4-(3-Methylbutoxy)aniline hydrochloride (1:1)

CP-24879 (hydrochloride) is a potent, selective and combined delta5D/delta6D inhibitor. CP-24879 (hydrochloride) 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, and can be used for non-alcoholic steatohepatitis research[1][2].

Signaling Pathways >> Apoptosis >> Ferroptosis

Signaling Pathways >> Others >> Others

Research Areas >> Inflammation/Immunology

IC50: 0.015 μM (delta6D in ABMC-7 cells), 0.56 μM (delta6D in Liver microsomes), 0.67 μM (delta5D in ABMC-7 cells), 3.4 μM (delta5D in ABMC-7 cells)[1]

CP-24879 (hydrochloride) (0-10 μM, 4 days) inhibits Δ6 + Δ5 desaturase activities in a concentration-dependent manner, with a concentration-dependent depletion of AA and decrease in LTC4 production[1]. CP-24879 (hydrochloride) (0-10 μM, 16 h) shows the inhibitory responses on oleic acid-induced triglyceride accumulation in hepatocytes[2]. CP-24879 (hydrochloride) (0-10 μM, 16 h) blocks LPS-induced expression of inflammatory cytokines in a concentration-dependent manner[2]. CP-24879 (hydrochloride) (0-2 μM, 4 h) inhibits desaturase activity and ameliorates ferroptosis[3]. Cell Viability Assay Cell Line: Mouse mastocytoma ABMC-7 cells[1] Concentration: 0, 100 nM, 300 nM, 1 μM, 3 μM, and 10 μM Incubation Time: 4 days Result: Inhibited Δ6 + Δ5 desaturase activities in a concentration-dependent manner, with a concentration-dependent depletion of AA and decrease in LTC4 (Leukotriene C4) production, and did not inhibit either 5-lipoxygenase or LTC4 synthase activity.

CP-24879 (hydrochloride) (3 mg/kg, IP, three times a day, for 6 or 4 days) inhibits Δ6 + Δ5 desaturase activities in vivo, causing depletion of AA in the livers of chow-fed mice and preventing repletion of AA in the livers of EFAD mice[1]. CP-24879 (hydrochloride) (33 mg/kg, IV, once) is cleared quite rapidly and has a relatively short half-life[1]. Animal Model: Chow-fed and EFAD Balb/C mice (N = 5/group) [1] Dosage: 3 mg/kg Administration: IP, three times a day, for 6 or 4 days Result: 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). Animal Model: Swiss-Webster mice (male, 25 g) [1] Dosage: 33 mg/kg Administration: IV in the tail vein, once (Pharmacokinetic Analysis) Result: Was readily distributed to the peripheral tissues, with the volume of distribution (V) of 1.9 mL/g, was cleared quite rapidly (CL = 0.56 mL/min) and had a relatively short half-life (T1/2 = 59 min).

[1]. Obukowicz MG, et al. Identification and characterization of a novel delta6/delta5 fatty acid desaturase inhibitor as a potential anti-inflammatory agent. Biochem Pharmacol. 1998 Apr 1;55(7):1045-58.

[2]. [2]López-Vicario C, et al. Molecular interplay between Δ5/Δ6 desaturases and long-chain fatty acids in the pathogenesis of non-alcoholic steatohepatitis. Gut. 2014 Feb;63(2):344-55.

[3]. [3]Lee JY, Nam M, Son HY, et al. Polyunsaturated fatty acid biosynthesis pathway determines ferroptosis sensitivity in gastric cancer. Proc Natl Acad Sci U S A. 2020;117(51):32433-32442.