tcsc0040410 Seladelpar sodium salt

Seladelpar sodium salt (MBX-8025) is an orally active, potent and specific PPARδ agonist with an EC₅₀ of 2 nM, showing more than 750-fold and 2500-fold selectivity over the PPARα and PPARγ receptors, respectively.

IC50 & Target: EC50: 2 nM (PPARδ)^[1][2]

In Vitro: MBX-8025 is an orally active, potent (EC₅₀=2 nM), and specific (750-fold and 2500-fold compared with PPARα or PPARγ receptors, respectively) PPARδ agonist being developed as a lipid-altering agent^[2][3].

In Vivo: In atherogenic diet-fed Wt mice, administration of Seladelpar sodium salt reduces body weight by ~18% (P<0.05). In contrast, Seladelpar sodium salt produces minimal effect on body weight in atherogenic diet-fed foz/foz mice. Seladelpar sodium salt lowers 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].