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GW501516 (Cardarine)
20mg/ml x 30ml INFORMATION

Description

Cardarine, also known as GW501516 or Endurobol, is a PPAR (peroxisome proliferator-activated receptor) agonist and ligand-activated transcription factor that binds to receptors in skeletal muscle tissue and body fat and pushes skeletal muscle cells towards preferential lipid utilization and fat burning. It is often wrongly classified as a selective androgen receptor modulator (SARM). As a PPAR, it shares certain commonalities with SARMs but differs from them in a few important ways. GW 501516 does not affect androgen receptors or alter testosterone levels.

 

Cardarine Mechanism of Action

Invented in the early 1990s, Cardarine is also known by a number of alternate names, including GW1516 and GSK-516. It displays high affinity (Ki = 1 nM) and potency for PPARδ with over 1,000-fold selectivity over PPARα and PPARγ [5]. Binding of GW501516 to PPARδ recruits the coactivator PGC-1α. The PPARδ/coactivator complex in turn upregulates the expression of proteins involved in energy expenditure [6]. By activating AMP-activated protein kinase, it is widely believed to provide a broad range of experimental effects, such as:

  • Increases fatty acid oxidation and promotes fat loss

  • Lower LDL cholesterol (“bad cholesterol”)

  • Higher HDL cholesterol (“good cholesterol”)

  • Increases endurance

  • Reduces inflammation

  • Decreases insulin resistance and improves glucose tolerance

 

Data indicates that PPAR activity preserves glucose for use in tissues like the brain while promoting the mobilization of fatty acids for muscular endurance [10]. PPAR has also been observed playing an important role in temperature regulation, inflammation mediation, mitochondrial respiration, keratinocyte differentiation, and skin and muscle repair. Molecular analyses revealed that PPAR regulates the expression of genes associated with contractile proteins, lipid oxidation, and mitochondrial biogenesis [10].

The benefits and side effects of GW501516 however, have not been confirmed by the Food and Drug Administration (FDA) and like other SARMs for sale, it should be used for research purposes only. Due to its tendency to increase endurance and energy, the World Anti Doping Agency (WADA) has banned the use of Cardarine in professional sports and several athletes have tested positive for the drug and dismissed.

 

Studies Including Cardarine

 A number of human and animal studies have been performed that point to the Cardarine’s ability to enhance certain physiological processes related to energy metabolism as well as potential improvements in blood lipids:

  • One study on mice found that GW501516 promotes fatty acid oxidation and fat burning in skeletal muscle tissue and alleviates metabolic syndrome [1]

  • Another study discovered that peroxisome proliferator-activated receptors can markedly increase running endurance in Kunming mice [2].

  • Yet another study on mice revealed that PPARs augment exercise endurance by preventing exhaustion of glucose (“hitting the wall”) [3].

  • A study involving obese rhesus monkeys found that GW 501516 increased high-density lipoprotein (HDL) and lowered very-low-density lipoprotein (VLDL), indicating potential cardioprotective effects from Cardarine [6].

  • Two separate phase II clinical studies in humans found positive effects of Cardarine on obesity, diabetes, dyslipidemia, and cardiovascular disease, as well as suppression in macrophage-derived inflammation [7, 8].

  • A study in rats that were fed a high fructose diet found that GW 501516 reduced inflammation markers, especially in the liver, and increased the expression of genes that regulate beta-oxidation [11]

 

Side Effects of Cardarine

While Cardarine is not known to cause androgenic side effects like anabolic androgenic steroids, data in rats indicates that doses of 3mg/kg/day (180-240mg per day in the average 60-80kg adult), significantly higher than those used in human trails, caused cancer to develop quickly in several organs [9]. Anecdotal data online indicates little in the way of noticeable side effects but more research is necessary to determine the overall safety profile of GW501516 before it can be approved for human use.

Cardarine FAQ

Can Cardarine suppress natural testosterone?

  • GW 501516 does not interact with the androgen receptor at all so it does not cause suppression of natural testosterone.

Can women participate in research with Cardarine?

  • Cardarine is non-hormonal and is not known to interrupt menstrual cycles or cause virilization in female test subjects. Doses as high as 18mg per day have been used in clinical trails for women. Pregnant women or women who may become pregnant should not engage in clinical research with Cardarine.

Does Cardarine improve cholesterol?

  • GW501516 has been shown to increase HDL and decrease LDL in rhesus monkeys.

