretical cancer risk (based on extreme-dose animal studies)
- Banned by WADA for competitive athletes
Dosage Protocol
For lipid and cardiovascular benefits, use conservative dosing: Start at 2.5mg daily for 2 weeks to assess tolerance. May increase to 5-10mg daily maximum. Clinical studies showing lipid improvements used 2.5-10mg for 2-12 weeks. Split dose if using 20mg (10mg morning, 10mg afternoon). Always cycle: 8-12 weeks maximum, followed by equal time off. Monitor lipid panels every 4-6 weeks. Best taken on empty stomach or with fats (not carbs). For pure metabolic benefits, 2.5-5mg is sufficient and minimizes any theoretical risks.
Reconstitution
Dosing Schedule
Negative Interactions
- Carbohydrates immediately pre-dose (reduces effectiveness)
- Alcohol (impairs PPARδ activation)
- Other PPARδ agonists (redundant mechanism)
- Cancer history (theoretical risk)
- Long-term continuous use (cycle properly)
Cancer Risk Context: The 2007 cancer findings occurred in rats given doses equivalent to 40-200mg daily in humans for 2+ years, using rats genetically predisposed to cancer. Human clinical trials at 2.5-10mg for 2-12 weeks showed no safety concerns and significant cardiovascular benefits. Conservative dosing (2.5-10mg for 8-12 weeks) appears to offer an excellent risk/benefit profile for metabolic and cardiovascular health. NOT FDA approved and banned by WADA. Use at own discretion, preferably under medical supervision with regular bloodwork.