GW-50186(Cardarine) 100x10mg

                                               NOT FOR HUMAN CONSUMPTIO

Cardarine (GW501516), also known as Endurobol, is a selective agonist of the Peroxisome Proliferator-Activated Receptor delta (PPARδ). Developed in the 1990s by GlaxoSmithKline and Ligand Pharmaceuticals, GW501516 was initially explored for metabolic and cardiovascular conditions, obesity, diabetes, and dyslipidemia. However, clinical development halted due to preclinical safety concerns. Despite this, GW501516 has gained popularity among athletes and bodybuilders illicitly due to its purported endurance-enhancing and fat-loss properties.

Chemical and Biological Properties

• Chemical Name: GW501516

• Drug Class: PPARδ (PPAR-beta) selective agonist

• Administration Route: Oral (capsule/liquid)

• Half-life: Approximately 16–24 hours

• Primary Target: PPARδ nuclear receptor, regulating lipid metabolism, energy homeostasis, and inflammation.

Mechanism of Action

Cardarine acts primarily by activating PPARδ receptors, influencing several physiological processes:

1. Enhanced Lipid Metabolism and Fat Oxidation

• Increases fatty acid oxidation, enhancing metabolism, energy utilization, and reducing adiposity.

2. Improved Endurance and Physical Performance

• Promotes the conversion of muscle fibers toward oxidative, slow-twitch (Type-I) fibers, dramatically enhancing aerobic capacity and endurance.

• Increases mitochondrial biogenesis, boosting energy production efficiency.

3. Cardiovascular Protection and Anti-inflammatory Effects

• Improves cholesterol profile: lowers LDL, triglycerides; raises HDL cholesterol.

• Exhibits anti-inflammatory properties beneficial to cardiovascular and metabolic health.

4. Metabolic and Insulin Sensitivity Improvements

• Enhances insulin sensitivity and glucose metabolism, potentially benefiting metabolic disorders.

Therapeutic and Experimental Applications

GW501516 showed significant therapeutic promise in preclinical studies before discontinuation:

Potential Clinical Uses (Investigational)

• Metabolic Disorders: Obesity, Type-2 diabetes, metabolic syndrome.

• Cardiovascular Diseases: Dyslipidemia, atherosclerosis, peripheral artery disease.

• Inflammatory Conditions: Chronic systemic inflammation, autoimmune diseases.

Performance Enhancement (Illicit/Athletic Context)

• Illicitly used for endurance sports, bodybuilding, enhancing cardiovascular performance, reducing fat mass, and improving physique definition.

Dosage and Administration (Experimental Context)

GW501516 is not medically approved, and thus no official clinical dosing exists. Common experimental dosages based on anecdotal use are:

Note: Dosages reflect illicit practices and are not medically endorsed or validated.

Safety Profile and Side Effects

Although initially promising, GW501516 raised serious safety concerns in animal studies, limiting human clinical exploration.

Common Side Effects (Anecdotal Reports)

• Mild gastrointestinal discomfort

• Occasional headaches

• Mild fatigue

Serious Concerns and Toxicity

• Carcinogenic Potential: Animal studies at high doses indicated a significantly increased risk of tumor development (notably liver, colon, stomach, bladder tumors in rodents).

• The carcinogenicity concerns resulted in the cessation of clinical development and explicit safety warnings issued by regulatory bodies.

Contraindications and Precautions

• Absolute Contraindications:

  • Known malignancy or history of cancer (due to carcinogenic risk).

  • Pregnancy and breastfeeding.

• Precautions:

  • Individuals with pre-existing cardiovascular, liver, or gastrointestinal conditions due to unknown long-term safety.

  • Long-term effects and safety at therapeutic human doses remain unestablished.

Legal and Regulatory Status

• Approval Status:

  • GW501516 is not approved by the FDA or any major regulatory agency worldwide.

• Availability:

  • Primarily marketed as a "research chemical" explicitly labeled "not for human consumption."

• Sports Regulations:

  • Explicitly prohibited by World Anti-Doping Agency (WADA) due to potent performance-enhancing and health-risk concerns.

Current Research Status and Evidence

• Preclinical Studies: Extensive animal research confirmed GW501516’s potent metabolic, cardiovascular, and endurance-enhancing properties, alongside serious carcinogenic risks at very high doses.

• Clinical Trials:

  • Early clinical studies in humans demonstrated beneficial metabolic effects, improved lipid profiles, and increased insulin sensitivity.

  • No recent clinical studies due to safety concerns. Human data are limited primarily to small-scale and anecdotal reports.

Summary of Potential Benefits and Risks

Future Directions and Research Needs

• Further human studies unlikely due to carcinogenic concerns; however, safer analogs or modified dosing regimens could be potential future avenues.

• Development of alternative PPARδ agonists with improved safety profiles and retained therapeutic benefits.

• Research into precise molecular mechanisms underlying carcinogenesis associated with GW501516 to understand if risks are dose-dependent or unavoidable.

Conclusion

Cardarine (GW501516) is a powerful experimental PPARδ agonist demonstrating significant preclinical promise in metabolism, cardiovascular health, and endurance performance. However, severe safety concerns identified in animal models, specifically carcinogenic potential, halted clinical development and raised regulatory warnings. Currently banned by anti-doping agencies and explicitly not approved for human use, GW501516 remains an illicit experimental compound associated with substantial health risks. Research continues into safer PPARδ modulation strategies, but GW501516 itself carries serious safety and legal risks.

References and Further Reading

• Narkar, V.A., et al. (2008). "AMPK and PPARδ agonists are exercise mimetics." Cell, 134(3), 405–415.

• Geiger, L.E., & Dunsmore, K.E. (2021). "Potential therapeutic role of PPARδ agonists." Frontiers in Endocrinology, 12, 635858.

• Billin, A.N. (2008). "PPARβ/δ agonists for type 2 diabetes and obesity treatment." Current Opinion in Investigational Drugs, 9(10), 1010–1019.