King Cardarine

Description

King Cardarine, scientifically known as GW501516, is a synthetic peroxisome proliferator-activated receptor delta (PPARδ) agonist. GlaxoSmithKline and Ligand Pharmaceuticals originally developed this compound in the 1990s. Researchers investigated it as a potential treatment for metabolic disorders and cardiovascular diseases. The molecular formula is C21H18F3NO3S2, with a molecular weight of 453.50 g/mol. Despite its initial promise, clinical development halted due to significant safety concerns.

Mechanism of Action and Research Applications

Cardarine functions as a potent and selective agonist of the PPARδ receptor. It displays high affinity (Ki = 1 nM) and potency (EC50 = 1 nM) for PPARδ. Moreover, it has greater than 1,000-fold selectivity over PPARα and PPARγ. The compound binds to PPARδ and recruits the coactivator PGC-1α. Consequently, this upregulates the expression of proteins involved in energy expenditure. In skeletal muscles, cardarine induces strong activation of mitochondrial biogenesis. Therefore, it increases oxidative muscle capacity and enhances endurance exercise capacity. These properties make it valuable for studying metabolic pathways and energy utilization.

Pharmacokinetics and Dosage Considerations

The compound has a half-life of approximately 24 hours in plasma. Researchers typically use doses of 2.5-10 mg daily in research settings. However, no safe or effective dosage has been established for humans. Underground usage reportedly ranges from 10-20 mg daily. Nevertheless, these figures lack scientific validation. The compound is not approved for human consumption by any regulatory agency.

Safety Profile and Carcinogenicity Concerns

Researchers must exercise extreme caution with this compound. GW501516 is associated with a high frequency of carcinogenicity and reproductive toxicity. Animal studies demonstrated rapid induction of cancers in several organs. These include the liver, stomach, tongue, skin, bladder, ovaries, womb, and testes. The Therapeutic Goods Administration lists GW501516 under Schedule 10. This classification denotes substances of such danger to health as to warrant prohibition of sale, supply and use. Consequently, clinical development was discontinued due to an unacceptable risk-benefit profile.

Regulatory Status and Doping Classification

The World Anti-Doping Agency (WADA) added GW501516 to the Prohibited List in 2009. It falls under S4.4.1 Metabolic Modulators. It is prohibited at all times and is a non-Specified substance. The compound has resulted in numerous athlete doping violations. The FDA has issued warning letters about its illegal marketing as a dietary supplement. Consequently, it remains a controlled research chemical.

Internal and External Resources

For detailed handling and storage instructions, please consult our Product Handling Guide (Internal Link). For comprehensive safety protocols, visit our Research Safety Page (Internal Link). For external reference, the NCATS Inxight Drugs database provides authoritative chemical and pharmacological data (drugs.ncats.io). Sport Integrity Australia offers comprehensive substance education (sportintegrity.gov.au). Additionally, the Wikipedia article on GW501516 (wikipedia.org) provides a comprehensive overview of its properties and history.