2. Neuronal Signaling
  3. Cholinesterase (ChE)
  4. AChE/BChE-IN-35

AChE/BChE-IN-35，Tacrine (HY-111338) 衍生物，是一种可穿透血脑屏障的双重 AChE/BChE 抑制剂，对电鳗 AChE 的 IC50 为 123.66 nM，对人源 AChE 的 IC50 为 122.34 nM，对马源 BChE 的 IC50 为 488.00 nM。AChE/BChE-IN-35 可通过 LAT1 介导的主动转运穿过细胞膜。AChE/BChE-IN-35 表现出增强的脑暴露量以及更慢的脑组织清除速率。AChE/BChE-IN-35 可用于阿尔茨海默病的相关研究。

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AChE/BChE-IN-35

AChE/BChE-IN-35 Chemical Structure

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AChE/BChE-IN-35 相关抗体

Top Publications Citing Use of Products

查看 Cholinesterase (ChE) 亚型特异性产品:

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AChE BChE

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AChE/BChE-IN-35, Tacrine (HY-111338) derivative, is a brain-penetrant dual AChE/BChE inhibitor with an Electric Eel AChE IC50 of 123.66 nM, human AChE IC50 of 122.34 nM, and equine BChE IC50 of 488.00 nM. AChE/BChE-IN-35 undergoes LAT1-mediated active transport across cell membranes. AChE/BChE-IN-35 exhibits enhanced brain exposure with slower brain tissue elimination. AChE/BChE-IN-35 can be used for the research of alzheimer's disease[1].

IC50 & Target[1]

hAChE

122.34 nM (IC50)

electric eel AChE

123.66 nM (IC50)

eqBCHE

488.00 nM (IC50)

体外研究
(In Vitro)

AChE/BChE-IN-35 (Compound L3) (5 min) 可抑制 eeAChE、hAChE 和 eqBChE，其 IC50 值分别为 123.66 nM、122.34 nM 和 488.00 nM[1]。
AChE/BChE-IN-35 (50-100 μM; 24 h) 对 bEnd.3 细胞表现出低细胞毒性，在 100 μM 处理 24 h 后细胞存活率仍接近 80%[1]。
AChE/BChE-IN-35 (5 μg/mL; 30-300 min) 可穿过体外 bEnd.3 细胞血脑屏障模型，其表观渗透系数为 11.25 × 10-6 cm/s[1]。
AChE/BChE-IN-35 (4 h) 可通过 LAT1 转运进入 U87 细胞：在 LAT1 竞争性抑制剂存在时，其细胞内水平无法检测到[1]。
AChE/BChE-IN-35 (10-50 μM; 24 h) 对 HBMEC、BV2、PC-12、SH-SY5Y 细胞表现出低细胞毒性，经 24 h 处理后，在测试浓度下细胞存活率仍保持在 50%以上[1]。
AChE/BChE-IN-35 (10-100 μM; 24 h) 在 HepG2 细胞和 L02 细胞中表现出较低的肝毒性，在测试浓度下处理 24 小时后，细胞存活率仍保持在 50% 以上[1]。

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

AChE/BChE-IN-35 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: mouse brain microvascular endothelial cells (bEnd.3)
Concentration: 50, 100 μM
Incubation Time: 24 h
Result: Maintained cell viability close to 80% at 100 μM.
Maintained cell viability nearly 100% at 50 μM.

Cell Cytotoxicity Assay[1]

Cell Line: human brain microvascular endothelial cells (HBMEC), murine microglial cells (BV2), rat adrenal pheochromocytoma cells (PC-12), human neuroblastoma cells (SH-SY5Y), human normal hepatocyte (L02), human hepatocellular carcinoma cells (HepG2)
Concentration: 10, 20, 50, 100 μM (HBMEC, BV2, PC-12, SH-SY5Y); 1.25, 2.5, 5, 10, 20, 50, 100, 200 μM (HepG2, L02)
Incubation Time: 24 h
Result: Maintained viability above 50% across 10-50 μM in HBMEC, BV2, PC-12, and SH-SY5Y cells.
Maintained viability above 50% across 10-100 μM in HepG2 and L02 cells.
药代动力学
(Parmacokinetics)
Species Dose Route AUC Brain-to-Plasma Ratio Tmax
Mice[1] 10 mg/kg i.p. 20037 min·ng/mL 68 % 15 min
体内研究
(In Vivo)

AChE/BChE-IN-35 (Compound L3) (10 mg/kg；腹腔注射；单次给药) 表现出比 Tacrine (HY-111338) 更强的血脑屏障通透性，其脑-血浆 AUC0-t 比值为 0.68，总脑暴露量高 21.3%[1]。

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

446.54

Formula

C26H30N4O3
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

AChE/BChE-IN-35 相关分类

  • 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.

Keywords:

AChE/BChE-IN-35Cholinesterase (ChE)Electric Eel AChEbEnd.3 cellsblood-brain barrierbutyrylcholinesterasehuman AChELAT1alzheimer's diseaseequine BChEU87 cellsacetylcholinesteraseInhibitorinhibitorinhibit

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