1. Metabolic Enzyme/Protease GPCR/G Protein
  2. Lipoxygenase Leukotriene Receptor
  3. 5-LOX-IN-6

5-LOX-IN-6 (compound 11a) 是一种 5-lipoxygenase (5-LO) 的直接可逆抑制剂。5-LOX-IN-6 抑制人中性粒细胞和重组人 5-LO 中的 5-LO 活性,IC50 值分别为 0.23 和 0.086 µM。5-LOX-IN-6 阻止白三烯生物合成。5-LOX-IN-6 可用于炎症和过敏性疾病研究。

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5-LOX-IN-6 Chemical Structure

5-LOX-IN-6 Chemical Structure

CAS No. : 1159576-98-3

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1 mg ¥1440
3 - 4 周
5 mg ¥5850
3 - 4 周
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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

5-LOX-IN-6 (compound 11a) is a direct and reversible inhibitor of 5-lipoxygenase (5-LO). 5-LOX-IN-6 inhibits 5-LO activity in human neutrophils and recombinant human 5-LO with IC50 values of 0.23 and 0.086 µM, respectively. 5-LOX-IN-6 prevents leukotriene biosynthesis. 5-LOX-IN-6 can be used for inflammatory and allergic disorders research[1].

IC50 & Target

5-LO

 

LTB4

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.6 μM
Compound: S17
Inhibition of mPGES-1 in IL-1beta-stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 formation incubated for 15 mins using PGH2 substrate by RP-HPLC method
Inhibition of mPGES-1 in IL-1beta-stimulated human A549 cell microsomal membranes assessed as reduction in PGE2 formation incubated for 15 mins using PGH2 substrate by RP-HPLC method
[PMID: 26088337]
A549 IC50
2 μM
Compound: 7a
Inhibition of mPGES1 in IL1-beta induced human A549 cells assessed as PGE2 production preincubated for 10 mins
Inhibition of mPGES1 in IL1-beta induced human A549 cells assessed as PGE2 production preincubated for 10 mins
[PMID: 19884011]
体外研究
(In Vitro)

5-LOX-IN-6 (compound 11a) (0-10 µM) 可有效阻断人全血测定中 5-LO 产物的形成 (IC50=0.83-1.6 µM)[1]
5-LOX-IN-6 (0-10 µM) 无法阻断 A23187 (HY-N6687,2.5 µM) 诱导的中性粒细胞中 5-LO 易位[1]

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

体内研究
(In Vivo)

5-LOX-IN-6 (compound 11a) (4 mg/kg,腹腔注射)可显著阻止 λ-carrageenan (HY-N9470) 治疗的大鼠胸腔渗出物中白三烯 B4 的产生,胸膜炎严重程度降低[1]

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

Animal Model: Male Wistar Han rats (220-230 g, n=10 per group)[1]
Dosage: 4 mg/kg
Administration: IP, 30 min before λ-carrageenan administration. Rats were anaesthetized and λ-carrageenan (HY-N9470) was injected into the pleural cavity.
Result: significantly reduced the inflammatory reaction measured as exudate volume (77%), inflammatory cell numbers (40%), and LTB4 levels (49%) in the pleural exudates.
分子量

379.84

Formula

C22H18ClNO3

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
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  • 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.

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产品名称:
5-LOX-IN-6
目录号:
HY-120502
需求量: