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Chemical Name:2-[[4-[2-[[(Cyclohexylamino)carbonyl](4-cyclohexylbutyl
)amino]ethyl]phenyl]thio]-2-methylpropanoic acid
Biological Activity:
Potent
and highly selective PPARα agonist (EC50 values are
6, 1100 and 6200 nM for human PPARα, PPARγ and PPARδ receptors respectively). Modulates
oleate metabolism and mitochondrial enzyme gene expression in mature myotubules
in vitro. Has lipid-lowering effects following oral administration in vivo.
Brownet al (2001) Identification
of a subtype selective human PPARα agonist through parallel-array synthesis.
Bioorg.Med.Chem.Lett. 11 1225. Cunardet al (2002)
Regulation of cytokine expression by ligands of peroxisome proliferator
activated receptors. J.Immunol. 168 2795. Muoioet al
(2002) Peroxisome proliferator-activated receptor-α regulates fatty acid utilization in
primary human skeletal muscle cells. Diabetes 51 901.
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