2. Neuronal Signaling Others
  3. Cholinesterase (ChE) Drug Intermediate
  4. BuChE-IN-22

BuChE-IN-22 是一种拟不可逆的丁酰胆碱酯酶 (BuChE) 抑制剂，其对于 hBuChE 和 hAChE 的 IC50 分别为 4 和 157 nM。同时也是 7-hydroxysertraline 的前药。BuChE-IN-22 可在抑制 BuChE 的过程中释放 7-hydroxysertraline。BuChE-IN-22 可在阿尔茨海默病小鼠模型中完全逆转 Aβ25-35 诱导的短期和长期记忆损伤。BuChE-IN-22 可用于阿尔茨海默病的相关研究。

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BuChE-IN-22

BuChE-IN-22 Chemical Structure

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BuChE-IN-22 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

BuChE-IN-22 is a pseudo-irreversible butyrylcholinesterase (BuChE) inhibitor, with IC50 values of 4 nM and 157 nM against hBuChE and hAChE, respectively. It also acts as a prodrug of 7-hydroxysertraline. BuChE-IN-22 releases 7-hydroxysertraline during BuChE inhibition. BuChE-IN-22 completely reverses Aβ25-35-induced short-term and long-term memory impairments in a mouse model of Alzheimer's disease. BuChE-IN-22 can be used in research related to Alzheimer's disease[1].

IC50 & Target[1]

hBCHE

4 nM (IC50)

hAChE

157 nM (IC50)

体外研究
(In Vitro)

BuChE-IN-22 (Compound 8e) (255 μM； 48 小时) 在无 hBuChE 的环境中性质稳定，但会被 hBuChE 在 48 小时内完全代谢，释放出 85% 的 5-羟色胺再摄取抑制剂 HO-Sert[1]。

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

BuChE-IN-22 相关抗体:
体内研究
(In Vivo)

BuChE-IN-22 (Compound 8e) (0.3-3 mg/kg；腹腔注射；每日给药；连续 7 天) 在阿尔茨海默病小鼠模型中，3 mg/kg 剂量可完全逆转 Aβ25-35 诱导的空间工作记忆损伤，1 mg/kg 剂量可完全逆转其诱导的长期非空间记忆损伤[1]。

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

Animal Model: Swiss mice (male, 6 weeks old, 30-35 g, intracerebroventricular injection of 9 nmol oligomeric Aβ25-35 peptide)[1]
Dosage: 0.3 mg/kg; 1 mg/kg (long-term non-spatial memory); 3 mg/kg (spatial working memory)
Administration: i.p.; daily; 7 days (starting 20 minutes post-Aβ25-35 injection)
Result: Completely prevented Aβ25-35-induced deficits in spontaneous alternation (spatial working memory) at 3 mg/kg.
Completely prevented Aβ25-35-induced deficits in passive avoidance retention latency (long-term non-spatial memory) at 1 mg/kg.
分子量

433.37

Formula

C23H26Cl2N2O2
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

BuChE-IN-22 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)

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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:

BuChE-IN-22Cholinesterase (ChE)Drug IntermediateDrug Iintermediateserotonin reuptake inhibitorAlzheimer's disease mouse modelbutyrylcholinesteraseacetylcholinesteraseAβ25-357-hydroxysertralinehAChEhBuChEInhibitorinhibitorinhibit

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