Wy-14643 is a selective PPARα agonist with EC50 values of 5μM and 0.63μM for human and murine PPARα, also exhibited less potency to human PPARγ/δwith IC50 values of 60 and 35μM, respectively, and murine PPARγ with IC50 value of 32μM in cell-based transactivation assays. Wy-14643 has been developed as hypolipidemic agents through optimization of their lipid-lowering activity in rodents[1]. Wy-14643 induced expression of UCP3 in rat neonates[2]. Oral administration of Wy-14643 0.1% in diet for 10 days in high-fat-diet mice or chow-fed foz/foz mice reduced steatosis in nonalcoholic steatohepatitis and simple steatosis livers and fewer inflammatory foci, with hepatoprotection against ischemia–reperfusion injury by alanine aminotransferase release. The reduction of hepatic VCAM-1 and ICAM-1 expression, IL-1α, TNF-α, IL-12 and activated NF-κB, p38, IL-6 production and cell cycle entry observed[4].
Activation of human PPARalpha ligand binding domain expressed in COS7 cells by luciferase reporter gene assay, IC50=36.3 μM
25037914
EAhy926 cells
10 uM
Function assay
12 h
Inhibition of tube formation in human EAhy926 cells at 10 uM pre-incubated for 12 hrs measured after 24 hrs by phase-contrast microscopy
19036594
HEK293 cells
Function assay
Agonist activity at human PPARalpha expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay, EC50=23.33 μM
23265844
Hep G2 cells
Function assay
Agonist activity at mouse PPARalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay, EC50=0.04 μM
Activation of human PPARalpha ligand binding domain expressed in COS7 cells by luciferase reporter gene assay, IC50=36.3 μM
25037914
EAhy926 cells
10 uM
Function assay
12 h
Inhibition of tube formation in human EAhy926 cells at 10 uM pre-incubated for 12 hrs measured after 24 hrs by phase-contrast microscopy
19036594
HEK293 cells
Function assay
Agonist activity at human PPARalpha expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay, EC50=23.33 μM
23265844
Hep G2 cells
Function assay
Agonist activity at mouse PPARalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay, EC50=0.04 μM
19053776
HepaR cells
25 μM
Function assay
1 day
Agonist activity at PPARalpha in human HepaR cells assessed as increase in HMGCS2 gene expression at 25 uM incubated for 1 day by quantitative PCR method relative to untreated control
25497132
MCF7 cells
Function assay
Agonist activity at human PPARalpha expressed in MCF7 cells co-transfected CPTI DR1-type RE after 6 hrs by luciferase reporter gene assay, EC50=0.542 μM
24936232
mouse NIH3T3 cells
0.1-10 μM
Function assay
Transactivation of mouse recombinant PPARalpha expressed in mouse NIH3T3 cells at 0.1 uM to 10 uM by PPRE activation based dual luciferase reporter gene assay relative to control
19237283
U2OS cells
Function assay
Agonist activity at human PPARalpha in U2OS cells by transactivation assay, EC50=12 μM
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