2. Metabolic Enzyme/Protease Immunology/Inflammation
  3. Epoxide Hydrolase FLAP
  4. sEH/FLAP-IN-2

sEH/FLAP-IN-2 是一种选择性 sEH (IC50 = 12.6 nM)/FLAP 双重抑制剂。sEH/FLAP-IN-2 可显著减少 5-LOX/FLAP 和 sEH 衍生的脂质体，从而促进脂质体的重新分布。sEH/FLAP-IN-2 可用于腹膜炎的研究。

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sEH/FLAP-IN-2

sEH/FLAP-IN-2 Chemical Structure

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sEH/FLAP-IN-2 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

sEH/FLAP-IN-2 is a selective sEH (IC50 = 12.6 nM)/FLAP dual inhibitor. sEH/FLAP-IN-2 highlights the reduction of 5-LOX/FLAP- and sEH-derived LMs, resulting in a favourable redistribution of LMs. sEH/FLAP-IN-2 can be used for the study of peritonitis[1].

体外研究
(In Vitro)

sEH/FLAP-IN-2 (Compound 6) 对 5-LOX 无显著抑制活性，IC50 值 >10 μM[1]。
在人中性粒细胞中，sEH/FLAP-IN-2 (10 μM，15 分钟) 在 FLAP 依赖性系统中，在无外源性花生四烯酸 (AA) 的情况下，显著抑制 5-LOX 产物 (LTB4、反式-LTB4 和 5-HETE) 的生成，残余活性为 35.7%；在存在外源性 AA 的情况下，其抑制活性减弱 (IC50 > 10 μM)[1]。
sEH/FLAP-IN-2 (0.1-10 μM，16 分钟) 对 COX-1、COX-2 和 mPGES-1 的活性无显著影响[1]。
sEH/FLAP-IN-2 (0.1-10 μM，120 分钟) 浓度依赖性地抑制 5-LOX/FLAP 衍生的介质 (如 LTB4 和 LTC4) ，尤其是在 M1-MDM 中；同时，它增加 COX 衍生的前列腺素 (如 PGE2 和 PGD2)，但不影响 SPM (如 RvD5) 的水平[1]。

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

sEH/FLAP-IN-2 相关抗体:
体内研究
(In Vivo)

sEH/FLAP-IN-2 (Compound 6) (10 mg/kg，腹腔注射，一次) 通过双重抑制 FLAP 和 sEH，有效调节小鼠腹膜炎模型中的脂质介质谱，使脂质介质谱从促炎状态 (LTs 和 DHETs) 转变为抗炎状态 (EETs)[1]。

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

Animal Model: CD-1 mice (33-39 g, 8 weeks old) were given an acute inflammatory response via intraperitoneal injection of Zymosan (HY-159069) (1 mg/mouse)[1].
Dosage: 10 mg/kg
Administration: I.p., once, 30 mins before zymosan
Result: Significantly reduced zymosan-induced levels of pro-inflammatory mediators, including LTB4, 5-HETE, and LTE4.
Increased levels of anti-inflammatory EETs (particularly 11,12-EET and 14,15-EET) while decreasing levels of pro-inflammatory DHETs (such as 11,12-DHET), resulting in an elevated EET/DHET ratio.
PGE2 levels were significantly reduced, but TXB2 was unaffected.
分子量

447.57

Formula

C26H33N5O2
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

sEH/FLAP-IN-2 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:

sEH/FLAP-IN-2Epoxide HydrolaseFLAP5-lipoxygenase-activating protein5-LO activating proteinsEHsoluble epoxide hydrolaseInhibitorinhibitorinhibit

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