GW-501516 (CARDARINE)

Cardarine was developed to increasing lean muscle, improve strength, and prevent muscle wastage.

Qty: 30 tablets

EACH TABLET CONTAINS 20MG OF GW-501516 

Supplied for Research Purposes Only

This information and product is provided for research purposes only. We do not provide any advice on the usage of these products as UK Law prevents this. Customers should check the legality of this product in their own country prior to purchase.

Benefits and uses:

Increased endurance

Improved cardiovascular health

Fat loss

Dose:

20mg per day.

What is GW-501516 (Cardarine)?

GW 50156 is a PPARδ receptor agonist (Peroxisome Proliferator Activated Receptor Delta). In spite of this, it is frequently referred to as a "SARM" because of its comparable anabolic and fat-burning benefits.

Cardarine was only recently developed in 1992, and as a result, it is considered to be a "research molecule." Like SARMs, the effects of cardarine are not yet completely understood, and the FDA has not granted approval for its use. However, due to the fact that early research has shown cardarine to have good benefits on body composition and athletic performance, it has been banned from use in sports. Cardarine has been added to the list of substances that are prohibited to compete with by the World Anti-Doping Agency (WADA). It has been included in the category of 'hormones and metabolic modulators.'

Cardarine's significant fat burning benefits provide initial hope for the medical community, in the treatment of obesity. In the meantime, weightlifters are already using cardarine to maintain muscle mass and improve fat loss during cutting cycles. It has been shown to improve insulin sensitivity, lipid balance, and glucose tolerance, all of which work together to increase lipolysis. Cardarine causes a shift in energy metabolism by increasing fatty acid oxidation while simultaneously decreasing glucose consumption. This means that the body will utilise its fat stores as its major source of energy rather than glucose.

Users see a reduction in both their subcutaneous and visceral fat mass as a result of this, which results in a slimmer and more defined appearance. Its lipolytic effects are comparable to those of other selective androgen receptor modulators (SARMs), such as ostarine. There is some anecdotal evidence that suggests the fat-burning properties of cardarine are significantly more potent than its capacity to create lean muscle tissue.

Because of the favourable effects that cardarine has on insulin and blood glucose, there is a possibility that in the future it could be used as a treatment for type II diabetes.

Hypertrophy of muscle

A phase II study observed an increase in lean mass in users of cardarine by 1.3 kilogrammes (1), following a dosage of 10 milligrammes per day for a period of 12 weeks. This finding provides evidence that cardarine has a simultaneous anabolic effect.

This slight increase in muscularity is comparable to that caused by SARMs, resulting in a beneficial effect, but one that is somewhat weaker than that caused by anabolic steroids.

Muscle Endurance

The remodelling of muscle tissue that takes place as a result of mitochondrial biogenesis is responsible for cardarine's substantial impact on muscular endurance. Researchers discovered that cardarine changes more fast-twitch fibres into slow-twitch fibres (2), which makes people who take it less likely to become fatigued during physical activity.

Due to the presence of mitochondria, slow twitch fibres are more effective at utilising oxygen, which enables greater levels of ATP generation (energy) within the muscle cells.

Cardarine was found to boost endurance in mice by 68% in just three weeks, according to a study that used mice (3).

In the past, a user might have been able to complete 30 minutes of cardiovascular exercise before becoming exhausted; after taking cardarine, however, they might be able to complete 50 minutes of cardiovascular exercise before reaching the same level of weariness.

The effects of cardarine on muscular endurance are rather spectacular, and when combined with regular cardiovascular exercise, they will also (indirectly) aid to burn more fat stores. This will be achieved by increasing the amount of fat that is burned (due to increased calorie burn).

The majority of the endurance-boosting effects of cardarine are very transient and will disappear once a cycle of treatment has been completed. However, due to the fact that cardarine improves muscle memory, users are likely to feel increased endurance after taking the supplement (the heart is a muscle).

Whether or not an individual continues to engage in endurance training after completing a cardarine cycle will determine the amount of endurance that is retained from the previous cycle.

Glycogen Storage

As a result of cardarine's ability to boost glycogen storage within the muscles, users report feeling like they have fuller muscles while on-cycle.

Bodybuilders and fitness models, both of whom need to have full muscle bellies when they perform and are prone to glycogen depletion as a result of following calorie restrictive diets, may find this to be useful.

As a result of the reduced amounts of extracellular fluid, an increase in the vascularity of the tissue may also take place.

