2. Neuronal Signaling Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation
  3. Cholinesterase (ChE) Epoxide Hydrolase TNF Receptor Interleukin Related
  4. sEH/AChE-IN-5

sEH/AChE-IN-5 是一种具有选择性、口服活性且可穿透血脑屏障的乙酰胆碱酯酶 (AChE) 和可溶性环氧化物水解酶 (sEH) 双重抑制剂，其 IC50 值分别为 1.7 nM 和 0.7 nM。sEH/AChE-IN-5 可通过降低 TNF-α、IL-1β、IL-6、iNOS 水平发挥神经保护和抗炎作用。sEH/AChE-IN-5 可改善东莨菪碱 (HY-N0296) 诱导的小鼠学习记忆障碍。sEH/AChE-IN-5 可用于阿尔茨海默病的研究。

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sEH/AChE-IN-5

sEH/AChE-IN-5 Chemical Structure

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sEH/AChE-IN-5 相关抗体

Top Publications Citing Use of Products

查看 Cholinesterase (ChE) 亚型特异性产品:

查看所有亚型
AChE BChE

查看 TNF Receptor 亚型特异性产品:

查看所有亚型
TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

查看 Interleukin Related 亚型特异性产品:

查看所有亚型
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

sEH/AChE-IN-5 is a selective, orally active and brain-penetrant acetylcholinesterase (AChE) and soluble epoxide hydrolase (sEH) dual inhibitor with IC50 values of 1.7 nM and 0.7 nM. sEH/AChE-IN-5 mediates neuroprotection and anti-inflammation via reduced TNF-α, IL-1β, IL-6, iNOS. sEH/AChE-IN-5 improves Scopolamine (HY-N0296)-induced learning and memory deficits mice. sEH/AChE-IN-5 can be used for the research of Alzheimer's disease[1].

IC50 & Target[1]

AChE

1.7 nM (IC50)

sEH

0.7 nM (IC50)

IL-1β

 

IL-6

 

体外研究
(In Vitro)

sEH/AChE-IN-5 (Compound z43) 可强效抑制重组人乙酰胆碱酯酶 (hAChE)，其 IC50 为 1.7 nM；同时可抑制人丁酰胆碱酯酶 (hBuChE)，IC50 为 942.0 nM[1]。
sEH/AChE-IN-5 可强效抑制重组 hsEH，其 IC50 为 0.7 nM[1]。
sEH/AChE-IN-5 (20 μM; 48 h) 在 HepG2、SMMC7721 和 SH-SY5Y 细胞系中表现出低细胞毒性，其 IC50 值分别为 82.27 μM、>100 μM 和 >20 μM[1]。
sEH/AChE-IN-5 (1.25-20 μM) 在浓度高达 20 μM 时，对 PC12 和 BV-2 细胞系无显著细胞毒性[1]。
sEH/AChE-IN-5 (5-20 μM; 26 h) 可保护 PC12 细胞免受 H2O2 诱导的毒性，在 5 μM 浓度下以剂量依赖方式使细胞存活率提升 20% 以上[1]。
sEH/AChE-IN-5 (5-20 μM; 预处理 1 小时) 可剂量依赖性降低 LPS (HY-D1056) 诱导的 BV-2 细胞中 TNF-α、IL-1β、IL-6 和 iNOS 水平，在 20 μM 时可将炎症因子水平恢复至接近正常水平[1]。
sEH/AChE-IN-5 不抑制 CYP1A2，对 CYP2C9、CYP2C19 和 CYP2D6 表现出中度抑制作用，对 CYP3A4 具有强抑制作用 (IC50 = 0.324 μM)，且经 PAMPA 实验检测显示出较高的血脑屏障通透性 (Pe = 3.33 × 10-6 cm/s)[1]。
sEH/AChE-IN-5 在人、犬血浆中表现出较高的血浆蛋白结合率，所有受试物种的结合率均超过 99.9%[1]。

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

sEH/AChE-IN-5 相关抗体:

ELISA Assay[1]

Cell Line: BV-2 cells
Concentration: 5, 10, 20 μM
Incubation Time: 1 h pretreatment before LPS
Result: Does-dependently reduces LPS-induced TNF-α, IL-1β, IL-6.
Restored inflammatory factor levels to near normal at 20 μM.
体内研究
(In Vivo)

sEH/AChE-IN-5 (Compound z43) (5-30 mg/kg；灌胃；每日给药；11天) 可剂量依赖性地改善 Scopolamine (HY-N0296) 诱导的雄性 ICR 小鼠学习记忆障碍[1]。
sEH/AChE-IN-5 (30-1200 mg/kg；灌胃) 在雌性昆明小鼠中显示出良好的急性安全性，未观察到器官毒性或不良事件[1]。

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

Animal Model: Alzheimer's disease ICR mice (male, 3-4 weeks old, 18-22 g, Scopolamine-induced cognitive impairment)[1]
Dosage: 5 mg/kg; 10 mg/kg; 30 mg/kg
Administration: I.g.; daily; 11 days
Result: Increased Scopolamine-reduced spontaneous alternation rate from 42.28% to 55.93% (5 mg/kg), 56.79% (10 mg/kg), and 59.35% (30 mg/kg) in the Y-maze test.
Maintained stable total arm entries across all groups, indicating no motor impairment.
Increased Scopolamine-reduced discrimination index from 11.80% to 21.62% (5 mg/kg), 23.82% (10 mg/kg), and 27.99% (30 mg/kg) in the novel object recognition test.
Reversed Scopolamine-elevated brain acetylcholinesterase activity in a dose-dependent manner.
分子量

660.09

Formula

C34H29ClF3N7O2
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/AChE-IN-5 相关分类

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

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浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
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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/AChE-IN-5Cholinesterase (ChE)Epoxide HydrolaseTNF ReceptorInterleukin RelatedTumor Necrosis Factor ReceptorTNFRILSH-SY5YacetylcholinesteraseAlzheimer's diseaseBV-2SMMC7721PC12HepG2ICR miceKunming micesoluble epoxide hydrolaseInhibitorinhibitorinhibit

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