 

Abuse Warning

Cardarine is an investigational compound still awaiting FDA approval and is not a dietary supplement. At Mass to Brass LLC we are not medical doctors, and our expertise is sourcing and quality control. Where we do not encourage or condone consumer use of SARMs products, they are for research purposes only. Anecdotal reports online indicate Cardarine dosage of 10mg and 20mg per day used by many individuals. A Cardarine dose of 30mg per day has even been reported by several individuals in online forums. These dosages may not match those used in carefully designed medical research protocols and may pose a serious risk of adverse effects in users.

We consider the duplication of anecdotal protocols online to be a risky practice. SARMs should only be used under the supervision and direction of a medical doctor or designated research authority. We strongly discourage the use of SARMs for performance enhancement in sports and bodybuilding, and warn against “bro science” and peer consensus when making decisions about human health.

 

References:

  1. T. Tanaka et al., Activation of peroxisome proliferator-activated receptor δ induces fatty acid β-oxidation in skeletal muscle and attenuates metabolic syndrome, Proc. Natl. Acad. Sci. U.S.A., vol. 100, no. 26, pp. 15924–15929, Dec. 2003 https://pubmed.ncbi.nlm.nih.gov/14676330/

  2. Chen, W. et al. A metabolomic study of the PPARd agonist GW501516 for enhancing running endurance in Kunming mice. Sci. Rep. 5, 09884; doi: 10.1038/srep09884 (2015) https://www.nature.com/articles/srep09884

  3. Fan W., Waizenegger W., Lin C.S., Sorrentino V., He M.-X., Wall C.E., Li H., Liddle C., Yu R.T., Atkins A.R., et al. PPARδ Promotes Running Endurance by Preserving Glucose. Cell Metab. 2017;25:1186–1193.e1184. doi: 10.1016/j.cmet.2017.04.006 https://www.ncbi.nlm.nih.gov/pmc/articles/PMC5492977/

  4. https://sportstechnologylabs.com/gw501516/

  5. Oliver WR Jr, Shenk JL, Snaith MR, Russell CS, Plunket KD, Bodkin NL, Lewis MC, Winegar DA, Sznaidman ML, Lambert MH, Xu HE, Sternbach DD, Kliewer SA, Hansen BC, Willson TM. A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport. Proc Natl Acad Sci U S A. 2001 Apr 24;98(9):5306-11. doi: 10.1073/pnas.091021198. Epub 2001 Apr 17. PMID: 11309497; PMCID: PMC33205.

  6. Sprecher DL. Lipids, lipoproteins, and peroxisome proliferator activated receptor-delta. Am J Cardiol. 2007 Dec 3;100(11 A):n20-4. doi: 10.1016/j.amjcard.2007.08.009. PMID: 18047848.

  7. Barish GD, Narkar VA, Evans RM. PPAR delta: a dagger in the heart of the metabolic syndrome. J Clin Invest. 2006 Mar;116(3):590-7. doi: 10.1172/JCI27955. PMID: 16511591; PMCID: PMC1386117.

  8. Dressel U, Allen TL, Pippal JB, Rohde PR, Lau P, Muscat GE. The peroxisome proliferator-activated receptor beta/delta agonist, GW501516, regulates the expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells. Mol Endocrinol. 2003 Dec;17(12):2477-93. doi: 10.1210/me.2003-0151. Epub 2003 Oct 2. PMID: 14525954.

  9. Sahebkar A, Chew GT, Watts GF. New peroxisome proliferator-activated receptor agonists: potential treatments for atherogenic dyslipidemia and non-alcoholic fatty liver disease. Expert Opin Pharmacother. 2014 Mar;15(4):493-503. doi: 10.1517/14656566.2014.876992. Epub 2014 Jan 16. PMID: 24428677.

  10. Teresa Coll, David Álvarez-Guardia, Emma Barroso, Anna Maria Gómez-Foix, Xavier Palomer, Juan C. Laguna, Manuel Vázquez-Carrera, Activation of Peroxisome Proliferator-Activated Receptor-δ by GW501516 Prevents Fatty Acid-Induced Nuclear Factor-κB Activation and Insulin Resistance in Skeletal Muscle Cells, Endocrinology, Volume 151, Issue 4, 1 April 2010, Pages 1560–1569, https://doi.org/10.1210/en.2009-1211

  11. Magliano, D.C., Penna-de-Carvalho, A., Vazquez-Carrera, M. et al. Short-term administration of GW501516 improves inflammatory state in white adipose tissue and liver damage in high-fructose-fed mice through modulation of the renin-angiotensin system. Endocrine 50, 355–367 (2015). https://doi.org/10.1007/s12020-015-0590-1

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