Exploring the Molecular Structure of Cardarine

Exploring the Molecular Structure of Cardarine
Table of Contents

Recent studies have shown long-term and unsupervised anabolic androgenic steroids presented issues with cardiac health, hypogonadism, and hepatoxicity. Researchers are now studying a new solution: SARMs. Cardarine, also known as GW 501516, – a common SARM – is popular amongst researchers but is not regulated or approved by the FDA for human consumption [6]. 

Research indicates it is an ideal candidate because it could hold the key to a broader range of benefits beyond fat burning and skeletal muscle tissue building for patients with debilitating conditions [6,7]. Clinical research on GW 501516 is ongoing and more research must be conducted to expand on these findings.

Luckily, we have put together a complete guide on what cardarine GW 501516 is, what the research shows, where to buy cardarine, and how to get started with future research today. Keep reading for more information and where to buy cardarine for your research institution!

What Are SARMs?

SARMs are selective androgen receptor modulators. They are non-steroidal experimental compounds that have been in circulation for the last few decades [8,9].

Currently, they are not FDA-approved for human use and are not dietary supplements. However, there are several ongoing clinical trials and studies utilizing GW 501516. 

Several common SARMs include:

  • Ostarine

  • Andarine

  • YK-11

  • S23

  • S4

  • Ligandrol

  • RAD-140

You may see their generic names or a series of letters and numbers. For example, Cardarine is often referred to as GW 501516. Active SARMs research is targeting more than just muscle growth. Studies look at SARMs results in breast cancer, prostate cancer, stress urinary incontinence, and sarcopenia [11]. 

Cardarine Molecular Makeup

Cardarine is categorized along with SARMs and is also known as GW501516. It is a synthetic compound, or research chemical, and falls under a classification of chemiclas known as peroxisome proliferator-activated receptor (PPAR) agonists [8]. 

Most of these PPARs are located in skeletal muscle cells. PPAR agonists are thought to improve energy expenditure and metabolism within these cells [8].

Its molecular formula is C21H18F3NO3S2, and it has a molecular weight of 453.2. Cardarine’s mechanism of action is it regulates fatty acid oxidation  [6].

Cardarine targets cells in skeletal muscle and adipose tissue while targeting metabolic adaptations found in common metabolic diseases. Main clinical investigations include obesity, lipid disorders, and cardiovascular disease as GW 501516 lipid catabolism as seen in animal studies [5,6,8].

The Science Behind Cardarine

Much of the early research targeted cardarine within animals.

Cardarine research has shown the following effects in rodents [6,12]:

  • Less fat storage

  • Decreased obesity incidence

  • Improved blood glucose (with gestational diabetes)

  • Less damage to islet cells

  • Improved diabetic wound healing  with better glucose tolerance

Based on the research above, some experts speculate that cardarine’s role as a PPAR agonist can help simulate exercise and weight loss. Although, this is not widely accepted because of minimal human research involvement as it is not currently FDA approved and for laboratory research purposes only [6,12].

Since cardarine is a PPAR agonist, it could also play a critical role in cancer research. Studies have found that this agonist is closely tied to [5,6,12]:

  • Cancer prevention (e.g., breast, lung, pancreatic)

  • Lipid regulation such as improving HDL cholesterol [6]

  • eNOS activation

  • Improved immunity

  • Inflammation control 

Cardarine in Research

In recent studies, 13 subjects participated in controlled cardarine trials [6].

They all presented with poor cholesterol levels and increased visceral fat. A test group given GW 501516 showed improvements with  [6]:

  • Triglycerides

  • Fatty acids

  • VLDL proteins

Most mammalian research on cardarine has ranged daily. The dangers of fluctuations are a heightened risk of cancer and poor fetal development [6]. 

GW501516 Early Clinical Trialing

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 [2]. Studies in rhesus monkeys showed that cardarine increased HDL and reduced LDL indicating its potential for cardiovascular improvement [3]. 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 [4].

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 [1].

In animal studies, they investigated the important role of PPARD in pancreatic intraepithelial neoplasia lesions (PanINs) and its impact on pancreatic tumorigenesis in mice [1]. 

Their findings revealed that PPAR is upregulated in PanINs at early stages of pancreatic tumorigenesis in mutant Kras mice. Furthermore, transgenic overexpression of PPARD in pancreatic epithelial cells significantly accelerated the development and progression of pancreatic ductal adenocarcinoma in mutant Kras mice [1]. 

This occurred 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 [1].  

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 [1]. 

It is to note 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.

Cardarine Side Effects

With ongoing trials and future research, side effects can be better mitigated and managed. A case study looked at a subject who combined cardarine and ostarine.

