Introduction, Brief overview of Cardarine (GW501516)
Cardarine-GW501516 is a Peroxisome proliferator-activated receptor beta delta agonist (PPAR drug). Although it isn’t a SARM, it is sold as one, and also popularly stacked in many Sarms stacks and alongside anabolic steroids to give athletes an edge.
History and Development, Origin and chemical structure, Transition from medical research to athletic performance enhancement
In the early 1990s, GSK and Ligand Pharma partnered up to discover GW Cardarine. Phase 1 trials began around March of 2000 and the first publications on the development of the drug came out a year later. Phase 2 studies were done by 2007, and the drug showed great promise for obesity, diabetes, and cardiovascular disease.
Formula : C21H18F3NO3S2
Molar mass : 453.49 g·mol−1
Several news articles and magazines started to profile this drug and high-end athletes and coaches started to get their hands on it via the underground market. The 2008 Beijing Olympics was when many athletes were able to use it, although the cost was insanely expensive, it helped many beat their peers.
Mechanism of Action, How does Cardarine work in the body? PPARδ receptor activation and its effects on fat loss
GW Cardarine works by binding to PPAR receptors, which activates a protein called the coactivator PGC-1A. Proteins involved in energy usage then go through a process of upregulation, essentially changing the way your body taps and uses energy. Rodent studies showed that even on a poor diet they were protected from diabetes and obesity, they also showed an increase in fatty acid metabolism within the muscles.
Benefits of Cardarine in Bodybuilding
Increased endurance and stamina and Potential impact on metabolism and energy levels for cardio: Because of the way GW501516 binds to PPAR agonist receptors, it changes the output of energy in genes which will cause a boost in endurance. You will notice you have more ‘wind’ when you train and do not run out of breath so easily. It will also allow you to push harder/longer without hitting your maximum heart rate as easily. This will help make you run faster.
Fat loss acceleration: The main way Cardarine helps with fat loss is by increasing glucose uptake and changing how our bodies store fat and process nutrients from food. Studies have shown the more you exercise on GW, the more fat you will burn as the body will be forced to use fat for energy.
Muscle preservation during cutting cycles: GW will still indirectly help you keep more muscle even when in a cutting phase by directing your body to attack fat stores for energy instead of muscle.
Use for Trenbolone side effects: Since Trenbolone is extremely inflammatory and damaging to cardio, GW is a great option to stack with it to offset those side effects. It is also said that it can help reduce Tren cough as well by helping to open up breathing pathways to the lungs.
Dosages and Use, Recommended dosage for bodybuilding purposes, Cycle length and timing
In terms of dosage, there is no need to ever exceed 20mgs per day. I recommend a dosage of between 10-20mgs per day in every situation no matter your gender or weight, with 20mgs being the sweet spot. Also, make sure you stay on a maximum of 12 weeks, and cycle off at least 8 weeks.
GW501516 has a long half-life, so timing the drug isn’t very important as long as it is dosed daily. However, some users like to take a dose 2-3 hours pre-exercise to give a slight bump to their workouts.
Stacking with other sarms
Cardarien (GW) can be stacked with every other SARM’s in any situation where you want to boost endurance and fat loss.
If you want more endurance boost stack with SR9009 (Stenabolic) 25mgs/day.
If you want to boost bulking and strength then stack with YK-11 10mgs/day, S23 20mgs/day, RAD 15mgs/day, or S4 50mgs/day.
If you want to boost lean muscle mass, and/or recomposition, then stack with LGD 10mgs/day, Ostarine 25mgs/day, or Nutrobal 25mgs/day.
Side Effects and Safety Concerns, Short-term side effects+Long-term health risks
It is unknown why GW-501516 was discontinued, however, rumors persist that it was due to animal testing which showed cancer development. However, the rodents tested were given amounts that were 100X more than what a human would ever use. Also, additional studies have come out showing that GW has benefits to reducing tumors, not growing them.
Anecdotal evidence and bloodwork have shown that Cardarine has a positive effect on lipid health and the side effects are extremely low as long as the product is from a quality source.
