Cardarine, also known as GW-501516/Endurobol, is a novel and selective PPARδ agonist used in the treatment of dyslipidemia. PPARδ expresses in adipose tissue, liver, skin, brain, and skeletal muscle.
The research to its discovery began in 1992 during the collaboration between GSK and Ligand Pharmaceuticals.
Clinical trials on this compound were conducted only up to phase II and were discontinued in 2007 as intestinal adenoma was observed in mice. But later on, when a higher dose was used, it was observed that the physical performance of rats was enhanced.
In this review, the information on the research conducted on Cardarine, its mode of action, its uses, and side effects is covered. Also, details on where to buy this product for the best price are mentioned.
Cardarine Overview: Is it a SARM?
SARMs (Selective Androgen Receptor Modulators) are very much like anabolic agents or androgenic drugs but act selectively on tissues. They do not generate tissue-related side effects.
Cardarine activates the PPAR-δ pathway and does not work on the androgen receptors in the muscle and bone tissues directly. Hence, it is NOT considered to be a SARM. Nevertheless, Cardarine can be taken along with any other SARM, depending on the goal.
Is Cardarine a legal compound?
Cardarine may be legal to be consume all over the world, except Australia, though you might need a doctor’s prescription for consuming it.
It may be labeled “Research Chemical” or “Not for human consumption,” but it only means that it is not FDA-approved yet and is meant only for research purposes. Cardarine does cause side effects in humans, but some of them can be avoided if it is taken at the right amounts.
How Does Cardarine Works?
Cardarine selectively binds to PPARδ. The coactivator PGC-1α then binds to form the PPARδ-coactivator complex. The expression of proteins involved in the dissipation of energy is increased by this complex, thereby aiding in a high amount of energy.
During physical exercise or long-term fasting, fatty acids burn. The amounts of PPARδ will increase in the muscles. Cardarine activates PPARδ which leads to an increase in the lipid catabolism of skeletal muscles.
Cardarine Pros and cons
- Boosts stamina
- Improves cardiovascular health
- Burns extra fats quickly
- Preserves muscle mass
- Promotes the development of muscle fibers
- Protects the liver and kidneys from damage
- Takes around 2 months to show best results
- Consuming excess can give negative results
- May cause digestive problems like constipation and stomach cramps
Lab tests and results
- The oxidative capacity and metabolic efficiency of skeletal muscle are elevated by endurance exercise training. Healthy, normally physically active subjects participated in a study and were subjected to knee extensor exercises. The study concluded that in the skeletal muscles, transcription, and mRNA content of the transcription factor coactivator PGC-1α increased due to prolonged exercise.
- Another study subjecting human subjects to cycling also proved that because of the increased expression of FAT/CD36 and CPT I mRNA, there was an increase in the total lipid oxidation by 24%.
- GW501516 and 2-BP were administered to bovine embryos separately in a study. Compared to the control- and 2-BP-treated embryos, it was observed that the embryos treated with GW501516 hatched quicker and had low ROS levels and apoptosis.
- The activation of PPARδ by GW501516 improved PEPCK and CPT1 protein expression in the embryos. Due to this, there was a balance between lipolysis and fatty acid β-oxidation. It has been demonstrated that PPAR-δ agonist lowered plasma insulin levels when given the right doses, without having negative effects on the glycemic control. In obese mouse models, it was found that this agonist improved glucose tolerance and insulin sensitivity by reducing adiposity.
- A two-week clinical study was conducted in healthy and moderately overweight human volunteers. The results demonstrated that synthetic Cardarine improved dyslipidemia and glucose metabolism by reducing plasma insulin. There was a reduction in the content of liver fat.
- When Cardarine was treated with TNFα (a pro-inflammatory cytokine), the expression of adiponectin was reduced. That means the expression of the insulin receptor was increased, which hints that PPARδ might serve as a treatment of insulin resistance in patients with type 2 diabetes mellitus.
- There was a significant attenuation in the hydrogen peroxide (H2O2)-induced expression of TSP-1 in VSMCs, ie, vascular smooth muscle cells due to the activation of PPAR-δ by Cardarine. Cellular oxidative stress was reduced.