The subject’s goal was to increase muscle mass. Upon examination in the emergency department, the subject showed [4,9]:

  • Rhabdomyolysis 

  • Liver cytolysis

While Ostarine is known to be anabolic to muscle tissue, it may damage the liver and the researchers suspect that the combination still poses a risk. This warrants future research on organ injuries when studied in combination. It is worthwhile to note, this report only includes one test subject, a sample size too small to establish causation of effects [4,9].

Current Cardarine Studies and Trials

In the U.S. National Library of Medicine, there are four clinical trials found under GW 501516 (cardarine). Three have been completed, and one was terminated. The conducted trials examined cardarine’s role in [7]:

  • Low level of high-density lipoprotein cholesterol [7]

  • Body fat and inflammation [7]

  • Lipoprotein transport in metabolic syndromes [7]

Cardarine’s function in lowering high-density lipoprotein cholesterol was completed in 2017, and no results were posted. This was a phase II clinical trial that looked at tolerability and effects. Subjects received different amounts daily [8].

One of the more recent examinations on cardarine’s effects was released in 2017. The researchers broke up cardarine’s benefits into two main regions [9]:

  • Peripheral

  • Neurological

The peripheral benefits showed muscular endurance increased by 50% to 70%, and weight gain was reduced by approximately 50 percent [9]. In mice studies, they also discovered that 3 mg/kg reduced inflammatory markers [10]. 

Neurologically, mice studies showed positive neurological outcomes regarding neuronal protection and reduced ischemia-induced brain damage [5]. 

Where to Buy SARMs

More SARMs results are needed to see the effects of cardarine in research. Quality research must rely on purchasing SARMs through reliable manufacturers.

Fake SARMs and mislabeling is abound the internet. Here are some tips for finding high-quality SARMs and where to buy cardarine for your research:

  • Check for third-party testing
  • Check for reliable and refundable payment methods
  • Check for diverse product lines
  • Check for a professional website
  • Avoid shopping for the lowest prices
  • Check FDA disclaimers

Manufacturers and companies cannot promote SARMs as FDA-approved. At this time, SARMs like GW 501516 are only approved for research purposes and are not for human consumption.

Your Ultimate SARMs Guide

Before diving into research, it helps to better understand cardarine’s molecular makeup.

Current research shows that it rides a fine line between cancer prevention and cancer-causing agents. Its versatility also makes it a worthwhile research project for learning how cardarine effects glucose uptake and its effects on a high fat diet [6,9].

If you have an interest in conducting a project on cardarine, contact Sports Technology Labs today and we can help discuss your SARMs needs! We guarantee to offer great customer service for all of your trialing needs.

Scientific References:

1. Oliver Jr, W. R., Shenk, J. L., Snaith, M. R., Russell, C. S., Plunket, K. D., Bodkin, N. L., … & Willson, T. M. (2001). A selective peroxisome proliferator-activated receptor δ agonist promotes reverse cholesterol transport. Proceedings of the national academy of sciences98(9), 5306-5311.

2. “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.

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

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

5. 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.

6. Thevis M, Geyer H, Thomas A, Schänzer W (May 2011). “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): 331–6. doi:10.1002/dta.283. PMID 21538997.

7. Guerrieri D, Moon HY, van Praag H. Exercise in a pill: The latest on exercise-mimetics. Brain plasticity (Amsterdam, Netherlands). 2017 Mar 28 [accessed 2022 May 5].

8. GW501516 in subjects who have low level of high-density lipoprotein cholesterol – full text view. Full Text View – ClinicalTrials.gov. 2017 May 30 [accessed 2022 May 5].

9. https://pubmed.ncbi.nlm.nih.gov/?term=gw+501516&filter=simsearch2.ffrft&filter=datesearch.y_5

10. Mitchell, J. A., & Bishop-Bailey, D. PPARß/da potential target in pulmonary hypertension blighted by cancer risk. Pulmonary Circulation.

11. Machek, S. B., Cardaci, T. D., Wilburn, D. T., & Willoughby, D. S. (2020). Considerations, possible contraindications, and potential mechanisms for deleterious effect in recreational and athletic use of selective androgen receptor modulators (SARMs) in lieu of anabolic androgenic steroids: A narrative review. Steroids164, 108753.

12. Hwai, H. (2019). PPAR-δ GW501516.

13. Kintz P, Gheddar L, Paradis C, Chinellato M, Ameline A, Raul J-S, Oliva-Labadie M. Peroxisome proliferator-activated receptor delta agonist (PPAR- δ) and selective androgen receptor modulator (SARM) abuse: Clinical, analytical and biological data in a case involving a poisonous combination of GW1516 (cardarine) and MK2866 (ostarine). Toxics. 2021 Oct 7 [accessed 2022 May 5]. 

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