2. Neuronal Signaling
  3. Cholinesterase (ChE) Amyloid-β Tau Protein
  4. BChE-IN-41

BChE-IN-41 有一种有高效选择性的丁酰胆碱酯酶 (BChE) 抑制剂 (IC50 = 12 nM, Ki = 6.6 nM)。BChE-IN-41 具有高脑渗透性，脑血浆比为 9.0。BChE-IN-41 对东莨菪碱和 Aβ1-42 诱导的阿尔茨海默病症状的小鼠具有促认知作用[1]。

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BChE-IN-41 Chemical Structure

BChE-IN-41 Chemical Structure

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BChE-IN-41 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

BChE-IN-41 is a highly selective Butyrylcholinesterase (BChE) inhibitor (IC50 =12 nM, Ki = 6.6 nM). BChE-IN-41 has high brain penetration with a brain-to-plasma ratio of 9.0. BChE-IN-41 has pro-cognitive effects on mice with AD-like symptoms induced by Scopolamine (HY-N0296) and Aβ1-42[1].

IC50 & Target

hAChE

22110 nM (IC50)

体外研究
(In Vitro)

BChE-IN-41 (Compound (R)-(−)-3) (5 μM, 48 h) 具有神经保护活性，减少了 Aβ1-42 诱导的 SH-SY5Y 细胞死亡[1]。

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

BChE-IN-41 相关抗体:

Cell Viability Assay[1]

Cell Line: HepG2 cells, SH-SY5Y cells
Concentration: 1 μM, 5 μM, 10 μM, 20 μM, 50 μM, 100 μM
Incubation Time: 48 h
Result: Had comparable cytotoxicity profiles in both HepG2 cells and SH-SY5Y cells.

Cell Cytotoxicity Assay[1]

Cell Line: SH-SY5Y cells
Concentration: 2.5 μM, 5 μM
Incubation Time: 48 h
Result: Reversed Aβ toxicity and reduced cell death at 5 μM; its effect was not significant at 2.5 μM.
体内研究
(In Vivo)

BChE-IN-41 (Compound (R)-(−)-3) (10-100 mg/kg, i.g, 单次给药) 在野生型Balb/c小鼠中效力强，具有高脑渗透性，且具备低毒性，小鼠无组织病理学变化[1]。
BChE-IN-41 (1-10 mg/kg, i.p, 单次给药) 可在东莨菪碱诱导的成年雄性 CD-1 小鼠中改善情境记忆缺陷和识别记忆缺陷[1]。
BChE-IN-41 (10 mg/kg, i.p, 连续给药14天) 可在Aβ1-42 寡聚体诱导的 ICR 雄性小鼠中改善学习能力和认知功能[1]。

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

Animal Model: Female and male wild-type Balb/c mice (3 months)[1]
Dosage: 10 mg/kg, 100 mg/kg
Administration: Oral gavage (i.g.), sing dose
Result: Exhibited high brain penetration with a brain-to-plasma ratio of 9.0.
Caused no mortality or tissue lesions in mice, and no abnormalities were found in histological examination.
Caused steady weight gain with no signs of acute toxicity.
Animal Model: Scopolamine (HY-N0296) (1 mg/kg, s.c) induced AD model in adult male CD-1 mice (18-22 g)[1]
Dosage: 1 mg/kg, 10 mg/kg
Administration: Intraperitoneal injection (i.p.), sing dose
Result: Prolonged the latency to enter the dark chamber and improved the contextual memory deficit.
Demonstrated prolonged step-through latency compared to mice treated with scopolamine only.
Enhanced preference for novel objects and increased the discrimination index (DI) and reversed the recognition memory deficit.
Animal Model: Aβ1-42 oligomers (10 µg per mouse, i.c.v) induced AD-like cognitive deficits model in ICR male mice (8-10 weeks, 18−20 g)[1]
Dosage: 10 mg/kg
Administration: Intraperitoneal injection (i.p.), at the corresponding doses for 14 days.
Result: Caused no motor impairment in the rotarod test (6/18/24 rpm).
Resulted in shorter escape latency and shorter distance to reach the target area, and improved Aβ1-42-induced cognitive deficits.
分子量

394.53

Formula

C23H26N2O2S
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

BChE-IN-41 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 *
= × ×

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.

Keywords:

BChE-IN-41Cholinesterase (ChE)Amyloid-βTau Proteinβ-amyloid peptideAβAbetaAlzheimer’s DiseaseHepG2 cellsSH-SY5Y cellsBALB/C miceICR miceCD-1 micehBChEInhibitorinhibitorinhibit

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目录号：
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