L-165461

L-165461 is a PPARδ and PPARγ agonist with K_i values of 3 nM and 15 nM, respectively. L-165461 can be used for research on diabetes^[1][2][3]. In Vitro:L-165461 (~16 h) is a potent dual ligand for both PPARγ (K_i = 15 nM) and PPARδ (K_i = 3 nM)^[1].
L-165461 (48 h) acts as an agonist for both hPPARγ and hPPARδ, producing robust transactivation of the UAS reporter gene in COS-1 cells expressing either receptor^[1].
L-165461 binds to and activates the human PPARδ ligand binding domain with an EC₅₀ of 0.012 µM^[3].
L-165461 (4 days) promotes preadipocyte differentiation in 3T3-L1 cells, as measured by aP2 mRNA expression, consistent with its PPARγ binding affinity^[1].
L-165461 (50 μM; 1 h) does not inhibit LPS-induced TNF-α or IL-6 production in freshly isolated or 5-day cultured human monocytes^[2].
L-165461 (50 μM; 1 h) does not inhibit PMA-induced TNF-α or IL-6 production in freshly isolated or 5-day cultured human monocytes^[2].
L-165461 (50 μM; 1 h) does not inhibit LPS-induced TNF-α production in murine RAW 264.7 macrophage-like cells^[2].