Cardarine (GW501516)

INTRODUCTION

Cardarine also known by GW501516, is a chemical that has been developed by conjoint research of Ligand Pharmaceuticals and Glaxo Smith Kline in 1992.

The drug was initially manufactured and launched in the market for its phenomenal ability to reduce predisposition to dyslipidemic disorders like: atherosclerosis – the most imperative pathophysiological determinant of various vascular diseases like myocardial infarction (cardiac arrest), stroke etc.

But, the drug gained popularity in the modern world among athletes for its excellent contribution to enhance endurance, strength – dream come true for all aspiring athletes.

How does it work?

The PPAR Agonists

Cardarine is one of the PPAR (peroxisome proliferator-activated receptor) agonists. Similar to SARMs (selective androgen receptor modulators), PPAR agonists also activate the androgen receptors of muscles.

These Receptors increase glucose and amino acids uptake into skeletal muscles by increasing insulin sensitivity.

Glucose

Glucose enters into the cell through GLUT- 4 receptors on the cell surface membrane. The membrane is sensitive to anabolic hormone insulin.

The increased entry of amino acids mean more proteins could be synthesized, increasing muscle hypertrophy and growth. This means whatever we consume, the body does not store it as carbohydrate or fat. Instead, our bodies use it to promote lean muscle mass.

The class PPAR is a group of nuclear receptors, involved in initiating genetic pathways involved in energy expenditure. (i.e. the ones that are activated during exercise)

Thus, it also increases the levels of ABCA1, cholesterol transporter.

HDL & LDL

Cardarine increases the levels of HDL (good cholesterol) that transfers cholesterol from the periphery to liver for metabolism and decreases the levels of LDL (bad cholesterol) that work antagonistic to HDL. Cardarine also improves liver function and allows body to get rid of any excess fat. Overall, these result in decrease in triglyceride, cholesterol, glucose levels in the body.

Benefits

Development of Cardarine is considered to be one of the legendary innovations in the sport’s industry as well as in medicine. Because of its tremendous contributions, we will list some of which in the following section.

1. Bioavailability

Bioavailability of the drug is very high, which means the body readily absorb it into the system and a small dose is sufficient enough to produce the desired performance.

2. Halt the Synthesis of Fatty Acid

GW501516 releases pro-inflammatory mediators in fat cells and reduces the gene activity involved in lipogenesis. In simpler terms, that the body is able to halt the synthesis of fatty acid.

3. Non Stimulant

Cardarine doesn’t act as a stimulant, which means its euphoric effects on the body do not come with anxiety or fatigue.

4. Non Toxic

The drug has no adverse effects on liver or any other organs and users won’t develop tolerance to the drug. Hence, unlike SARM, you do not need a PCT (post cycle therapy).

5. Non Estrogenic

Cardarine has no effect on testosterone or estrogen levels, so there are no associated adverse effects such as hair loss (learn how n2shampoo stops hairloss), high blood pressure, gynecomastia, weight gain, water retention.

6. Work Well In Stack

Users can take GW501516 with anything and addition of SARM or any other endurance enhancing drug would increase the outcome.

7. Reduce Glucose Level

By increasing glucose intake into the cell, it reduces the glucose level in the blood and hence has potential to be a treatment of obesity and type- 2 diabetes mellitus.

8. Boost Recovery

Along with other benefits in bodybuilders, Cardarine also elevates the mood and allows rapid recovery. This allows athletics to train them harder for longer period of time, with shorter resting periods.

Cardarine Uses

Role in sport’s industry

The actions of Cardarine as PPAR agonists have gained its fame as the ultimate endurance enhancer. This process includes expression of PPAR gene in slow twitch muscles, allowing more usage of oxygen and promoting muscle hypertrophy and growth, which as a result improves stamina and performances.

Therefore, athletics can invest most of their time on training themselves, with shorter breaks in between work outs. Additionally, Cardarine improves liver function and healing process, allowing rapid recovery from any trauma. This helps maintaining a healthy equilibrium and improves the overall productivity.

Effect on metabolism and weight

Sometimes, even with proper balanced diet and regular physical activities, health enthusiasts fail to shed that extra calories from the body due to poor metabolism rate. Promoting fat loss still remains a daunting, exhausting task. Fortunately, development of Cardarine came as a savior to medical industry for its ability to enhance metabolism. It increases lipolysis, the main mechanism that is activated during starvation. But, unlike starvation, there is no catabolic effect on muscles, i.e. no muscle wasting, this means there is preservation of the lean muscle mass. Even with high calorie diet, Cardarine can promote conversion of stored fat to energy. This property qualifies Cardarine as a cure for obesity.

Role in metabolic disorders

As odd as it might sound, glucose being the prime source of fuel for all the metabolic reactions in the body, it is still hazardous if excess amounts remain floating in the blood. For example, one such disorder of hyperglycemia is Diabetes mellitus (DM). In type -2 DM, there is relative insulin deficiency, most commonly due to reduced insulin sensitivity. This results in failure of glucose to enter in to the cells, increasing blood glucose levels. In addition, Cardarine promote insulin sensitivity and could possibly reduce the prevalence of type -2 diabetes mellitus.

Adverse effects

There has been no reported major side effects, but during trails there has been incidence of cancer in mice but recent researches have concluded that Cardarine prevents malignant growth of cancer cells in prostrate, colon and breast.

In current study, we analyzed the impact of PPARβ/δ activation on the growth of the NPC cells with a PPARβ/δ agonist, GW501516, who had shown anti-tumor effect on breast and skin tumors.

Front Pharmacol. 2018; 9: 648.

Dosage

Even though Cardarine exhibit such phenomenal activities, but like any other medicines, users should closely monitor the dosage. An average dose of 10-20 mg per day for 8/12 weeks with 4/6 weeks breaks in between is sufficient. Also, you can use it with other SARM for better outcome. One of the most common choice would be ostarine in a cutting stack.

Conclusion

With appropriate dose, Cardarine is a promising drug, even when consumed alone, without any adverse effects related to anabolic steroids.

However, WADA (The World Anti-Doping Agency) has banned Cardarine for professional athletics because of the competitive benefits it has on the body as performance enhancer. That being said, the drug still has profound usage in medicine as treatment of obesity, diabetes mellitus and dyslipidemia.