2. Metabolic Enzyme/Protease Immunology/Inflammation
  3. Lipoxygenase PGE synthase
  4. 5-LO/mPGES1-IN-1

5-LO/mPGES1-IN-1 (Compound 16) 是一种微粒体前列腺素 E2 合成酶-1 (mPGES-1) 和 5-脂氧合酶 (5-LO) 双重抑制剂，IC50 值分别为 0.3 和 0.4 μM。5-LO/mPGES1-IN-1 具有抗炎活性。

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5-LO/mPGES1-IN-1 Chemical Structure

5-LO/mPGES1-IN-1 Chemical Structure

CAS No. : 1492060-44-2

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规格 价格 是否有货 数量
1 mg ￥1980
3 - 4 周
5 mg 现货 3 - 4 周
10 mg   询价  
50 mg   询价  

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5-LO/mPGES1-IN-1 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

5-LO/mPGES1-IN-1 (Compound 16) is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1) and 5-lipoxygenase (5-LO). IC50 values are 0.3 and 0.4 μM, respectively. 5-LO/mPGES1-IN-1 has anti-inflammatory activity[1].

IC50 & Target

5-LOX

0.4 μM (IC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
0.4 μM
Compound: 16
Inhibition of mPGES-1 from human A549 cell microsomal membranes using PGH2 as substrate incubated 15 mins prior to substrate addition measured after 1 min by RP-HPLC analysis
Inhibition of mPGES-1 from human A549 cell microsomal membranes using PGH2 as substrate incubated 15 mins prior to substrate addition measured after 1 min by RP-HPLC analysis
[PMID: 24171493]
A549 IC50
0.4 μM
Compound: 13
Inhibition of mPGES-1 in human A549 cells microsomes assessed as reduction in PGE2 formation by RP-HPLC assay
Inhibition of mPGES-1 in human A549 cells microsomes assessed as reduction in PGE2 formation by RP-HPLC assay
[PMID: 25037914]
COS-7 EC50
1.3 μM
Compound: 13
Activation of human PPARgamma ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
Activation of human PPARgamma ligand binding domain expressed in COS7 cells by luciferase reporter gene assay
[PMID: 25037914]
PMNL IC50
0.2 μM
Compound: 13
Inhibition of 5-LOX in human PMNL cells assessed as reduction in 5-LOX product formation pre-incubated for 15 mins by HPLC method
Inhibition of 5-LOX in human PMNL cells assessed as reduction in 5-LOX product formation pre-incubated for 15 mins by HPLC method
[PMID: 25037914]
PMNL IC50
0.3 μM
Compound: 13
Inhibition of 5-LOX in human PMNL cells assessed as reduction in 5-LOX product formation pre-incubated for 15 mins by HPLC based cell-free assay
Inhibition of 5-LOX in human PMNL cells assessed as reduction in 5-LOX product formation pre-incubated for 15 mins by HPLC based cell-free assay
[PMID: 25037914]
体内研究
(In Vivo)

5-LO/mPGES1-IN-1 (10 mg/kg, 腹腔注射, 腹膜炎诱导前 30 分钟预处理) 在 zymosan 诱导的小鼠腹膜炎模型中，可降低血管通透性和炎症细胞浸润，并伴有半胱氨酸-白三烯和前列腺素 E2 水平受损[1]。

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

Animal Model: Zymosan-Induced Peritonitis in Mice[1]
Dosage: 10 mg/kg
Administration: i.p. pretreated 30 minutes before peritonitis induction
Result: Reduced vascular permeability by 57% and inhibited neutrophil infiltration by 45%.
分子量

513.07

Formula

C25H25ClN4O2S2
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

5-LO/mPGES1-IN-1 相关分类

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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.

Keywords:

5-LO/mPGES1-IN-11492060-44-2LipoxygenasePGE synthaseLOXProstaglandin E synthase5-LOmPGES-1InhibitorZymosan-Induced Peritonitis in MiceAnti-inflammatoryinhibitorinhibit

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产品名称：
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目录号：
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