1. Neuronal Signaling Apoptosis PI3K/Akt/mTOR Stem Cell/Wnt Immunology/Inflammation
  2. Cholinesterase (ChE) Bcl-2 Family GSK-3 Wnt β-catenin Amyloid-β Apoptosis Interleukin Related TNF Receptor
  3. BChE-IN-49

BChE-IN-49 是一种具有口服活性的 BChE 抑制剂,其对于 BChE AChEIC50 为 0.73 和 6.43 μM。BChE-IN-49 可降低 AChE 水平以抑制乙酰胆碱的降解。BChE-IN-49 通过抑制 GSK-3β,强力激活 Wnt/β-catenin 信号通路,挥强效抗 、抗氧化、抗神经炎症和抗细胞凋亡 (apoptosis) 的作用。BChE-IN-49 可用于阿尔茨海默病的相关研究。

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BChE-IN-49

BChE-IN-49 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BChE-IN-49 is an orally active BChE inhibitor with IC50 values of 0.73 μM and 6.43 μM against BChE and AChE, respectively. BChE-IN-49 reduces AChE levels to inhibit the degradation of acetylcholine. By inhibiting GSK-3β, BChE-IN-49 potently activates the Wnt/β-catenin signaling pathway, exerting potent anti-, antioxidant, anti-neuroinflammatory and anti-apoptotic effects. BChE-IN-49 can be used in research related to Alzheimer's disease[1].

IC50 & Target[1]

BChE

0.73 μM ()

AChE

6.43 μM ()

Bax

 

Bcl-2

 

IL-1β

 

GSK-3β

 

体内研究
(In Vivo)

BChE-IN-49 (Compound 10) (30 mg/kg; p.o.; 每日一次共 5 周) 可显著改善 AlCl3 诱导的 AD 大鼠的认知功能,减少阿尔茨海默病病理生理标志物,调控神经炎症、细胞凋亡及 Wnt/β-catenin 通路,并增强其氧化应激防御能力[1]

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

Animal Model: Sprague Dawley (adult male, 300-320 g, AlCl3-induced AD model)[1]
Dosage: 30 mg/kg
Administration: p.o.; daily; 5 weeks (concurrent with AlCl3 i.p. dosing)
Result: Effectively reversed the cognitive dysfunction induced by AlCl3 in rats.
Inhibited the key enzyme (BACE1) that generates Aβ to reduce Aβ deposition.
Significantly increased the level of BDNF, which had neuroprotective and repair effects.
Reduced levels of pro-inflammatory cytokines IL-1β and TNF-α.
Effectively inhibited neuronal apoptosis.
Strongly activated the Wnt/β-catenin neuroprotective pathway, while inhibiting its negative regulatory factor GSK-3β.
Significantly reversed the decline in DA, NE and 5-HT levels caused by AlCl3, restoring them by 4.5 times, 2.6 times and 5.6 times respectively.



分子量

395.90

Formula

C22H18ClNO2S

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
  • 摩尔计算器

  • 稀释计算器

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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.

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BChE-IN-49
目录号:
HY-181248
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