2. Neuronal Signaling Protein Tyrosine Kinase/RTK
  3. Cholinesterase (ChE) DYRK
  4. hAChE-IN-8

hAChE-IN-8 (Compound S-12) 是口服有效的 hAChE 选择性的抑制剂 (IC50=0.486 μM)。hAChE-IN-8 对 BACE-1 也有抑制效果 (IC50=0.542 μM)，对 Dyrk1A 抑制效果不明显 (IC50>10 μM)。hAChE-IN-8 可以减少 Aβ 聚集，拥有良好的血脑屏障穿透性，具有口服活性。hAChE-IN-8 主要用于阿尔茨海默病的研究。

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hAChE-IN-8 Chemical Structure

hAChE-IN-8 Chemical Structure

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hAChE-IN-8 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 DYRK 亚型特异性产品:

查看所有亚型
DYRK1 DYRK2 DYRK3 DYRK4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

hAChE-IN-8 (Compound S-12) is a orally effective and selective inhibitor of hAChE (IC50=0.486 μM). hAChE-IN-8 also inhibits BACE-1 (IC50=0.542 μM), and does not inhibit Dyrk1A (IC50>10 μM). hAChE-IN-8 can reduce Aβ aggregation, has good blood-brain barrier penetration. hAChE-IN-8 is mainly used in Alzheimer's disease research[1].

IC50 & Target[1]

hBCHE

0.542 μM (IC50)

DYRK1A

>10 μM (IC50)

hAChE

0.486 μM (IC50)

体外研究
(In Vitro)

hAChE-IN- 8 (10-80 μM; 72 h) 在高浓度下对 SH-SY5Y 神经细胞无毒性[1]。
hAChE-IN- 8 (40 μM; 72 h) 在 Aβ1-42 引起的氧化应激中保护 SH-SY5Y 细胞存活率显著提高，细胞形态恢复正常[1]。
hAChE-IN- 8 (5-20 μM; 48 h) 显示出显著的抗 Aβ 聚集活性[1]。

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

hAChE-IN-8 相关抗体:
体内研究
(In Vivo)

hAChE-IN- 8 (500,1000 mg/kg; p.o.; single dose) 在高剂量下,所有大鼠在 14 天观察期内未显示任何毒性或异常反应[1]。
hAChE-IN- 8 (2.5-10 mg/kg; p.o.; single dose) 剂量依赖性下改善了东莨菪碱 (HY-N0296) 诱导的记忆丧失。在东莨菪碱诱导的氧化应激中表现出抗氧化潜力，并能恢复 ACh 和 AChE 水平[1]。
hAChE-IN- 8 (10 mg/kg; p.o.;once daily for 9 days) Aβ1-42 诱导的 AD 模型中表现出显著的认知改善效果。显著降低 AD 相关蛋白水平[1]。
hAChE-IN- 8 (10-200 μM) 添加到果蝇的培养基中，在较低浓度下对果蝇无明显毒性，但在高浓度下表现出一定的毒性[1]。
hAChE-IN- 8 (10-20 μM) 在果蝇 AD 模型中有效恢复了 Aβ42 诱导的眼部表型变化，表现出显著的神经保护作用[1]。
hAChE-IN- 8 (5-50 μM) 在较低浓度下对幼虫细胞具有较高的存活率，但在高浓度下细胞存活率显著下降，表现出一定的细胞毒性[1]。


Wistar 大鼠中的药代动力学分析[1]

Route Dose (mg/kg) Tmax (h) Cmax (ng/mL) t1/2 (h) MRT (h) AUC0-8 (ng/mL.h) AUCtotal (ng/mL.h)
p.o. 10 9 ± 1.041 355 ± 6.033 41 ± 1.017 32 ± 1.713 1136.18 ± 4.017 1736.18 ± 7.101

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

Animal Model: Wistar rats[1]
Dosage: 500,1000 mg/kg
Administration: p.o.; single dose
Result: At the maximum dose of 1000 mg/kg, the histology of organs (kidney, liver, brain and heart) was normal in rats after 14 days.
Animal Model: Scopolamine-induced memory loss in Wistar rats[1]
Dosage: 2.5 mg/kg, 5 mg/kg, 10 mg/kg
Administration: p.o.; single dose
Result: The effect of improvement in the 10 mg/kg dose group was similar to donepezil (HY-14566) group. Decreased AChE activity, increased ACh levels, decreased MDA levels, and increased SOD, CAT, and GSH levels.
Animal Model: Aβ1-42 induced AD mode[1]
Dosage: 10 mg/kg
Administration: p.o.; once daily for 9 days
Result: Significantly reduced escape latency (ELT) and increased number of plateau crossings, similar to the donepezil (HY-14566) group. Significantly reduced BACE-1, α-synuclein, APP and Tau protein levels. Significantly reduced BACE-1 and Aβ levels in the DG, CA1 and CA3 regions.
Animal Model: AD Drosophila model [1]
Dosage: 10 μM, 20 μM
Administration: /
Result: At a concentration of 10 μM, the recovery of the eye phenotype in Drosophila was 21%. At 20 μM, the recovery rate increased to 57%.
分子量

442.47

Formula

C25H22N4O4
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-IN-8 相关分类

  • 摩尔计算器

  • 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:

hAChE-IN-8Cholinesterase (ChE)DYRKDual specificity tyrosine phosphorylation regulated kinaseDual specificity tyrosine regulated kinaseMTDLAlzheimer's diseaseAChE inhibitorAnti-Aβ aggregationNeuroprotective effectsDrosophila modelWistar ratsInhibitorinhibitorinhibit

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