PPARβ/δ Activator

Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC₅₀ of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research.

9 (10)-Nitrooleate (9(10)-Nitrated oleic acid) is an endogenous lipid signaling mediator with vasoprotective effects. 9 (10)-Nitrooleate enhances enzymatic activity and improves nitric oxide bioavailability by inducing phosphorylation of Akt and ERK1/2, regulating the multi-site phosphorylation status of eNOS and optimizing its interaction with Hsp90. 9 (10)-Nitrooleate also activates PPARα, PPARδ and PPARγ receptors, thereby regulating adipogenesis, glucose uptake and inflammation-related gene expression, and exhibits immunosuppressive effects by inhibiting neutrophil migration and cytokine secretion. 9 (10)-Nitrooleate is widely used in studies of sepsis and related inflammatory diseases.

E0924G is an orally active activator for PPARδ with EC₅₀ of 2.82 μM. E0924G promotes the upregulation of osteoprotegerin (OPG) with an EC₅₀ of 0.29 μM. E0924G reduces RANKL-induced osteoclast differentiation and inhibites F-actin ring formation in RAW264.7 macrophages. E0924G regulates the bone density and bone loss in ovariectomized (OVX) and age-related osteoporosis models.