- The increase of muscle PGC-1α was shown to reduce muscle atrophy and improved muscle function in the cases of Duchenne Muscular Dystrophy (DMD).
To buy the product, you may visit www.provenpeptides.com. This is one of the most reliable places to buy it, as many websites are selling the product for a higher price and most importantly with a compromise on the quality. Here, a 15 ml bottle is available for $39.99. Free shipping is available for orders above $75. Therefore, purchasing a 60 ml bottle costing $99.99 would save a lot of money.
If the order is placed via a credit card, shipping will be done in 1 business day. It will take around 3 days for shipping if the order is placed via eCheck. Packages will be delivered anywhere in the US within 3 business days after shipment, and internationally within 2 weeks. International orders may get delayed sometimes due to customs issues.
The product is eligible for a full refund if
- you are unsatisfied with it; although the return shipping cost will not be reimbursed. It has to be sent before 90 days of purchase
- the product does not arrive due to USPS problems
- an international shipment does not pass the US customs
- international customers return the product
- There will be no refund if
- the item is marked as “delivered” by USPS and you cannot find it
- if the item is held by foreign customs although it was passed by the US customs
- if the shipment passes through US customs but the foreign delivery service losses the package.
Does Cardarine cause cancer?
Many recent studies support the evidence that Cardarine aids in inhibiting tumorigenesis. It promotes apoptosis (cell death) in the undifferentiated C666-1 nasopharyngeal carcinoma (NPC) cells, thereby preventing the birth of new cancer cells.
A study did relate PPARδ to be playing a role in causing colitis-associated colorectal cancer in mice, but the mechanism is still unclear. A reduction in the tumorigenicity in breast cancer cells of mice was seen when GW501516 was administered to act along with PPARδ. PPARδ forms an antitumorigenic complex with c‐Myc in the presence of Cardarine.
Benefits of Cardarine
Although the mechanism that modulates the inflammatory response in muscle is not clear, routine activities indeed lead to tissue damage and inflammation that impairs muscle recovery and function.
Improvement in insulin sensitivity
Cardarine activates PPARδ which will lead to the burning of fatty acids. This, in turn, leads to an improvement in the insulin sensitivity of the liver, muscle, and adipose tissues.
PGC-1 co-activates glucocorticoid receptor and the liver-enriched transcription factor HNF-4α. This, in turn, activates the PEPCK promoter, resulting in healthy hepatic gluconeogenesis.
Reduction of inflammation in skeletal muscles
Using Cardarine reduces the production of pro-inflammatory cytokines. The reduced local inflammatory response generated will control the tissue damage and restores muscle tetanic contraction.
Increase in good cholesterol (HDL) levels
Studies have proven that when Cardarine was given to patients with a low amount of high-density lipoprotein (HDL), the amount of HDL increased after a few weeks.
Also, the amount of low-density lipoprotein (LDL) significantly decreased.
Enhancement of running endurance
Cardarine was found to enhance the running endurance by increasing serum galactose and β-hydroxybutyrate when administered to mice.
Good effect on blood vessels
Nitric oxide relaxes the blood vessels. Cardarine elevates nitric oxide and protects the blood vessels.
Cardarine is also known to lower the oxidative damage that happens in blood vessels.
Protection of the liver from damage
It is a known fact that the liver plays a major role in the regulation of fat. Normally, glucose is converted into energy. But, Cardarine makes the liver convert unwanted fatty acids into energy.
This way, there will be a reduction in unwanted fats in the body.
Less lipid accumulation in adipose cells
Cardarine ensures low accumulation of lipids in the adipose cells. This may allow the normal production of adipocytokines and promotes the burning of fats in the liver and muscle.
Side effects of Cardarine
When the clinical study was conducted in mice, Cardarine did cause cancer. But the dosage given was high and it was given for a very long time.
In humans, it was seen that Cardarine had a role to play in killing cancer cells. If taken at a proper dosage, Cardarine does not produce any significant side effects.
Pregnant women and men with already low testosterone levels are not supposed to take Cardarine.
