CP-24879 hydrochloride 是选择性的delta5D/delta6D联合抑制剂。它能显著降低肝细胞内脂质积聚和炎症损伤。它在脂肪-1 和 ω-3 处理的肝细胞中表现出优越的抗脂肪变性和抗炎作用,可用于非酒精性脂肪性肝炎的研究。
产品描述
CP-24879 hydrochloride, 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.
体外活性
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].
体内活性
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].
Cas No.
10141-51-2
分子式
C11H18ClNO
分子量
215.72
别名
CP-24879 HCl;CP-24879 hydrochloride
储存和溶解度
DMSO:55 mg/ml (254.96 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years