产品
编 号:F006032
分子式:C11H18ClNO
分子量:215.72
产品类型
结构图
CAS No: 10141-51-2
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产品详情
生物活性:
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.
体内研究:
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.CP-24879 (hydrochloride) (33 mg/kg, IV, once) is cleared quite rapidly and has a relatively short half-life.Animal Model:Chow-fed and EFAD Balb/C mice (N = 5/group)
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)
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).
体外研究:
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.CP-24879 (hydrochloride) (0-10 μM, 16 h) shows the inhibitory responses on oleic acid-induced triglyceride accumulation in hepatocytes.CP-24879 (hydrochloride) (0-10 μM, 16 h) blocks LPS-induced expression of inflammatory cytokines in a concentration-dependent manner.CP-24879 (hydrochloride) (0-2 μM, 4 h) inhibits desaturase activity and ameliorates ferroptosis.