CP-24879 hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

CP-24879 盐酸盐是一种 Δ5D/Δ6D 双抑制剂，可显着减少肝细胞内脂质积累和炎症损伤。 CP-24879 盐酸盐在 fat-1 和 ω-3 处理的肝细胞中表现出优异的抗脂肪变性和抗炎作用。

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.(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. 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.(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).

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. Cell Viability Assay Cell Line:Mouse mastocytoma ABMC-7 cells 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. 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).

CP24879 hydrochloride | CP 24879 hydrochloride | CP-24879 HCl

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Other Targets

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10141-51-2

215.72

C11H18ClNO

>98% (HPLC)

In Vitro:?DMSO : ≥ 100 mg/mL (463.56 mM)

Cl.CC(C)CCOc1ccc(N)cc1

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(-20℃)

With Ice Pack

≥ 2 years