GW501516 (Cardarine): The PPAR-Delta Metabolic Modulator

Active Substance: GW501516 (Also known as Cardarine, Endurobol, or GSK-516)1

Manufacturer: Deus Medical

Pack: 1 Box of 2x 25 Tablets ($10 \text{ mg}$ per Tablet)

Form: Oral

What Is GW501516 (Cardarine)?

GW501516, commonly sold as Cardarine, is a research chemical that is often misclassified as a ²$\text{SARM}$ (Selective Androgen Receptor Modulator).³ It is actually a highly selective agonist of the PPAR-Delta (⁴$\text{PPAR}\delta$) Receptor (Peroxisome Proliferator-Activated Receptor Delta).⁵

Originally developed in the 1990s to treat metabolic disorders like obesity, diabetes, and cardiovascular disease, it gained notoriety in the athletic community for its powerful effects on endurance and fat metabolism.⁶

Core Functions and Performance Effects

GW501516 acts by activating the ⁷$\text{PPAR}\delta$ genes, which play a crucial role in regulating energy homeostasis, particularly in active metabolic tissues like skeletal muscle and the heart.⁸

• Fuel Switching (Fat Loss): ⁹$\text{PPAR}\delta$ activation causes skeletal muscles to switch their fuel preference from glucose to fatty acids.¹⁰ This dramatically increases fatty acid oxidation (fat burning), reducing adiposity and sparing glycogen stores.¹¹

• Enhanced Endurance: By forcing the body to use fat as a primary energy source, Cardarine increases oxidative muscle capacity and endurance exercise capacity.¹² Users report improved stamina and the ability to train for longer periods without fatigue, leading to its inclusion on the ¹³$\text{WADA}$ Prohibited List.¹⁴

• Metabolic Improvement: Preclinical and limited human studies showed it could reverse metabolic abnormalities like dyslipidemia (poor cholesterol) and insulin resistance.

 Usage and Dosage (Controversial)

GW501516 is banned by all major sports bodies, and its clinical development was halted due to severe safety concerns.

• Typical Dose (Limited Research): Limited human studies used doses ranging from ¹⁵$2.5 \text{ mg}$ to ¹⁶$10 \text{ mg}$ per day.¹⁷ Athletes on the black market typically misuse ¹⁸$10 \text{ mg}$ to ¹⁹$20 \text{ mg}$ per day.²⁰

• Administration: Due to its half-life, it is typically taken once per day.

• Storage: Store below $30^\circ\text{C}$. Protect from light. Do not freeze.

 CRITICAL SAFETY WARNING (Cancer Risk)

GW501516 was pulled from human clinical trials in 2007 because extensive animal testing showed that the compound caused cancer to rapidly develop in several organs (including the liver, stomach, testes, and colon) at dosages only a few times higher than the human equivalent dose.²¹

• USADA and WADA Warning: The World Anti-Doping Agency (²²$\text{WADA}$) and the U.S. Anti-Doping Agency (²³$\text{USADA}$) have issued urgent public safety warnings, advising athletes not to use this substance due to the potential health risks.²⁴ The long-term effects in humans are unknown, and therefore, it is not considered safe for human consumption.²⁵

• WADA Classification: It is prohibited under S4.5 Metabolic Modulators on the ²⁶$\text{WADA}$ Prohibited List.²⁷

Frequently Asked Questions (FAQs)

1. Why is GW501516 often mistaken for a SARM?

GW501516 is often incorrectly marketed as a ²⁸$\text{SARM}$ due to the general popularity of the ²⁹$\text{SARM}$ class of research chemicals.³⁰ However, GW501516 is a ³¹$\text{PPAR}\delta$ agonist and does not primarily target the androgen receptor, distinguishing it from true ³²$\text{SARMs}$ like Ostarine (³³$\text{MK}-2866$).³⁴

2. Is Cardarine legal to buy and use?

No. GW501516 is not an approved medication anywhere in the world and has no recognized therapeutic uses.³⁵ It is sold illegally as a "research chemical" (often labeled "not for human use"). It is explicitly prohibited in professional and amateur sports by ³⁶$\text{WADA}$.³⁷

3. What were the specific health risks identified in the animal studies?

The major concern is the rapid induction of cancer in multiple organs, including the liver, stomach, tongue, and testes, observed in long-term rodent studies.³⁸ Although the animals were given high doses, the severity and speed of cancer development led researchers to immediately halt all human clinical trials, deeming further testing unethical.³⁹

4. Does GW501516 require Post Cycle Therapy (PCT)?

No. Because GW501516 is a ⁴⁰$\text{PPAR}\delta$ agonist and not an androgen receptor modulator, it does not suppress the body's natural production of testosterone.⁴¹ Therefore, a traditional $\text{PCT}$ protocol (using Nolvadex or Clomid) is not necessary after using Cardarine, though the compound's general safety risks outweigh this benefit.