Seladelpar sodium salt (MBX-8025) is an orally active, effective and specific PPARδ agonist with an EC 50 of 2 nM which exhibiting more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively.

PPARδ:2 nM （EC50）

MBX-8025 is an orally active, potent (EC 50 =2 nM), and specific (750-fold and 2500-fold more potent than PPARα or PPARγ receptors, respectively) PPARδ agonist in development as a lipid-altering agent [2] [3].

In atherogenic diet-fed Wt mice, administration of Seladelpar sodium salt reduces body weight by ~18% (P<0.05). On the contrary, Seladelpar sodium salt produces minimal effect on body weight in atherogenic diet-fed foz/foz mice. Seladelpar sodium salt reduces serum alanine aminotransferase (ALT) levels in foz/foz mice (P<0.05) and similarly (but not significantly) in Wt mice. Seladelpar sodium salt normalizes serum cholesterol and decreases triglycerides in both genotypes (P<0.05). Seladelpar sodium salt abolishes hepatocyte ballooning (P<0.05) and decreases the nonalcoholic fatty liver disease (NAFLD) activity score by ~50%. Seladelpar sodium salt also significantly reduces sirius red-positive areas in foz/foz mice (P<0.05) [4].