1. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  2. Epoxide Hydrolase Reactive Oxygen Species (ROS) Interleukin Related NF-κB
  3. sEH-IN-23

sEH-IN-23 是一种可溶性环氧化物水解酶抑制剂,其对人源的 IC50 为 0.8 nM,对鼠源的 IC50 为 0.7 nM。sEH-IN-23 可抑制 NF-κB 激活介导的炎症因子生成、活性氧 (ROS) 产生、促炎细胞因子 IL-1βIL-6TNF-α 的释放。sEH-IN-23 在急性肺损伤模型中表现出抗炎活性。sEH-IN-23 可用于急性肺损伤的研究。

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sEH-IN-23

sEH-IN-23 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

sEH-IN-23 is a soluble epoxide hydrolase inhibitor with a IC50 of 0.8 nM against human sEH and 0.7 nM against murine sEH. sEH-IN-23 inhibits inflammatory factor production mediated by NF-κB activation, reactive oxygen species (ROS) generation, and the release of pro-inflammatory cytokines IL-1β, IL-6 and TNF-α. sEH-IN-23 exhibits anti-inflammatory activity in acute lung injury models. sEH-IN-23 can be used for the research of acute lung injury[1].

IC50 & Target[1]

EH1

 

IL-6

 

IL-1β

 

体外研究
(In Vitro)

sEH-IN-23 (compound 20K) (100 μg/mL; 0-60 min) 在体外大鼠肝微粒体稳定性试验中的半衰期为 189.00 min[1]
sEH-IN-23 (12.5-100 μM; 48 h) 在 CCK-8 实验中孵育 48 h 后,可使 RAW264.7 巨噬细胞的存活率维持在 75%以上[1]
sEH-IN-23 (10-20 μM; 1-2 h pre-incubation) 可呈剂量依赖性抑制 LPS (HY-D1056) 诱导的 M1 型极化,减少 IL-6 和 TNF-α 的释放,并可降低 RAW264.7 巨噬细胞的 ROS 生成[1]

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

Cell Viability Assay[1]

Cell Line: RAW264.7 macrophages
Concentration: 12.5, 25, 50, 100 μM
Incubation Time: 48 h
Result: Maintained cell viability higher than 75% at all tested concentrations.
药代动力学
(Parmacokinetics)
Species Dose Route Tmax Cmax T1/2 CL Vz AUC0-12 AUC0-∞ F
Rat[1] 8 mg/kg i.v. 0.12 h 14.38 μM 9.77 h 0.33 L/h 4.68 L 12.11 μM·h 24.07 μM·h 125.9 %
Rat[1] 50 mg/kg i.p. 3.00 h 35.35 μM 1.09 h 0.27 L/h 0.44 L 186.87 μM·h 189.49 μM·h /
体内研究
(In Vivo)

sEH-IN-23 (15-30 mg/kg;腹腔注射;每日 1 次;连续 5 天) 在 LPS (HY-D1056) 诱导的急性肺损伤小鼠模型中表现出剂量依赖性的抗炎和抗氧化活性[1]
sEH-IN-23 (2 g/kg;口服;每日;连续 14 天) 在小鼠中具有良好的耐受性,在监测指标或主要器官组织病理学中未观察到毒性[1]

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

Animal Model: C57BL/6 (male, 20-22 g, intraperitoneal injection of LPS)[1]
Dosage: 15 mg/kg; 30 mg/kg
Administration: i.p.; once daily; 5 consecutive days
Result: Reduced lung histopathology scores.
Alleviated alveolar obstruction, alveolar wall thickening, and neutrophil exudation in lung tissue.
Inhibited serum inflammatory cytokines in a dose-dependent manner, reduced levels of IL-1β, IL-6, and TNF-α.
Reduced CD68-positive macrophage infiltration in lung tissue.
Inhibited LPS-induced nuclear translocation of p65 (NF-κB pathway component) in lung tissue and in F4/80-marked lung macrophages.
Reduced lung tissue myeloperoxidase (MPO) activity in a dose-dependent manner.
Reduced reactive oxygen species (ROS) levels in lung tissue.
分子量

514.88

Formula

C22H22ClF3N4O5

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
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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:
sEH-IN-23
目录号:
HY-182283
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