| Description | 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. |
| In vitro | 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 vivo | 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]. |
| Target activity | 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) |
| Synonyms | CP-24879 HCl |
| molecular weight | 215.72 |
| Molecular formula | C11H18ClNO |
| CAS | 10141-51-2 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 55 mg/ml (254.96 mM) |
| References | 1. Simón MV, et al. Synthesis of docosahexaenoic acid from eicosapentaenoic acid in retina neurons protects photoreceptors from oxidative stress. J Neurochem. 2016 Mar;136(5):931-46. 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. 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. 4. 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. |