Cardarine (GW501516) is a PPAR receptor agonist invented by Ligand Pharmaceuticals and GlaxoSmithKline in the 1990s. Cardarine was originally developed to treat obesity, diabetes, lipid strain, and cardiovascular diseases. Those who run blood work when using cardarine will notice that their cholesterol levels improve substantially.
PPAR receptor agonists are drugs which stimulate the expression of genes involved in the metabolism of glucose and fatty acids. There are three different PPAR isoforms:
• alpha (α)
• beta/delta (β/ δ)
• gamma (γ)
PPAR-alpha activation increases the expression of lipoprotein lipase and apolipoprotein A-V (apoA-V) and decreases the expression of apoC-III in the liver. This decreases LDL (bad) cholesterol, decreases blood triglycerides and liberates fatty acids, allowing them to be oxidized and burned.
In addition, PPAR-alpha activation increases hepatic apoA-I andapoA-II, which increasing HDL (good) cholesterol. PPAR-alpha activation increases fat loss and improves cholesterol levels by lowering LDL levels, decreasing blood triglycerides and increasing HDL levels.
Note: LDL stands for low density lipoprotein (bad cholesterol). HDL stands for high density lipoprotein and if often referred to as good cholesterol.
Note: Lipase is an enzyme that helps break down fats into glycerol and fatty acids.
The exact actions of PPAR-beta/delta in humans is still under development. Animal studies show that PPAR-beta/delta activation decreases adiposity tissue (body fat). Most researchers speculate that PPAR-beta/delta acts similarly to PPAR-alpha but has more specific actions in skeletal muscle.
Activation of PPAR-gamma increases the transcription of genes and enzymes involved in insulin sensitivity and decreases their activity in adipogenesis (fat cell creation). Activation of PPAR-gamma could theoretically cure type 2 diabetes since obesity and insulin resistance suppress PPAR-gamma activation. The anti-diabetic drug thiazolidinediones has successfully treated type-2 diabetes in human clinical trials through its role in activating PPAR-gamma, though hepatoxicity and risk of congestive heart failure discontinued the research on the drug.
Side Effects, Dosages and Half Life
Side effects are rare with Cardarine. Since cardarine is non hormonal, there is no need to worry about post cycle therapy (PCT) or hormone suppression. The recommended dose for both men and women is 10-20 milligrams (mg) per day. Since Cardarine is non-hormonal, you could theoretically run it forever. However, I personally don’t think running anything indefinitely is smart. I recommend 12-16 week cycles of caradrine with 4 week breaks in between.
The half-life of cardarine is 20-24 hours, meaning that all you need is only a once per day dose. It does not matter if you take cardarine on an empty stomach or with food. Also, since cardarine is not a stimulant, taking it near bedtime will not affect sleep in any way.