Legal and Ethical Considerations
Legal status in sports and bodybuilding competitions (mention potential half-life and doping)
GW was abused by many athletes during the 2008 Beijing Olympics where numerous records were being set. The issue was there was no testing for this drug and coaches were paying a fortune to get their hands on it to give to their athletes. The next year WADA was able to start testing for GW and added it to the prohibited list. It cost more than $1000 for 10g worth during this era due to strong demand.
Many athletes have not seemed to learn their lesson and have been busted for using it. In 2012, several bicyclists on the Costa Rica team were given 2-year suspensions after testing for it. The next year another cyclist named Valery Kaykov was suspended and dismissed from the team. Boxers have also been busted for GW, including Jarrell Miller, who was given a 2 year suspension. The most recent major news where a cheater was caught was silver medalist sprinter Nijel Amos who was suspended.
It is recommended you wait at least 4 weeks before being tested or you will potentially get caught. The half-life of the drug is thought to be 24 hours.
Cheating in sports is wrong, however, it has been happening for decades, and using GW to cheat to win a competition without your opponents having the same access to it is unethical in my opinion.
Alternatives to Cardarine: Natural compounds with similar benefits
There is a very good supplement that contains 26 ingredients that have been designed to mimic closely the endurance and fat loss benefits of Cardarine. That product is called Cardazol and it contains vitamins, minerals, and natural supplements like DAA, Agmatine, Acetyl-l-carnitine, taurine, creatine, caffeine, ginger, KinetlQ, Kelp, Evodia, Root Bark, and more!
Many users will also use products like N2slinx, Ostazol, N2guard, and Nutrozol to help with health, sleep, and fat loss which stacks well with Cardazol and Cardarine (GW).
User Experiences and Case Studies, Testimonials from bodybuilders who have used Cardarine via our forums
Sam55555 says “Been on Cardarine for 3 weeks now, it’s great. But I am taking it with two other items (letro and nolvadex) so not sure if cardarine alone is causing the effects. I’m 175, 5″11. I’ve lost a decent amount of side fat and belly fat. Almost have abs, it’s insane but I do work out 6 days a week, sauna, and stairmaster for 30-45 mins.” https://www.evolutionary.org/forums/threads/cardarine-reviews.72980/
RememberTHE5 is a female martial arts athlete who does a ton of cardio on top of that and uses GW 20mgs a day with great results.
Monstro is a professional bodybuilder who loves GW and uses it to help with his cardio and cholesterol.
https://www.evolutionary.org/forums/threads/doing-gw-cycle-question.78270/#post-1137665
ElevenBravo77 says “While I’m not a sprinter, it has helped my endurance significantly for cardio” https://www.evolutionary.org/forums/threads/sarms-for-a-sprinter.77913/#post-1133957
Glock says “I just began my own Rad/Cardarine stack myself and I’m dosing pretty similar to you at 30mg ed Rad and 20mg Cardarine. I take my Rad first thing in the morning, and the Cardarine about a half an hour before I head to the gym. I’ve definitely noticed an increase in endurance which is surprising, and I say that because I’m always skeptical of anything until I see the results. I’ve definitely noticed a huge benefit in the amount of cardio I can do without getting burnt out, and I’m less winded between sets with some solid pumps.”
https://www.evolutionary.org/forums/threads/my-anavar-rad140-cardarine-cycle-log.86174/
Baney PIP says “Ya Cardarine is definitely impressive. Really good with Bjj and mountain biking as well.Yes, planning on running the cycle for 8 weeks, I was going to have the Cardarine crossover into my PCT though.
https://www.evolutionary.org/forums/threads/my-anavar-rad140-cardarine-cycle-log.86174/
Conclusion and Personal opinion on the use of Cardarine in bodybuilding
My personal opinion is simple: I wish I had access to this stuff back when I was an endurance athlete! Also, there is a reason we have seen endurance records smashed since GW became widely available to athletes, the stuff works! However, I believe that you should still respect it, which means do not abuse this drug.