Enhanced levels of Cholesterol

Cardarine has been demonstrated to possess cardioprotective qualities, in part because of the substantial impact it has on HDL cholesterol (the good type that you want high).

When compared to other anabolic agents like SARMs and anabolic steroids, which can lead to undesirable shifts in cholesterol levels, this advantage is truly exceptional.

The earlier phase II trial that was quoted found that HDL levels climbed by 17 percent and LDL cholesterol decreased by 7 percent when a dosage of 10 mg/day was used.

Combining cardarine with anabolic steroids or SARMs may therefore not only further improve body composition and performance, but also minimise the chance of developing cardiovascular disease.

Due of cardarine's propensity to improve cholesterol levels, there is a possibility that it could one day be used as a viable treatment for dyslipidemia.

Does Not Affect Testosterone Levels In Any Way

Because of an excessive stimulation of the androgen receptor, anabolic steroids and SARMs bring to a reduction in the body's natural production of testosterone. Cardarine, on the other hand, does not impact the HPT (hypothalamic-pituitary-testicular) axis; hence, testosterone levels will not fluctuate while taking it, and post-cycle therapy will not be necessary.

There is no virilization in females.

In terms of suppressing the adverse effects that are associated with being masculine, cardarine is an appropriate substance for females to ingest. Therefore, cardarine may be a better option for women who are interested in taking anabolic steroids or SARMs with the primary purpose of reducing their subcutaneous fat. This is because cardarine helps women maintain their feminine traits.

This is because cardarine does not have any effect on hormones, particularly testosterone, and as a result, it does not cause side effects such as hair loss, clitoral enlargement, breast reduction, or a deepened voice box.

Toxic effect on the liver

At doses of up to 10 milligrammes per day, cardarine had no discernible effect on levels of ALT and AST in the liver measured in humans participating in studies of phases I and II.

However, Dr. Thomas O'Connor has worked with patients who have used cardarine, and as a result, he has compared the hepatotoxicity of cardarine to the toxicity that would be caused by taking 50 mg per day of anavar (a mega dose).

It's possible that the fact that cardarine causes cellular proliferation is to blame for the study and anecdotal findings that don't match up with one other. As a result, it promotes the growth and division of cells, which ultimately results in an increased cell count. This is absolutely fine in a healthy person, but cardarine has the potential to hasten the death of liver cells in a person who already has a hepatic damage.

Users frequently combine cardarine with other hepatotoxic chemicals, which may explain why such hepatic issues occur. This is because cardarine is frequently taken by individuals who have also taken SARMs or/and anabolic steroids.

Note that taking antidepressants with cardarine, in addition to drinking alcohol, could be a very dangerous combo.

Insomnia

Insomnia is reported by some people who use cardarine, which points to a stimulating effect on the central nervous system (CNS) and a rise in the output of adrenaline.

Users may be able to avoid this adverse effect by taking their dose earlier in the day (ideally in the morning), so leaving a significant amount of time for the central nervous system (CNS) to regulate before going to bed.

Although there is a possibility that the central nervous system (CNS) would become more stimulated, it is not thought that this effect will be overwhelming. Therefore, cardarine does not imitate the jittery effects of other thermogenic fat burners that are more well-known, such as clenbuterol. Cardarine, on the other hand, keeps users' energy levels consistent (which prevents crashes) while simultaneously enhancing their general sense of well-being.

Because cardarine has a stimulating effect, it is probably best to schedule your workouts for earlier in the day rather than later. Consequently, taking it prior to your workout, preferably in the morning, will provide your central nervous system with adequate time to wind down before bedtime.

Reference:

 Koh B (2013-03-22). "Anti-doping agency warns cheats on the health risks of Endurobol". The Conversation.

 Sahebkar A, Chew GT, Watts GF (March 2014). "New peroxisome proliferator-activated receptor agonists: potential treatments for atherogenic dyslipidemia and non-alcoholic fatty liver disease". Expert Opinion on Pharmacotherapy. 15 (4): 493–503. doi:10.1517/14656566.2014.876992. PMID 24428677. S2CID 21158696. Despite these promising early results, the further investigation and development of GW501516 was discontinued after observations in animal studies of its association with the rapid induction of cancers in several organs (liver, stomach, tongue, skin, bladder, ovaries, womb and testes

 "GW501516 GlaxoSmithKline, Ligand milestone payment". R & D Focus Drug News. 28 June 2004.

 Wolf G (November 2003). "The function of the nuclear receptor peroxisome proliferator-activated receptor delta in energy homeostasis". Nutr. Rev. 61 (11): 387–90. doi:10.1301/nr.2003.nov.387-390. PMID 14677574. S2CID 12362203.

