CP-24879 hydrochloride|cas:10141-51-2|西域试剂

CP-24879 hydrochloride,98.00%

产品编号：Bellancom-115319| CAS NO：10141-51-2| 分子式：C₁₁H₁₈ClNO| 分子量：215.72

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货号	价格	库存与货期
Bellancom-115319	￥1150.00	杭州北京（现货）
Bellancom-115319	￥1850.00	杭州北京（现货）
Bellancom-115319	￥3500.00	杭州北京（现货）
Bellancom-115319	￥6000.00	杭州北京（现货）
Bellancom-115319	￥9000.00	杭州北京（现货）

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CP-24879 hydrochloride

产品介绍

CP-24879 (hydrochloride) 是一种有效且选择性的 delta5D/delta6D 联合抑制剂。CP-24879 (hydrochloride) 能显著降低肝细胞内脂质积聚和炎症损伤。CP-24879 (hydrochloride) 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。

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
(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.
CP-24879 (hydrochloride) (33 mg/kg, IV, once) is cleared quite rapidly and has a relatively short half-life.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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 (T_1/2 = 59 min).

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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 (T_1/2 = 59 min).

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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 (T_1/2 = 59 min).

性状

Solid

溶解性数据

In Vitro:

DMSO : ≥ 100 mg/mL (463.56 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.6356 mL	23.1782 mL	46.3564 mL
5 mM	0.9271 mL	4.6356 mL	9.2713 mL
10 mM	0.4636 mL	2.3178 mL	4.6356 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (11.59 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (11.59 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (9.64 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (9.64 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明