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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, PPARδ agonist. Exhibits selectivity for PPARδ compared to PPARα and PPARγ. Does not exibit any activity against other nuclear or non-nuclear receptors. Reported to increase cholesterol efflux and ABAC1 expression in macrophages, fibroblasts, and intestinal cells.

Agonist of peroxisome proliferator-activated receptor δ/β (PPARδ/β). The compound activates the nuclear receptor PPARδ downstream signalling and affects hepatic AMPK levels. It boosts the activity of the lipin 1-PPARα-PPARγ coactivator 1 (PGC-1)-α pathway and increases hepatic fatty acid oxidation. It was reported that GW 501516 prevents high-fat diet induced hypertriglyceridemia. 

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. Studies demonstrate that GW501516 can regulate expression of genes involved in lipid catabolism and energy uncoupling in skeletal muscle cells. Additionally, GW501516 has been shown to block insulin resistance and fatty acid-induced nuclear factor-κB (NF-κB) activation.