GW501516, otherwise known as GW1515 or GSK 516 is a kind of drug that is considered as a PPAR-delta modulator. This drug is known to activate the AMP activated protein-kinase. It stimulates the uptake of the glucose in the tissue of skeletal muscles. The drug is also proven to demonstrate the reversal of abnormalities of the metabolic processes of men who are obese. It is also known to cure conditions like the pre-diabetic metabolism syndrome in which it is observed to stimulate the oxidation of fatty acids.
Also, in the previous years, the drug has been known to be proposed as a potent drug for treating other conditions that are related to obesity. When coupled with another compound known for its synergistic property, the AICAR, subjects, mainly laboratory animals, are seen to be more enduring when it comes to physical exercise.
Initially, GW501516 was discovered in 1992 by the GSK and another company called the Ligand Pharmaceuticals. In a report in the year 2000, it was stated that the companies used the drug in the phase I trial stage to treat hyperlipidemia. According to another report, it was said that GSK utilized structure-based designing procedure of drugs. The company is reported to use combinatorial chemistry techniques as well.
After the first phase of the trial of the drug, it was reported that Ligand Pharmaceuticals earned a total of one million dollars. The second development phase pushed through in 2007. For undisclosed reasons, however, GSK abandoned further development of this drug.
It was Ronald Evans from the Salk Institute who wished to create a drug that can significantly enhance performance and at the same time, in a radical manner, boost the endurance of human beings. In 2004, marathon mice were engineered genetically to display the
PPAR-delta traits in their muscle cells. Upon giving them the developed GW501516, it was found that higher dosage can significantly increase laboratory mice’s endurance.
At this point, you might be wondering how the drug works. According to its creators, the drug is a selective activator or agonist of the receptor called PPAR-delta. It has high potency and affinity for the PPAR-delta. It can efficiently select PPAR-delta over PPAR-alpha and PPAR-gamma.
For rats, the binding between the PPAR-delta and the drug results to the activation of PGC-1a. The complex, in return, turns up to regulate protein expression that is involved in the expenditure of energy. Also, the rats that are treated with the drug have increased the capability to metabolize fatty acid in their skeletal muscles. The rats are likewise protected from the development of type II diabetes and diet-induced obesity. When the drug was used in monkeys, they were noted to lower their levels of VLDL or very low density lipoprotein. Also, an increase in the HDL or the high density lipoprotein is also noted.
Now, you might be asking how GW501516 is used. Basically, there are two main classifications of uses of the drug. The first and the more popular means of utility of this drug is to increase the level of endurance. It is important to note that the GW has already been banned among athletes who are in the professional category. This is due to the fact that the drug can give any athlete an unfair level of advantage over his competition.
Therefore, for people who wish to drastically improve his level of endurance, this drug is clearly one of the best choices. It was also noted that the results are quite quick and the results can be very staggering. Commonly, a dose of 10 milligrams per day can deliver the desired level of increase in endurance.
The second use of GW501516 is for fat loss. A lot of users rely on the drug because it was proven to melt the fat off without being catabolic. This means that you can still hold on to your muscles while losing the layers of fat. This can be further enhanced when used in conjunction with the other drugs.