2. Neuronal Signaling Immunology/Inflammation Metabolic Enzyme/Protease NF-κB
  3. Cholinesterase (ChE) Amyloid-β Tau Protein NOD-like Receptor (NLR) Reactive Oxygen Species Mitochondrial Metabolism
  4. AChE/BChE-IN-23

AChE/BChE-IN-23 (Compound 6e) 是一个 AChE/BChE 抑制剂 (AChE，eqBChE 和 hBChE的 IC50 分别为 0.91 μM，1.19 μM 和1.01 μM)。AChE/BChE-IN-23有抗氧化功效，抑制 Aβ1-42 和 Tau 蛋白聚集。AChE/BChE-IN-23 也通过抑制活性氧释放和线粒体损伤抑制小胶质细胞激活。AChE/BChE-IN-23 还减少人小胶质细胞中的 NLRP3 炎性小体。其也可逆转东莨菪碱 (HY-N0296) 诱导的小鼠记忆损伤。

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AChE/BChE-IN-23 Chemical Structure

AChE/BChE-IN-23 Chemical Structure

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AChE/BChE-IN-23 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 NOD-like Receptor (NLR) 亚型特异性产品:

查看所有亚型
NLRP3 NLRP1 NOD1 NOD2

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AChE/BChE-IN-23 (Compound 6e) is an AChE/BChE inhibitor (IC50: 0.91 μM, 1.19 μM and 1.01 μM for hAChE, eq BChE and hBChE, respectively). AChE/BChE-IN-23 has antioxidant activity and inhibits Aβ1-42 and Tau protein aggregation. AChE/BChE-IN-23 also inhibits microglial activation by reducing ROS release and mitochondrial injury. AChE/BChE-IN-23 suppresses NLRP3 inflammasome and pro-inflammatory cytokines in human microglial cells. AChE/BChE-IN-23 also reverses the Scopolamine (HY-N0296)-induced memory impairment in mice model[1].

IC50 & Target[1]

hAChE

0.91 μM (IC50)

eqBCHE

1.19 μM (IC50)

NLRP3

 

hBCHE

1.02 μM (IC50)

体外研究
(In Vitro)

AChE/BChE-IN-23 会导致碘化丙啶 (对 AChE 酶有亲和力) 移位 (5 μM，2.06%；10 μM，11.78%；20 μM，14.47%；50 μM，27.53%)[1].。
AChE/BChE-IN-23 具有抗氧化作用 (20 μM;对DPPH清除率为47.30%，IC50:15.17 μM) [1].。
AChE/BChE-IN-23 (3.125 μM, 72 h) 能有效抑制 Aβ1-42 (12.5 μM) 的聚集[1].。
AChE/BChE-IN-23 (1.125 μM, 72 h) 能有效抑制 Tau (5 μM) 的聚集[1].。
AChE/BChE-IN-23 (1-20 μM, 24 h) 对 PC-12 细胞没有毒性[1].。
AChE/BChE-IN-23 (12.5 μM, 24 h) 通过减少 ROS 的释放和恢复线粒体膜电位抑制小胶质细胞的激活[1]。
AChE/BChE-IN-23 (12.5 μM, 24 h) 通过抑制小胶质细胞中炎性小体和 NF-κB 的激活发挥抗炎作用[1]。

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

AChE/BChE-IN-23 相关抗体:

Western Blot Analysis[1]

Cell Line: HMC-3 cells
Concentration: 12.5 μM
Incubation Time: 24 h
Result: Suppressed NLRP3, caspase-1, IL-1β and IL-18 expression.

Immunofluorescence[1]

Cell Line: HMC-3 cells
Concentration: 12.5 μM
Incubation Time: 24 h
Result: Reduced mitochondrial ROS and stabilizes the mitochondrial membrane potential.
体内研究
(In Vivo)

AChE/BChE-IN-23 (10 mg/kg，腹腔注射，14 天) 通过增强 AD 小鼠的空间记忆和认知记忆，逆转了东莨菪碱诱导的阿尔兹海默症[1].。
AChE/BChE-IN-23 (2000 mg/kg，灌胃，14 天) 对 Swiss albino 小鼠无毒性，包括与急性毒性相关的体重增加、行为异常、抽搐、震颤或腹泻[1]。

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

Animal Model: Scopolamine (1 mg/kg) induced Alzheimer’s disease (AD) model; 6-week-old Swiss albino mice[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.), 14 days
Result: Decreased escape latency, distance traveled in Morris Water Maze (MWM) experiment.
Increased latency period in passive avoidance.
Increased BDNF and Nr4a2 in brain.
分子量

367.40

Formula

C19H21N5O3
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-23 相关分类

  • 摩尔计算器

  • 稀释计算器

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

AChE/BChE-IN-23Cholinesterase (ChE)Amyloid-βTau ProteinNOD-like Receptor (NLR)Reactive Oxygen SpeciesMitochondrial Metabolismβ-amyloid peptideAβAbetaAlzheimer's diseaseAntioxidant activityNeuroprotectionMicroglialNLRP3HMC-3 cellsInhibitorinhibitorinhibit

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