1. Neuronal Signaling Membrane Transporter/Ion Channel Immunology/Inflammation Apoptosis
  2. Cholinesterase (ChE) nAChR Interleukin Related TNF Receptor
  3. BChE-IN-44

BChE-IN-44 是一种高效、可穿透血脑屏障、高选择性的丁酰胆碱酯酶 (BChE) 抑制剂 [equine BChE IC50 = 18.00 pM,human BChE IC50 = 1.50 nM]。BChE-IN-44 对 Aβ1-42 诱导的损伤模型具有神经保护作用,并能抑制 Aβ1-42 的自聚集。BChE-IN-44 可降低 Lipopolysaccharides (HY-D1056) 诱导的 BV2 细胞中炎症因子 (NO、IL-6TNF-α) 的水平。BChE-IN-44 可显著改善 Scopolamine (HY-N0296) 诱导的认知障碍。BChE-IN-44 能够调节小鼠海马体中 BChEacetylcholine 的水平。BChE-IN-44 可用于阿尔茨海默病 (AD) 的研究。

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BChE-IN-44

BChE-IN-44 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BChE-IN-44 is a potent, brain-penetrant, highly selective BChE inhibitor [equine BChE IC50 = 18.00 pM, human BChE IC50 = 1.50 nM]. BChE-IN-44 shows neuroprotective effects against the Aβ1-42-induced injury model and inhibitory effects on Aβ1-42 self-aggregation. BChE-IN-44 reduces the levels of inflammatory factors (NO, IL-6, and TNF-α) in Lipopolysaccharides (HY-D1056)-induced BV2 cells. BChE-IN-44 can significantly ameliorate Scopolamine (HY-N0296)-induced cognition impairment. BChE-IN-44 exhibits capacity in the regulation of BChE and acetylcholine levels in the mouse hippocampus. BChE-IN-44 can be used for the study of Alzheimer’s disease (AD)[1].

IC50 & Target

IL-6

 

RatBuChE

 

体外研究
(In Vitro)

BChE-IN-44 (Compound N14) (50 μM,24 小时) 对 PC12 和 SH-SY5Y 细胞的毒性约为 15%,表明 BChE-IN-44 在体外具有较高的安全性[1]
BChE-IN-44 的 Kc 值为 0.017 μM,表明 BChE-IN-44 对 BChE 具有较高的亲和力[1]
BChE-IN-44 (5-20 μM,24 小时) 可显著降低Lipopolysaccharides (LPS) 诱导的 BV2 细胞中炎症因子 (NO、IL-6 和 TNF-α) 的水平[1]
BChE-IN-44 (20 μM,24 小时) 对 Aβ1-42 诱导的 PC12 细胞损伤具有显著的神经保护作用[1]
BChE-IN-44 (20 μM, 48 小时) 能有效抑制 Aβ1-42 聚集,证实了载体支架对 Aβ1-42 聚集的良好抑制作用[1]

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

Cell Viability Assay[1]

Cell Line: PC12 cells, SH-SY5Y cells
Concentration: 50 μM
Incubation Time: 24 h
Result: Led to about 15 % cell toxicity in PC12 and SH-SY5Y.

ELISA Assay[1]

Cell Line: BV2 cells
Concentration: 5 μM, 10 μM, 20 μM
Incubation Time: 24 h
Result: Significantly reduced the levels of inflammatory factors (NO, IL-6, and TNF-α) in LPS-induced BV2 cells.

Cell Viability Assay[1]

Cell Line: PC12 cells
Concentration: 20 nM
Incubation Time: 24 h
Result: Showed significant neuroprotective efficacy against Aβ1-42-induced injury in PC12 cells.
体内研究
(In Vivo)

BChE-IN-44 (5-20 mg/kg,腹腔注射,每日一次,持续 14 天) 可有效逆转 Scopolamine 引起的小鼠认知障碍、焦虑以及学习和记忆缺陷,抑制 BChE 活性,增加 ACh 水平,并减少神经炎症[1]

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

Animal Model: Thirty-six six-week-old male Kunming mice (weighing 25-30 g) were intraperitoneally injected with scopolamine (3 mg/kg) to mimic AD-like cognitive deficits[1].
Dosage: 5 mg/kg, 10 mg/kg, 20 mg/kg
Administration: I.p., once daily for 14 days, 30 mins after Scopolamine
Result: Increased the spontaneous alternation rate to 72.6%, indicating improved working memory.
Increased central region dwell time and travel distance, and reduced anxiety-like behaviors.
Shortened escape latency, reduced travel distance, and increased platform crossings, showing improved spatial learning memory.
Behavioral trajectory plots showed more organized.
Increases ACh levels and decreases AChE and BChE activities.
Reduces IL-6 and TNF-α levels and inhibits neuroinflammation.
分子量

393.44

Formula

C22H23N3O4

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

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.

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产品名称:
BChE-IN-44
目录号:
HY-178356
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