| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S89801-5mg买3赠1 |
98.10% | ￥860.00 |
6 | - | - | - | - |
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S89801-10mg买3赠1 |
98.10% | ￥1380.00 |
7 | - | - | - | - |
|
S89801-25mg买3赠1 |
98.10% | ￥2620.00 |
5 | - | - | - | - |
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| 产品描述： | 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 | ||||||||||||||||||||
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| 靶点： | 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) | ||||||||||||||||||||
| 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. 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. | ||||||||||||||||||||
| 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). | ||||||||||||||||||||
| 参考文献： | 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. 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. | ||||||||||||||||||||
| 溶解性： | soluble in DMSO | ||||||||||||||||||||
| 保存条件： | 2-8℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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