2. Neuronal Signaling
  3. Cholinesterase (ChE)
  4. hAChE/hBACE-1-IN-1

hAChE/hBACE-1-IN-1 (compounds 5d) 是具有血脑通透性的 hAChE 的口服活性抑制剂。hAChE/hBACE-1-IN-1抑制 hAChE 和 hBACE-1，IC50 值分别为 0.076 和 0.23 μM。hAChE/hBACE-1-IN-1抑制 Aβ1-42 聚集并改善小鼠的学习和记忆能力。hAChE/hBACE-1-IN-1 可用于研究阿尔茨海默病。

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hAChE/hBACE-1-IN-1 Chemical Structure

hAChE/hBACE-1-IN-1 Chemical Structure

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hAChE/hBACE-1-IN-1 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

hAChE/hBACE-1-IN-1 (compounds 5d) is an orally active inhibitor of hAChE with blood-brain permeability. hAChE/hBACE-1-IN-1 inhibits hAChE and hBACE-1 with IC50 values of 0.076 and 0.23 μM, respectively. hAChE/hBACE-1-IN-1 inhibits Aβ1-42 aggregation and improves mouse learning and memory ability. hAChE/hBACE-1-IN-1 can be used to research in Alzheimer's disease[1].

IC50 & Target

hAChE

0.076 μM (IC50)

hBACE-1

0.23 μM (IC50)

hBCHE

1.204 μM (IC50)

体外研究
(In Vitro)

hAChE/hBACE-1-IN-1 (10-80 μM，48 h) 在 SH-SY5Y 中最大浓度下仍具有安全性[1]。

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

hAChE/hBACE-1-IN-1 相关抗体:

Cell Viability Assay[1]

Cell Line: SH-SY5Y
Concentration: 10 μM, 20 μM, 40 μM, 80 μM
Incubation Time: 48 h, 72 h
Result: Indicated the similar in safety to donepezil (HY-14566) at a maximum 80 μM concentration.
Restored the cell that Aβ1-42 treated viability to 70% after 48 h, to 77% after 72 h cell.
体内研究
(In Vivo)

hAChE/hBACE-1-IN-1 (2.5-10 mg/kg，口服， 14 天) 在东莨菪碱诱导的认知缺陷小鼠模型中改善小鼠学习和记忆能力，减少 RTL 和张开双臂的时间[1]。
hAChE/hBACE-1-IN-1 ( 500 mg/kg，口服， 14 天) 耐受性良好，对小鼠没有毒性，包括大脑，肝脏，肾脏和心脏均没有异常[1]。
hAChE/hBACE-1-IN-1 (10 mg/kg，口服， 14 天) 在东莨菪碱诱导的小鼠模型中能够穿过血脑屏障，降低海马和皮层脑匀浆中的 AChE 水平或底物，具有延缓氧化应激和降低促炎细胞因子水平的潜力[1]。
hAChE/hBACE-1-IN-1 (10 mg/kg，口服， 14天)在 Aβ 诱导的模型中抑制 BACE-1、Aβ、APP/Aβ 和 tau 蛋白，保护不同脑区的脑组织[1]。

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

Animal Model: scopolamine-induced amnesia models in Swiss albino mice[1].
Dosage: 2.5, 5, 10 mg/kg/day
Administration: oral administration (p.o.) 14 days
Result: Improved learning and memory and reduce RTL and time spent in open arms.
Crossed the blood-brain barrier, and reduced AChE levels or substrate hydrolysis in hippocampal and cortex brain homogenates.
Reduced MDA, ROS levels, nitrite concentration, and increased GSH levels in a dose-dependent manner.
Reduced levels of proinflammatory cytokines.
Animal Model: Aβ-induced models in Swiss albino mice[1].
Dosage: 10 mg/kg/day
Administration: oral administration (p.o.) 14 days
Result: Inhibited BACE-1, Aβ, APP/Aβ, and tau protein and protected brain tissue in different brain regions.
分子量

433.53

Formula

C23H23N5O2S
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

hAChE/hBACE-1-IN-1 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:

hAChE/hBACE-1-IN-1Cholinesterase (ChE)SH-SY5Yblood-brain barrierMTDLscopolamine-induced amnesia modelAlzheimer’s diseaseInhibitorinhibitorinhibit

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