CP-24879 hydrochloride (CP-24879 HCl), a Δ5D/Δ6D dual-inhibitor, can significantly reduce intracellular lipid accumulation and inflammatory injury in hepatocytes. CP-24879 hydrochloride exhibits superior antisteatotic and anti-inflammatory actions in fat-1 and ω-3-treated hepatocytes.

Δ6D:0.56 μM(Liver microsomes), Δ6D:0.56 μM(ABMC-7 cells), Δ5D:3.4 μM (Liver microsomes), Δ5D:0.67 μM (ABMC-7 cells)

CP-24879 hydrochloride (0-10 μM, 16 h) blocked LPS-induced expression of inflammatory cytokines in a concentration-dependent manner and showed the inhibitory responses on oleic acid-induced triglyceride accumulation in hepatocytes[2]. CP-24879 hydrochloride (0-10 μM, 4 days) inhibited Δ6 + Δ5 desaturase activities in a concentration-dependent manner, with a concentration-dependent depletion of AA and a decrease in Leukotriene C4 (LTC4) production, and did not inhibit either 5-lipoxygenase or LTC4 synthase activity[4].

In Chow-fed and EFAD Balb/C mice, CP-24879 hydrochloride (3 mg/kg, i.p.) inhibited approximately 80% combined Δ6 + Δ5 desaturase activities, causing depletion of AA in the livers of chow-fed mice and preventing repletion of AA in the livers of EFAD mice, and increased OA and LA, with a higher ratio of LA/AA in the livers of mice injected with CP-24879 versus saline (4.70 vs 2.00, Chow-fed mice; 2.46 vs 1.40, EFAD mice; respectively)[4].