Development of PPAR-agonist GW0742 as antidiabetic drug: study in animals

GW0742, a selective peroxisome proliferator-activated receptor (PPAR)-δ agonist, has been shown to ameliorate (make better) metabolic abnormalities including IR in skeletal muscle in mice fed high-fructose corn syrup.

GW0742 (Super Cardarine)

 GW-0742, which is being dubbed as a ‘Super Cardarine’.

GW-0742 vs GW-501516

GW-0742 is a PPARβ/δ agonist that structurally looks like GW501516 but with one hydrogen atom replaced with a fluorine atom. 

It has all the positive effects of Cardarine with better research results in the labs. 

Just like GW-501516, GW0742 has shown very impressive research results in body fat reduction and performance enhancement. 

GW-0742 differs from  GW-501516 due to enhanced synthesis and biological activity with user reports indicating it to be much more potent with more drastic results.

Currently there are no human trials to work with, and no animal trials looking at body composition / endurance (yet)

Cardarine Cancer studies

Cardarine has gotten a bad rap because of a study from 2007. The flawed study observed mice getting cancer when given GW 501516 in extremely high doses.  If you read the details of the study, you’ll see that the mice were given 3 MG of cardarine per day. To put this in perspective, the common 200 pound athlete only uses 10 to 20 MG per day.

Considering the size variance between rodents and humans, this would have been like giving a human nearly 100 mg per day.

Also worth noting is that the mice in the study were given 7,12-Dimethylbenz(A)Anthracene (DMBA)  for an entire year. DMBA is a known carcinogen that is considered extremely toxic.  It is an immune suppressor and a tumor accelerator. So, mice got cancer!

Therefore, this study is pretty flawed and the public concern over Cardarine has been blown out of proportion.

I’m not saying that there is no risk whatsoever as any synthetic compound has some level of risk. However, I truly believe the credibility of the cancer studies should be taken with a grain of salt, especially when considering the rats being given DMBA for a  whole year.

View our latest HPLC-Assay: Purity (3rd-party lab test) on GW-0742

1 bottle (30mL) of GW-0742, dosed at 20mg/mL:

  • Best 8-16 Week Cycles
  • Increase Endurance
  • Increase Energy
  • Increase Recovery
  • Increase Metabolic Rate
  • Fatty Acid Oxidation
  • Increases Insulin Sensitivity in rats
  • In diabetic rats fed a high fructose diet, the group given GW0742 had lower blood sugar than control, and insulin sensitivity was increased
  • Improves Expression of Type 2 Collagen and also indirectly reduced cartilage wear and tear
  • Promotes reverse cholesterol transport. (This means is that it’s moving cholesterol back to the liver which should lower total cholesterol.)
  • Reduces Inflammation in Gut
  • Limits Right Heart Hypertrophy and shown to be cardiac protective
  • Enhances Lipid Metabolism


Methods and results and further read here

Male C57/Bl6 mice were injected with the specific PPARβ agonists GW0742 or GW501516, or vehicle. Cardiomyocyte size and vascularisation were determined at different time points. Expression differences were investigated by quantitative reverse transcriptase–polymerase chain reaction and western blotting. In addition, the effects of PPARβ stimulation were compared with hearts of mice undergoing long-term voluntary exercise or pharmacological PPARα activation. Five hours after GW0742 injection, we detected an enhanced angiogenesis compared with vehicle-injected controls. After 24 h, the heart-to-body weight ratios were higher in mice injected with either GW0742 or GW501516 vs. controls. The increased heart size was due to cardiomyocyte enlargement. No signs of pathological cardiac hypertrophy (i.e. apoptosis, fibrosis, or deteriorated cardiac function) could be detected. The effects are mediated via calcineurin A (CnA) activation as: (i) CnA was upregulated, (ii) GW0742 administration or co-transfection of PPARβ significantly stimulated the activity of the CnA promoter, (iii) PPARβ protein bound directly to the CnA promoter, (iv) the CnA target genes NFATc3, Hif-1α, and Cdk 9 were upregulated in response to PPARβ stimulation, and (v) the inhibition of CnA activity by cyclosporine A abolished the hypertrophic and angiogenic responses to PPARβ stimulation.

In other words  with  GW-0742 or GW-501516 at high doses

It increases the size of the rats heart which can be very dangerous. It does so through the activation of calcineurin.

This side effect doesn’t take weeks to come into fruition and high dosages aren’t the cause of it.

Quite on the contrary, mice developed a bigger heart just 24 hours after ingestion (read figure 3.1).

What Is GW-0742?

GW-0742 does NOT modulate androgen receptor function. GW-0742 has a role as a PPARbeta/delta (peroxisome proliferator-activated receptor) agonist.

Application Of GW-0742

In the following trial, GW-0742 illustrates novel progress in the endurance of mice:

GW-0742 Study 1

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