GW501516

説明

GW501516, also known as GW-1516 or cardarine and endurobol, is a peroxisome proliferator-activated receptor delta (PPAR-δ) agonist. Activation of the receptor will increase fat-burning capacity and muscle production, as it changes the body's fuel preference from glucose to lipids.

化学的特性

White Solid

来歴

GW501516, also known as Cardarine, was originally discovered in the early 1990s during a research collaboration between two large pharmaceutical companies. The initial proposed use was for the treatment of hyperlipidemia (elevated fats in the blood), though later studies looked at its effectiveness for treating obesity, diabetes, and cardiovascular disease.

使用

An experimental drug meant to control lipids and increase the level of HDL, or good cholesterol, in the bloodstream. A cell-permeable, thiazolyl compound that acts as a potent, high affinity, PPARd agonist. Exhibits selectivity for PPARd compared t

定義

ChEBI: An aromatic ether that is phenoxyacetic acid in which the phenyl group is substituted at position 2 by a methyl group and at position 4 by a (1,3-thiazol-5-ylmethyl)sulfanediyl group, and in which the 1,3-thiazolyl group is substituted at positions 2 and 4 by p-trifluoromethylphenyl and methyl groups, respectively.

一般的な説明

GW501516 is the most selective and potent PPARβ (EC50=1.1nM) agonist that has been demonstrated to be 1,000-fold more selective in comparison to existing subtypes. It can regulate expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells and has been shown to block insulin resistance and fatty acid-induced nuclear factor-κB (NF-κB) activation.

生物活性

GW 501516 is a potent and selective PPARδ agonist (EC50 = 1.2 nM). Displays <1000-fold selectivity over other PPAR subtypes. Increases ABC A1 transporter expression and induces apolipoprotein A1-mediated cholesterol efflux in vitro. Also increase serum HDL cholesterol and lowers small, dense LDL levels in obesity in vivo models.

作用機序

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 > 1,000 fold selectivity over PPARα and PPARγ.In rats, binding of GW501516 to PPARδ recruits the coactivator PGC-1α. The PPARδ/coactivator complex in turn upregulates the expression of proteins involved in energy expenditure.[31] 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).