Cardarine
Other Names
- GW 501516
- GW-501
- GW1516
- GSK-516
- Endurobol
General
- Cardarine is a synthetic PPAR-delta agonist that was originally developed for potential therapeutic use in metabolic and cardiovascular diseases.[1]
Performance Enhancing Effects
- improves endurance in animal models
- in human studies, cardarine has been shown to reduce plasma triglyceride and increase HDL cholesterol[2]
Medical Indications
- No medical indications
Adverse Effects
- increased risk of cancer in long-term animal studies
- Reduced bone mineral density
- insulin resistance in skeletal muscle [3]
- hepatomegaly and liver injury
- skeletal myopathy
Mechanism
- PPAR delta agonist
- Promotes fatty acid oxidation and promotes muscle remodeling through upregulating palmitoyltransferase 1 (CPT1) and other genes involved in lipid metabolism and increases AMPK phosphorylation[4]
WADA Considerations
- Banned by WADA.
See Also
References
- ↑ Pokrywka A, Cholbinski P, Kaliszewski P, et al. Metabolic Modulators of the Exercise Response: Doping Control Analysis of an Agonist of the Peroxisome Proliferator-Activated Receptor Δ (GW501516) and 5-Aminoimidazole-4-Carboxamide Ribonucleotide (AICAR). J Physiol Pharmacol. 2014;65(4):469–76.
- ↑ Olson EJ, Pearce GL, Jones NP, Sprecher DL. Lipid Effects of Peroxisome Proliferator-Activated Receptor-Δ Agonist GW501516 in Subjects With Low High-Density Lipoprotein Cholesterol: Characteristics of Metabolic Syndrome. Arterioscler Thromb Vasc Biol. 2012;32(9):2289–94. doi:10.1161/ATVBAHA.112.247890
- ↑ Cresser J, Bonen A, Chabowski A, et al. Oral Administration of a PPAR-delta Agonist to Rodents Worsens, Not Improves, Maximal Insulin-Stimulated Glucose Transport in Skeletal Muscle of Different Fibers. Am J Physiol Regul Integr Comp Physiol. 2010;299(2):R470–9. doi:10.1152/ajpregu.00431.2009
- ↑ Krämer DK, Al-Khalili L, Guigas B, et al. Role of AMP Kinase and PPARdelta in the Regulation of Lipid and Glucose Metabolism in Human Skeletal Muscle. J Biol Chem. 2007;282(27):19313–20. doi:10.1074/jbc.M702329200
Created by:
Khashayar ( Khash ) Farzam on 12 July 2019 02:55:13
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Last edited:
10 July 2025 19:06:34
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