Chemical Name: (S)-2-Ethoxy-3-[4-[2-(4-methanesulfonyloxyphenyl)ethoxy]phenyl]propanoic acid
Biological ActivityDual-specificity PPARα/γ agonist (IC50 values are 0.35 and 3.8 μM for PPARγ and PPARα respectively). Prevents atherosclerosis progression in E3L.CETP transgenic mice. Also reduces insulin resistance in obese Zucker rats. Orally active.
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Structure of the PPARβ and -γ ligand binding domain in complex with AZ 242; ligand selectivity and agonist activation in the PPAR family.
Cronet et al.
AZ 242, a novel PPARα/γ agonist with beneficial effects on Ins resistance and carbohydrate and lipid metabolism in ob/ob mice and obese Zucker rats.
Ljung et al.
J.Lipid Res., 2002;43:1855
Synthesis and biological and structural characterization of the dual-acting peroxisome proliferator-activated receptor α/γ agonist ragaglitazar.
Ebdrup et al.
The dual PPARα/γ agonist tesaglitazar blocks progression of pre-existing atherosclerosis in APOE*3Leiden.CETP transgenic mice.
van der Hoorn et al.
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HL-1 cardiomyocytes were incubated with Tesaglitazar (10 µM) for 30 min prior to addition of 15 µM 15d-PGJ2 for 30 min. Preincubation of cells with Tesaglitazar completely abolished activation of p42/44 MAPK indicating involvement of PPAR gamma in cellular signalling in response to 15d-PGJ2.