描述:AVE-8134 is a potent PPARα agonist, with EC50 values of 100 and 3000 nM for human and rodent PPARα receptor, respectively.
溶解性:DMSO*
体外研究:
AVE8134 is a full PPARα dominated PPAR agonist, but not active on PPARδ. In HUVEC, AVE8134 (1 μM) increases Ser-1177-eNOS phosphorylation but not eNOS expression. In monocytes, AVE8134 (10 μM) increases the expression of CD36 and the macrophage scavenger receptor 1, resulting in enhanced uptake of oxidized LDL.
体内研究:AVE8134 is a full PPARα dominated PPAR agonist, but not active on PPARδ. In HUVEC, AVE8134 (1 μM) increases Ser-1177-eNOS phosphorylation but not eNOS expression. In monocytes, AVE8134 (10 μM) increases the expression of CD36 and the macrophage scavenger receptor 1, resulting in enhanced uptake of oxidized LDL.