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What Is GW 501516 (Cardarine)?

GW 501516, often referred to as GW1516, GSK-516, and Cardarine is a peroxisome proliferator-activated receptor delta invented almost thirty years ago. Initially thought to be a candidate to provide relief for people struggling with metabolic diseases and some cardiovascular diseases, GW 501516 is still just starting to find its way in the world. There are a number of active studies among the more learned medical crowds when it comes to GW 501516 and some of the studies completed have had extremely exciting results. Let’s take a look at the history of GW 501516 and intelligently speculate at what the future may hold.

GW 501516 in the 1990’s

In 1992, GSK and Ligand Pharmaceuticals worked together on a ground-breaking collaboration that led to the discovery of GW 501516. The team consisted of several highly successful and esteemed scientists, including one Leo Sternbach – famous for discovering benzodiazepines back in the late 1960’s. After years of perfecting the GW 501516 solution, scientists were able to publish proof of the works. That’s when the real magic began.

2000 – 2010

After the Y2K crisis came and went, people were able to refocus their abilities on science beyond computers. There was a huge boom in medical research and relatively new solutions like GW 501516 were the focus of studies around the world. Not only were we starting to explore what the potential use cases were, but by 2006 we were making note of what effects the GW 501516 didn’t have, which is arguably just as important.

In 2008, there was a huge breakthrough. A group of researchers representing the Proceedings of the National Academy of Sciences of the United States of America discovered and proved out that not only does GW1516 lead to anti-inflammatory mechanisms, but that the mechanisms also inhibit angiotensin II-accelerated atherosclerosis. Mice saw a 40% increase in vascular expression and decrease in inflammation!

2011 – Present

As if to build on the findings completed by the 2008 team, a group of researchers published in a 2012 BioMed study learned that not only does GW 501516 improve vascular expression, but it also seems to promote liver fibrosis. Improved liver health is key to extended the lifespan of test mice struggling with liver failure. Moreover, after serious liver injury, the repair process can be erratic or even pathetic. The introduction of GW 501516 in test subjects enhanced fibrotic response, leading to an increase in healing rates.

As it turns out, GW 501516 has also been successfully linked to enhanced running endurance in Kunming mice. The study from just a few years ago shows us that mice introduced to GW 501516 doses managed to run much further without needing rest. Increased levels of GW 501516 resulted in a decreased need for rest for each test group.

The Future Looks Bright for GW 501516

It feels like we’ve really only just begun to understand the benefits of GW 501516. The early studies lead us to believe that this and other peptides can possibly be the future corner stone of heart disease and liver failure eradication. More research needs to be done, but one thing is for sure… The early results are promising!

(1) Wolf, and George. “Function of the Nuclear Receptor Peroxisome Proliferator–Activated Receptor Delta in Energy Homeostasis.” OUP Academic, Oxford University Press, 1 Nov. 2003, https://academic.oup.com/nutritionreviews/article-abstract/61/11/387/1933740?redirectedFrom=fulltext

(2) Terada, S, et al. “PPARdelta Activator GW-501516 Has No Acute Effect on Glucose Transport in Skeletal Muscle.” Current Neurology and Neuroscience Reports., U.S. National Library of Medicine, Apr. 2006, www.ncbi.nlm.nih.gov/pubmed/16278250.

(3) Yasunori Takata, Joey Liu, Fen Yin, Alan R. Collins, Christopher J. Lyon, Chih-Hao Lee, Annette R. Atkins, Michael Downes, Grant D. Barish, Ronald M. Evans, Willa A. Hsueh, Rajendra K. Tangirala. “PPARδ-mediated antiinflammatory mechanisms inhibit angiotensin II-accelerated atherosclerosis.” Proceedings of the National Academy of Sciences of the United States of America, U.S. National Library of Medicine, Mar. 18 2008, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC2393800/

(4) Radina Kostadinova, Alexandra Montagner, Erwan Gouranton, Sébastien Fleury, Hervé Guillou, David Dombrowicz, Pierre Desreumaux, Walter Wahli. “GW501516-activated PPARβ/δ promotes liver fibrosis via p38-JNK MAPK-induced hepatic stellate cell proliferation.” BioMed, U.S. National Library of Medicine, Oct. 10, 2012, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3519722/.

(5) Wei Chen, Rong Gao, Xinni Xie, Zhibing Zheng, Haijing Li, Song Li, Fangting Dong, Lili Wang. “A metabolomic study of the PPARδ agonist GW501516 for enhancing running endurance in Kunming mice.” Sci Rep, U.S. National Library of Medicine, May 6 2015, https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4421799/.


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