2. Neuronal Signaling Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. Cholinesterase (ChE) Reactive Oxygen Species (ROS)
  4. AChE/BChE-IN-27

AChE/BChE-IN-27 是一种可透过血脑屏障的 AChE 和 BChE 混合抑制剂 (Pe = 4.12)，IC50 值分别为 3.72 μM 和 9.65 μM。AChE/BChE-IN-27 具有强大的抗氧化活性，在 DPPH (HY-112053) 测定中 IC50 值为 6.32 μM，同时显示出强大的离体抗氧化活性。AChE/BChE-IN-27 显示出金属螯合特性。AChE/BChE-IN-27 对氧化应激具有神经保护潜力。AChE/BChE-IN-27 显著降低细胞内活性氧 (ROS)。在体内实验中，AChE/BChE-IN-27 有效地恢复了 AChE 和 BChE 水平，改善认知，可用于阿尔兹海默症(AD)。

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AChE/BChE-IN-27 Chemical Structure

AChE/BChE-IN-27 Chemical Structure

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AChE/BChE-IN-27 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AChE/BChE-IN-27 is a blood-brain barrier–permeable mixed inhibitor (Pe = 4.12) of AChE and BChE, with IC50 values of 3.72 μM and 9.65 μM, respectively. AChE/BChE-IN-27 has potent antioxidant activity with an IC50 value of 6.32 μM in the DPPH (HY-112053) assay and also exhibits potent in vitro antioxidant activity. AChE/BChE-IN-27 exhibits metal chelating properties. AChE/BChE-IN-27 has neuroprotective potential against oxidative stress. AChE/BChE-IN-27 significantly reduces intracellular reactive oxygen species (ROS). In in vivo experiments, AChE/BChE-IN-27 effectively restored AChE and BChE levels, improved cognition, and can be used for Alzheimer's disease (AD)[1].

IC50 & Target

hAChE

3.72 μM (IC50)

eqBCHE

9.65 μM (IC50)

体外研究
(In Vitro)

AChE/BChE-IN-27 (Compound 12d) (10 nM-100 μM，12 天) 表现出较高的抑制效果，IC50 分别为 3.72 μM (AChE) 和 9.65 μM (BChE)[1]。

AChE/BChE-IN-27 (1-30 μM，37 ℃，30 分钟) 在酶动力学测定中对 hAChE 和 eqBChE 表现出混合抑制作用[1]。

AChE/BChE-IN-27 (5-50 μM，25 ℃，6 小时) 在外周阴离子位点 (PAS) 抑制研究中，PI 置换率为 23.58 %[1]。

AChE/BChE-IN-27 (1.25-20 μM，37 ℃，30 分钟) 在 DPPH (HY-112053) 测定中表现出最强的抗氧化活性，IC50 值为 6.32 μM[1]。

AChE/BChE-IN-27 (500 μM，37 ℃，18 小时) 的 Pe 值大于 2.0，表明 BBB 通透性中等 (CNS ±)[1]。

AChE/BChE-IN-27 (18 μM，5 分钟) 可作为缓解金属离子失调的潜在治疗剂[1]。

AChE/BChE-IN-27 (5 μM, 37 ℃, 72 小时) 可抑制 Aβ 1-42 聚集，进而抑制 Aβ 1-42 原纤维形成，表明其具有作为聚集调节剂的潜力[1]。

AChE/BChE-IN-27 (5-80 μM, 24 小时) 对 SH-SY5Y 细胞无细胞毒性[1]。

AChE/BChE-IN-27 (5-80 μM, 24 小时) 可有效保护 SH-SY5Y 细胞免受 H2O2 诱导的神经毒性[1]。

AChE/BChE-IN-27 (1-80 μM, 24 小时) 可降低 ROS 水平，保护 SH-SY5Y 细胞[1]。

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

AChE/BChE-IN-27 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: SH-SY5Y cells
Concentration: 80, 60, 50, 40, 20, 10, and 5 μM
Incubation Time: 24 h
Result: Showed no cytotoxicity in SH-SY5Y cells.
体内研究
(In Vivo)

AChE/BChE-IN-27 (Compound 12d) (500 mg/kg，口服，一次) 对雄性瑞士白化小鼠无毒性[1]。

AChE/BChE-IN-27 (1-10 mg/kg，腹腔注射，每日一次，7 天) 表现出显著的抗胆碱酯酶活性，并可改善东莨菪碱诱发的遗忘症模型中的认知功能，同时具有胆碱酯酶抑制剂和强效抗氧化剂的双重药理活性[1]。

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

Animal Model: Scopolamine-induced Alzheimer's mice, albino mice of both sexes (male and female) weighing 25 and 30 g[1]
Dosage: 1 mg/kg , 5 mg/kg, 10 mg/kg
Administration: i.p., once a day, 7 days
Result: Exhibited significant anti-ChE activity and improves cognitive function, improved spatial working memory.
Attenuated the increased AChE and BChE activities after scopolamine administration, restored the decreased SOD level caused by scopolamine-induced oxidative stress.
分子量

379.41

Formula

C21H21N3O4
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

AChE/BChE-IN-27 相关分类

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  • 稀释计算器

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  • 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:

AChE/BChE-IN-27Cholinesterase (ChE)Reactive Oxygen Species (ROS)InhibitorSH-SY5Y cellsScopolamine-induced Alzheimer's miceAlzheimer's diseaseinhibitorinhibit

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