| Bioactivity | 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]. | ||||||||||||
| Target | 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) | ||||||||||||
| Invitro | 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: | ||||||||||||
| In Vivo | 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: | ||||||||||||
| Name | CP-24879 hydrochloride | ||||||||||||
| CAS | 10141-51-2 | ||||||||||||
| Formula | C11H18ClNO | ||||||||||||
| Molar Mass | 215.72 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [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. |