Gw-501516 is a PPAR receptor agonist invented by Ligand Pharmaceuticals and GlaxoSmithKline in the 1990s. Gw-501516 was originally developed to treat obesity, diabetes, lipid strain, and cardiovascular diseases. Those who run blood work when using gw-501516 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

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 particles (bad cholesterol), decreases blood triglycerides levels and liberates fatty acids, allowing them to be oxidized (burned). In addition, PPAR-alpha activation increases hepatic apoA-I andapoA-II, which increasing HDL levels (good cholesterol). In summary, 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 and is often referred to as bad cholesterol. HDL stands for high density lipoprotein and if often referred to as good cholesterol.

Note: A lipase is an enzyme that helps break down fats into glycerol and fatty acids.

PPAR-beta/delta

The exact actions of PPAR-beta/delta in humans are still being researched. Animal studies show that PPAR-beta/delta activation decreases adipose tissue (body fat). Most researchers speculate that PPAR-beta/delta acts similarly to PPAR-alpha but has more specific actions in skeletal muscle, in both humans and animals.

PPAR-Gamma

Activation of PPAR-gamma will increase the transcription of genes and enzymes involved in insulin sensitivity and decrease their activity in adipogenesis (fat cell creation) and the inflammatory process. Obesity and insulin resistance suppress PPAR-gamma activation. Activation of PPAR-gamma could theoretically cure type 2 diabetes. The anti-diabetic drug thiazolidinediones has been successfully used to treat 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 are rare with Gw-501516. Since Gw-501516 is non hormonal, there is no need to worry about post cycle therapy or hormone suppression. The recommended dose for both men and women are 10-20 milligrams (mg) per day. The half-life of gw-501516 is 20-24 hours, meaning that a once per day dose is all that is needed.

“20mg is my favourite GW-501516 dosage. I feel like it’s totally safe as long as it’s cycled. I prefer not to use it while bulking. Only while cutting. I feel like Gw-501516 sort of ‘flips a genetic switch’ that makes you more like an endurance athlete. I think it’s incredible while fasting, or when following a ketogenic or low carbohydrate diet. It’s also helpful in keeping energy levels high on low carb days when carb cycling. It’s very synergistic with other fat burners and I think it’s very helpful in preparing for a bodybuilding competition to keep energy and stamina up.

I typically recommend 20mg/day for both men and women. Unless a woman is less then 110 pounds, then I would tell her to use only 10mg. I don’t think GW-501516 loses its effectiveness but I think being on it for longer periods of time increases risks. I personally feel comfortable using it 5 days on/ 2 days off, 2 weeks on/1 week off, or 1 month on/1 week off.”

• Dr Tony Huge

“I don’t feel that GW-501516 is necessarily good for muscle gain, but it’s very good for weight loss and cardio benefits. I notice rapid improvement in cardio when taking it. It’s good for people getting ready for bodybuilding contests, endurance athletes, and fighters. It supports weight loss. Benefits start as low as 10mg/day. I’ve experimented with dosages as high as 50mg/day but noticed no benefits going past 30mg/day.

I found the injectable version (called cardiolone) superior to the oral version. If you suspend GW-50516 in water, it’s slow action. If you suspend it in solution, it is fast acting.”

• Coach Trevor