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What is GW501516 (aka Cardarine)?

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What is GW501516

GW501516, also known as Cardarine, is not a SARM but rather a selective PPAR delta pathway and AMP-K modulator developed in a collaboration between Ligand Pharmaceuticals and GlaxoSmithKline for targeting obesity, diabetes, dyslipidemia, cholesterol imbalance, and cardiovascular disease. 

PPAR delta pathway and AMP-K are the same pathways activated during exercise and are involved in energy production and fatty acid metabolism. GW501516 displays high affinity for the PPAR delta receptor with over 1000-fold selectivity over PPARα and PPARγ.

chemical formula of GW501516

Buy GW501516 (Cardarine)

 

GW 501516 – Early Clinical Trials

In 2000 and 2002 respectively, GlaxoSmithKline performed phase I clinical trials and by 2007 GW501516 had completed two phase II clinical studies and other studies related to obesity, diabetes, dyslipidemia, and cardiovascular disease. 

Studies in rhesus monkeys showed that cardarine increased HDL and reduced LDL indicating its potential for cardiovascular improvement. Further work on GW501516 was abandoned after it showed an increase in the rate of replication for cancer cells, a potential risk in the anabolic agents for further research.

Research On Mice

According to Liu and colleagues, the link between pro-obesity high-fat diets and increased incidence of pancreatic cancers is well established, but the underlying molecular mechanisms are not yet fully understood 

In animal studies, they investigated the important role of PPARD in pancreatic intraepithelial neoplasia lesions (PanINs) and its impact on pancreatic tumorigenesis in mice

Their findings revealed that PPAR is upregulated in PanINs at early stages of pancreatic tumorigenesis in mutant Kras mice

Furthermore, transgenic overexpression of PARD in pancreatic epithelial cells significantly accelerated the development and progression of pancreatic ductal adenocarcinoma in mutant Kras mice when activated by feeding the mice with a high-fat diet or a diet containing GW 501516 (50 mg/kg), a selective PPARD agonist

In contrast, pancreatic Ppard genetic deletion significantly suppressed the promotion of pancreatic tumorigenesis by these diets

Overall, the findings highlight the essential role of cardarine GW 501516 in promoting pancreatic tumorigenesis in response to a high-fat diet. Targeted inhibition of PPARD activation may represent a promising interventive strategy for the prevention and treatment of pancreatic cancer

It is noted that the studies above did not test the fatty acid oxidation, fatty acids, free fatty acids, skeletal muscle tissue, genes involved, insulin resistance, amp-activated protein kinase, skeletal muscle cells, or heart health of these mice. Further research is indicated to explore a wide range of areas related to GW 501516.

What Benefits of GW501516 Are Researchers Studying?

1. The effect on endurance for physical activity

2. The effect on insulin sensitivity and reduction of bodyfat

3. The effect on HDL/LDL/Triglycerides

Sports Technology Labs and Research

Buy Cardarine for your research so knowledge can be unlocked regarding this Cardarine sarm. There are many places to buy Cardarine online, but Sports Technology Labs offers the most quality product for research and testing needs. 

Our liquid SARMs come in glass bottles so that plasticizers do not contaminate the results of study. If you have any questions before purchasing this research chemical for testing on clinical trials, please reach out to our great customer service team. 

They will assist you promptly and provide fast shipping on every order of GW 501516 amongst other research chemicals for sale.

AT THIS TIME, CARDARINE / GW501516 IS ONLY APPROVED FOR LABORATORY RESEARCH AND IS NOT SOLD FOR HUMAN CONSUMPTION.

Abuse Warning

Selective Androgen Receptor Modulators are investigational compounds still awaiting FDA approval and are not dietary supplements. 

At Sports Technology Labs we are chemical suppliers, not medical doctors, and our expertise is sourcing and quality control. Sports Technology Labs does not encourage or condone consumer use of SARMs products, they are for research purposes only. 

Anecdotal reports and guides may not match those used in carefully designed medical research protocols and may pose a serious risk of adverse effects in users. 

Individual variables, comorbidities, and polypharmacy can also contribute significantly to the risk of health problems.

Scientific References:

1. Oliver WR, 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 (April 2001). “A selective peroxisome proliferator-activated receptor delta agonist promotes reverse cholesterol transport”. Proc. Natl. Acad. Sci. U.S.A. 98 (9): 5306–11. doi:10.1073/pnas.091021198. PMC 33205. PMID 11309497.

2. “GW501516 Glaxo Welcome phase change I, UK”. R & D Focus Drug News. 20 November 2000.

3. Sprecher DL (December 2007). “Lipids, lipoproteins, and peroxisome proliferator activated receptor-delta”. Am. J. Cardiol. 100 (11 A): n20–4.

4. Geiger LE, Dunsford WS, Lewis DJ, Brennan C, Liu KC, Newsholme SJ (2009). PS 895 – Rat carcinogenicity study with GW501516, a PPAR delta agonist (PDF). 48th Annual Meeting of the Society of Toxicology. Baltimore: Society of Toxicology. p. 105. Archived from the original (PDF) on 2015-05-04.5. Thevis M, Geyer H, Thomas A, Schänzer W (May 2011).

5. “Trafficking of drug candidates relevant for sports drug testing: detection of non-approved therapeutics categorized as anabolic and gene doping agents in products distributed via the Internet”. Drug Test Anal. 3 (5): 331–doi:10.1002/dta.283. PMID 21538997.

6. Shane Stokes: Four riders each handed two year bans for use of GW501516, velonation.com 30 July 2013

7. “European champion Valery Kaykov sacked for failing drug test”. BBC. 2013-04-11. Retrieved 2013-04-11

8. “Miguel Ubeto Aponte provisionally suspended”. UCI. 2013-05-13. Archived from the original on 2013-06-28. Retrieved 2013-05-15

9. Liu, Y., Deguchi, Y., Wei, D., Moussalli, M. J., Li, D., Wang, H., … & Shureiqi, I. (2020). Ppard Is Essential in Acceleration of Pancreatic Ductal Adenocarcinoma Development by High-Fat Diet in Mutant Kras Mice. BioRxiv, 2020-12

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