Selective Androgen Receptor Sarm gw-501516 for Bodybuilding CAS
GW501516 (also known as GW-501,516, GW1516, GSK-516) is a PPAR&
receptor agonist that was invented in a collaboration between
Ligand Pharmaceuticals and GlaxoSmithKline in the 1990s, was
entered into clinical development as a drug candidate for metabolic
diseases and cardiovascular diseases, and was abandoned in 2007
because animal testing showed that the drug caused cancer to
develop rapidly in several organs.
GW501516 is a selective agonist (activator) of the PPARδ receptor.
It displays high affinity (Ki = 1 nM) and potency (EC50 = 1 nM) for
PPARδ with > 1000 fold selectivity over PPARα and PPARγ.
In rats, binding of GW501516 to PPARδ recruits the co activator
PGC-1a. The PPARδ/coactivator complex in turn up regulates the
expression of proteins involved in energy expenditure. Furthermore
in rats treated with GW501516, increased fatty acid metabolism in
skeletal muscle and protection against diet-induced obesity and
type II diabetes was observed.
In obese rhesus monkeys, GW501516 increased high-density
lipoprotein (HDL) and lowered very-low-density lipoprotein (VLDL).
The mechanism by which PPARδ agonists increase HDL appears to be a
result of increased expression of the cholesterol transporter ABCA1
The regular dosage of Cardarine is 10 to 20 mg per day. 10 mg a day
is aimed for endurance, and the higher the dosage the greater the
fat loss benefits are going to be.
Expect to experience more intense endurance and fat burning when
taking 20 mgs, but you never want to take much more than that.
You can take it once a day or split the dosage (in the AM and PM).
GW 501516 is best taken 30-45 minutes before a workout. You'll feel
the difference the first time you take it.