Skin and acne problems might occur in some women upon consuming Cardarine. But all of these minor problems can be controlled if a nutritionist could guide you about the correct dosage and also the right diet plan for you.
Natural bodybuilding is trending amongst youngsters and middle-aged people. Bodybuilders must optimize their intake of calories such that calorie reduction leads to fat loss, but muscle mass is maintained.
Research has shown that natural bodybuilding requires effort. This depends on the following factors:
For lean body mass (LBM) to be retained, dieting which reduces weight must continue for more than two to four months. Around 0.5 to 1% of the body weight may be reduced this way. This varies for leaner people of course.
For good growth of lean body mass, athletes must consume more proteins. It was proved that leaner people require more proteins compared to the ones with more body fat.
Although carbohydrate requirement also varies individually like proteins, it is noteworthy that the insufficient amount of carbohydrates will reduce the performance and impair strength training. A higher protein to carbohydrate ratio is supposed to be maintained to preserve lean body mass.
Differences in individuals and ketogenic diets
The effect of ketogenic diets on bodybuilding has not been studied deeply. Some studies conducted on very few subjects showed that there was only an average reduction in calories.
Timing of meals
There was one study in which protein and carbohydrate were provided in higher quantities before and after exercise. This timing of nutrition resulted in a gain in strength and size when compared with the supplements given after the training bout.
Frequency of meals
When meals were fed in an irregular pattern for a week, it was noted that there was a decrease in post-prandial thermogenesis. Insulin sensitivity and blood lipid profiles were affected as well.
When trained, athletic subjects like boxers were fed 6 meals a day, their lean body mass was not lost as much as it did during consumption of the same diet as 2 meals a day.
Consumption of nutritional supplements
Along with resistance training and cardiovascular training, bodybuilders depend on nutritional supplements. Cardarine is one such popular supplement.
There has not been sufficient proof that micronutrient deficiency in bodybuilders could prevent them from achieving their goals. However, a good balance and availability of vitamin D, calcium, zinc, magnesium, and iron may be beneficial as these might be present in lower quantities due to constant dieting.
It is not easy to prepare for bodybuilding competitions. Many of such participants were seen binge eating before and after competitions. Some have reported anxiety, short tempers, and anger.
Open communication is very important to avoid these psychosocial issues. Studies have shown that women bodybuilders were scared of becoming fat, and were unable to control the urge to eat.
On the other hand, male bodybuilders, being unsatisfied with their muscle size, showed obsessive behavior. Eating disorders such as anorexia nervosa and bulimia nervosa were also exhibited.
Adam, Age: NA, United States
“Cardarine is currently one of the strongest endurance enhancers you can find. I can say this with confidence because I have tried other products like Stenabolic as well. Having been extensively used by bodybuilders, Cardarine has proved to be worth everything it has got. I observed that this product ensures to fulfill the claims it makes.”
Ed, Aged 39, United States
“I always complained of having metabolic issues and was not able to reduce unwanted fat no matter what ways I tried. But after consuming Cardarine for just 6 weeks, I could see remarkable changes in my body.”
Richy, Aged 42, UK
My muscle mass improved, and so did my energy levels. All the bad fat went down rapidly. I could say this with assurance because I have been observing this since I began consuming Cardarine.”
The Recommended Dosage of Cardarine: Cycles
After conducting dosage trials, the correct dosage of Cardarine to be taken is found to be 10 mg to 20 mg per day, for about 8 weeks. However, good results may be seen in 5 weeks. Begin with a dosage of 10 mg for a few weeks and eventually double the dosage.
Some athletes have used up to 30 mg per day, but it is recommended that the maximum dosage be 20 mg, as human trials for this compound are limited.
Conclusion: Would I recommend it?
Cardarine burns stored fat in the skeletal muscles and utilize fatty acids to convert to energy, leading to a reduction in body fats.
The above processes are unlikely to occur easily in many people. So, an excellent choice to have such gains would be to use Cardarine. I recommend it to people who are looking to build their bodies for professional gains and also to those wanting to boost up their energy and want to be fit.