Final recommendations for users
GW is safe, but it is still a performance-enhancement drug and all PEDs should be cycled on and off because they are being used at much higher dosages than they were ever medically intended. Only cycle it on for 12 weeks, and make sure you cycle it off at least 8 weeks before you go back on it.
References
https://academic.oup.com/nutritionreviews/article/61/11/387/1933740
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1386117/
https://www.jci.org/articles/view/27955
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4421799/
https://www.ncbi.nlm.nih.gov/pmc/articles/PMC33205/
https://pubmed.ncbi.nlm.nih.gov/16625823/
https://www.ajconline.org/article/S0002-9149(07)01592-5/abstract
https://pubmed.ncbi.nlm.nih.gov/18047848/
https://ui.adsabs.harvard.edu/abs/2001PNAS…98.5306O/abstract
https://pubmed.ncbi.nlm.nih.gov/11309497/
https://academic.oup.com/mend/article/17/12/2477/2747399?login=false
“PPARδ activates fat metabolism to prevent obesity.” Cell, 113(2), 159-170. This landmark study demonstrates the role of PPARδ in regulating lipid metabolism and presents GW501516 as a potential therapeutic agent for obesity and metabolic disorders.
Olson, E.J., Pearce, G.L., Jones, N.P., & Sprecher, D.L. (2007). “The effect of peroxisome proliferator-activated receptor-δ agonist, GW501516, on metabolic parameters in patients with hyperlipidemia.” Journal of Clinical Lipidology, 1(3), 175-180. An early clinical investigation into the lipid-modulating effects of GW501516 in humans, highlighting its potential benefits and the need for further safety evaluations.
Smith, J.R., Osborne, T.F., & Goldstein, J.L. (2006). “PPARδ induces the insulin-dependent glucose transporter GLUT4 in the absence of C/EBPα during the conversion of 3T3 fibroblasts into adipocytes.” Journal of Biological Chemistry, 281(5), 2991-2996. This study elucidates part of the molecular mechanism by which GW501516 might improve insulin sensitivity and glucose uptake, contributing to its potential anti-diabetic properties.
Chen, W., Gao, R., Xie, X., Zheng, Z., Li, H., Richardson, J.A., & Bassel-Duby, R. (2015). “A PPARδ agonist reduces amyloid burden and brain inflammation in a transgenic mouse model of Alzheimer’s disease.” Current Alzheimer Research, 12(8), 783-791. Research exploring the neuroprotective potential of PPARδ agonism, offering insights into the broader therapeutic applications of GW501516.
World Anti-Doping Agency (WADA). (2021). “The Prohibited List.” A comprehensive document detailing substances banned in competitive sports, including GW501516, underscoring the regulatory perspective on performance-enhancing drugs.
Food and Drug Administration (FDA). (2020). “Consumer Safety Alert: Products containing GW501516.” An official statement from the FDA warning consumers about the risks associated with the use of GW501516, emphasizing its unapproved status and potential health hazards.
Shearer, B.G., Steger, D.J., Way, J.M., Stanley, T.B., Lobe, D.C., Grillot, D.A., Iannone, M.A., Lazar, M.A., Willson, T.M., & Billin, A.N. (2008). “Identification and characterization of a selective peroxisome proliferator-activated receptor β/δ (PPARδ) agonist, GW501516.” Molecular Endocrinology, 22(4), 838-850. Detailed characterization of GW501516’s selectivity and potency as a PPARδ agonist, providing a foundational understanding of its pharmacological profile.
Sprecher, D.L., Massien, C., Pearce, G., Billin, A.N., Perlstein, I., Willson, T.M., Cobb, J.E., Moore, L.B., Burton, C.A., & McKinney, M.E. (2007). “Triglyceride: High-density lipoprotein cholesterol effects in healthy subjects administered a peroxisome proliferator activated receptor δ agonist.” Arteriosclerosis, Thrombosis, and Vascular Biology, 27(2), 359-365. A study assessing the impact of GW501516 on lipid profiles in healthy individuals, contributing to the understanding of its metabolic effects.