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Ki: 6 nM for PPARγ

Peroxisome proliferator-activated receptor (PPARγ) is known to be expressed ubiquitously and involved in lipid and glucose metabolism. Studies have demonstrated that PPARγ is expressed in endothelial cells and plays a potential role in endothelial proliferation and survival. L-165041 is reported as a selective and potent PPARγ ligand.

In vitro: L-165041, which is a selective and potent PPARδligand, displayed in this specified transactivation system, apart from its highly efficacious PPARδ agonist activity, partial and full agonism at, respectively, PPARγ2 and PPARαsubtypes [1].

In vivo: L-165041 could drastically reduce lipid accumulation in the mouse liver, decreasing total hepatic triglyceride and cholesterol content compared to the vehicle group. Gene analysis demonstrated that L-165041 lowered hepatic expression of PPARγ, apolipoprotein B, IL-1β, and interleukin-6. In contrast, L-165041 increased hepatic expressions of PPARδ, lipoprotein lipase, and ATP-binding cassette transporter G1 (ABCG1) [2].

Clinical trial: Up to now, L-165041 is still in the preclinical development stage.

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