2. Metabolic Enzyme/Protease GPCR/G Protein
  3. Lipoxygenase Leukotriene Receptor
  4. CGS 23885

CGS 23885 是一种具有口服活性的 5-脂氧合酶 (5-lipoxygenase) 抑制剂。CGS 23885 可减少 5-羟基二十碳四烯酸 (5-hydroxyeicosatetraenoic acid)、LTB4 以及 LT C4/D4/E4 的生成。CGS 23885 可抑制大鼠胸膜炎中的细胞浸润。CGS 23885 可用于胸膜炎相关研究。

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CGS 23885

CGS 23885 Chemical Structure

CAS No. : 134822-78-9

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CGS 23885 相关抗体

Top Publications Citing Use of Products

查看 Lipoxygenase 亚型特异性产品:

查看所有亚型
5-LOX 12-LOX 15-LOX

查看 Leukotriene Receptor 亚型特异性产品:

查看所有亚型
LTB4 LTC4/CysLT2 LTD4/CysLT1 LTE4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CGS 23885 is an orally active 5-lipoxygenase (5-lipoxygenase) inhibitor. CGS 23885 reduces the production of 5-hydroxyeicosatetraenoic acid (5-hydroxyeicosatetraenoic acid), LTB4, and LTC4/D4/E4. CGS 23885 inhibits cell infiltration in rat pleurisy. CGS 23885 can be used in pleurisy-related research[1][2].

IC50 & Target[1]

LTB4

 

5-LOX

 

体外研究
(In Vitro)

CGS 23885 (Compound 43) 可强效抑制豚鼠多形核白细胞 (PMNs) 中的 5-脂氧合酶活性，其抑制 5-HETE 生成的 IC50 值为 43 nM，抑制 LTB4 生成的 IC50 值为 48 nM[1]。
CGS 23885 可微弱抑制羊精囊环氧合酶，其 IC50 为 36 μM，对 5-脂氧合酶表现出高选择性[1]。
CGS 23885 可中度抑制人血小板 12-脂氧合酶，其 IC50 为 0.64 μM[1]。
CGS 23885 可抑制犬全血中的 5-脂氧合酶活性，其 IC50 为 0.11 μM[1]。
CGS 23885 可抑制人全血中 5-脂氧合酶的活性，其 IC50 为 0.89 μM[1]。

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

CGS 23885 相关抗体:
体内研究
(In Vivo)

CGS 23885 (1-30 mg/kg；口服；角叉菜胶注射前 1 小时及 A23187 注射前 1 小时给药) 可在大鼠胸膜炎模型中剂量依赖性地抑制 A23187 (HY-N6687) 诱导的 LTB4 和 LTC4/D4/E4 的生物合成，且胸膜腔积液中的药物浓度与 LTB4 抑制作用呈强正相关 (IC50 = 21 ng/mL)[2]。

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

Animal Model: Sprague-Dawley rats (male, 220-235 g, pleurisy induced by intrapleural κ-carrageenan and calcium ionophore A23187)[2]
Dosage: 1 mg/kg; 3 mg/kg; 10 mg/kg; 30 mg/kg
Administration: p.o.; 1 h before carrageenan injection and 1 h before A23187 injection
Result: Inhibited A23187-enhanced LTB4 biosynthesis by 32% and LTC4/D4/E4 biosynthesis by 4% at 1 mg/kg.
Inhibited A23187-enhanced LTB4 biosynthesis by 73% and LTC4/D4/E4 biosynthesis by 33-35% at 3 mg/kg.
Inhibited A23187-enhanced LTB4 biosynthesis by 93% and LTC4/D4/E4 biosynthesis by 52-67% at 10 mg/kg.
Inhibited A23187-enhanced LTB4 biosynthesis by 97% and caused a 24% significant reduction in total cellular influx at 30 mg/kg.
Showed a positive correlation between pleural fluid concentration and inhibition of LTB4 biosynthesis, with an IC50 of 21 ng/mL for LTB4 inhibition.
Produced no significant effect on exudate volume, PGE2 levels, or TXB2 levels at all doses; no significant effect on total cellular influx at 1, 3, 10 mg/kg.
分子量

312.32

Formula

C17H16N2O4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

CGS 23885 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CGS 23885134822-78-9CGS23885CGS-23885LipoxygenaseLeukotriene ReceptorLOXdog5-lipoxygenaseleukotriene B4human5-hydroxyeicosatetraenoic acid12-lipoxygenasesheep cyclooxygenaseleukotriene C4/D4/E4guinea pigcarrageenan-induced rat pleurisyInhibitorinhibitorinhibit

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