 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. Bibcode:2001PNAS...98.5306O. doi:10.1073/pnas.091021198. PMC 33205. PMID 11309497.

 Flynn J (11 February 2004). "Father and Son: In Two Generations, Drug Research Sees a Big Shift". The Wall Street Journal.[permanent dead link]

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

 "GW501516 GlaxoSmithKline phase change II, UK". R & D Focus Drug News. 25 February 2002.

 "Ligand Pharmaceuticals Incorporated Earns $1 Million Milestone Payment as GlaxoSmithKline Advances Development of 501516". Reuters Significant Developments. 5 June 2003.

 Barish GD, Narkar VA, Evans RM (March 2006). "PPAR delta: a dagger in the heart of the metabolic syndrome". The Journal of Clinical Investigation. 116 (3): 590–7. doi:10.1172/JCI27955. PMC 1386117. PMID 16511591.

 Dressel U, Allen TL, Pippal JB, Rohde PR, Lau P, Muscat GE (December 2003). "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". Molecular Endocrinology. 17 (12): 2477–93. doi:10.1210/me.2003-0151. PMID 14525954.

 Billin AN (October 2008). "PPAR-beta/delta agonists for Type 2 diabetes and dyslipidemia: an adopted orphan still looking for a home". Expert Opinion on Investigational Drugs. 17 (10): 1465–71. doi:10.1517/13543784.17.10.1465. PMID 18808307. S2CID 86564263.

 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.

 Newsholme SJ, Dunsford WS, Brodie T, Brennan C, Brown M, Geiger LE (2009). PS 896 - Mouse 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.

 Fan, Weiwei; Waizenegger, Wanda; Lin, Chun Shi; Sorrentino, Vincenzo; He, Ming-Xiao; Wall, Christopher E.; Li, Hao; Liddle, Christopher; Yu, Ruth T.; Atkins, Annette R.; Auwerx, Johan (2017-05-02). "PPARδ Promotes Running Endurance by Preserving Glucose". Cell Metabolism. 25 (5): 1186–1193.e4. doi:10.1016/j.cmet.2017.04.006. ISSN 1550-4131. PMC 5492977. PMID 28467934.

 Bezar M (2011-11-01). "Faster. Higher. Squeakier". Outside magazine. Retrieved 2013-04-02.

 Laurance J, Rajan A (2008-08-01). "Warning to Beijing Olympics over pills that mimic exercise". Health News, Health & Wellbeing. The Independent. Retrieved 2008-08-01.

 WADA 2009 Prohibited List Archived February 3, 2009, at the Wayback Machine

 "Anti-doping agency warns athletes of black market drug". New Scientist. 2013-03-26.

 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.

 Sanchis-Gomar F, Lippi G (March 2012). "Telmisartan as metabolic modulator: a new perspective in sports doping?". J Strength Cond Res. 26 (3): 608–10. doi:10.1519/JSC.0b013e31824301b6. PMID 22130396.

 "WADA issues alert on GW501516". World Anti-Doping Agency. 2013-03-21. Archived from the original on June 2, 2013.

 Stokes S (15 April 2013). "GW501516 positives confirmed, three of four riders are from same BCR Pizza Hut team". velonation.com.

 Stokes S (30 July 2013). "Four riders each handed two year bans for use of GW501516". velonation.com.

 List of sanctions Archived July 15, 2014, at the Wayback Machine, uci.ch

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

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

 Sanctioned athletes list – 26 June 2014

 Associated Press: Doping probe launched into Russian walkers, espn.com, 11 July 2014

 Dan Rafael (2019-04-19). "Sources: 'Big Baby' Miller failed three drug tests". ESPN.com. Retrieved 2019-04-21.

 "Heavyweight Miller gets 2-year PED suspension". ESPN.com. 2 December 2020. Retrieved 13 July 2022.

 "London 2012 medallist Nijel Amos suspended after positive doping test". the Guardian. 13 July 2022. Retrieved 13 July 2022.

 Pelton P (April 2006). "GW-501516 GlaxoSmithKline/Ligand". Current Opinion in Investigational Drugs. 7 (4): 360–70. PMID 16625823.

 Sprecher DL (December 2007). "Lipids, lipoproteins, and peroxisome proliferator activated receptor-delta". The American Journal of Cardiology. 100 (11 A): n20-4. doi:10.1016/j.amjcard.2007.08.009. PMID 18047848.