2. Neuronal Signaling Immunology/Inflammation
  3. Cholinesterase (ChE) COX
  4. BChE-IN-46

BChE-IN-46 是一种选择性且具有血脑屏障穿透性的 BChE 抑制剂（eqBChE IC50 = 7.44 × 10-5 μM，SI > 270,000，hBChE IC50 = 1.48 × 10-3 μM）。BChE-IN-46 还具有 COX-2 抑制活性（IC50 = 0.11 μM）。BChE-IN-46 可发挥神经保护作用，提升乙酰胆碱水平，并改善认知障碍、焦虑以及学习和记忆功能缺陷。BChE-IN-46 可用于抗阿尔茨海默病药物的研发。

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BChE-IN-46

BChE-IN-46 Chemical Structure

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100 mg   询价  
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Customer Review

BChE-IN-46 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 COX 亚型特异性产品:

查看所有亚型
COX COX-1 COX-2 COX-3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

BChE-IN-46 is a selective and brain-penetrant BChE inhibitor (eqBChE IC50 = 7.44 × 10−5 μM, SI > 270,000; hBChE, IC50 = 1.48 × 10−3 μM). BChE-IN-46 has COX-2 inhibitory activity (IC50 = 0.11 μM). BChE-IN-46 exhibits neuroprotective effects, enhances acetylcholine levels, and alleviates cognitive deficits, anxiety, and learning/memory impairments. BChE-IN-46 can be used for the development of anti-Alzheimer's disease drugs[1].

IC50 & Target[1]

COX-2

0.11 μM (IC50)

hBCHE

1.48 nM (IC50)

eqBCHE

74.4 pM (IC50)

体外研究
(In Vitro)

BChE-IN-46 (Compound 17) (100 μM, 24 h) 在 BV2，PC12 和 HT22 细胞中显示出良好的体外细胞安全性[1]。
BChE-IN-46 (5-20 μM, 24 h) 在 Lipopolysaccharides (LPS) (HY-D1056) 诱导的 BV2 细胞中表现出抗炎活性[1]。
BChE-IN-46 (10-40 μM, 24 h) 在 β-Amyloid (1-42) (Aβ1-42) (HY-P1363) 诱导的 PC12 细胞损伤模型中表现出针对 Aβ 的神经保护作用[1]。

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

BChE-IN-46 相关抗体:

Cell Viability Assay[1]

Cell Line: BV2, PC12 and HT22 cell
Concentration: 100 μM
Incubation Time: 24 h
Result: Exhibited weak or no toxicity on BV2, PC12 and HT22 cell.

ELISA Assay[1]

Cell Line: LPS (1 μg/mL)-induced BV2 cells
Concentration: 5, 10, and 20 μM
Incubation Time: 24 h
Result: Reduced LPS-induced NO, IL-6, and TNF-α production in a concentration-dependent manner.

Cell Viability Assay[1]

Cell Line: Aβ1-42-induced PC12 cell
Concentration: 10, 20, and 40 μM
Incubation Time: 24 h
Result: Exhibited a dose-dependent protection against Aβ1-42-induced toxicity in PC12 cells and the protective efficacy.
体内研究
(In Vivo)

BChE-IN-46 (compound 17) (3-25 mg/kg，腹腔注射，每日一次共计 16 天) 在 Kunming 小鼠中可改善东莨菪碱 (HY-N0296) 诱导的认知缺陷、焦虑以及学习/记忆障碍[1]。
BChE-IN-46 (250 mg/kg，腹腔注射，一次) 在 Kunming 小鼠中显示出良好的体内安全性[1]。
BChE-IN-46 (100 mg/kg，腹腔注射，一次) 在雄性 SD 大鼠中表现出有效的血脑屏障穿透和脑脊液滞留能力[1]
。

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

Animal Model: Scopolamine (3 mg/kg, i.p.) -induced male Kunming mice (25 g-30 g, 6 weeks)[1].
Dosage: 3, 12.5, 25 mg/kg
Administration: i.p., once daily, 16 days
Result: Increased both movement distance and residence time in the central region.
Produces no cholinergic adverse effects or motor deficits in mice.
Reduced path length.
Ameliorated scopolamine-induced cholinergic dysfunction primarily through BChE inhibition-mediated ACh restoration.
Attenuated increases in hippocampal TNF-α and IL-6.
Reversed the scopolamine-induced reduction in Nissl positive neurons and ameliorated neuronal damage.
Animal Model: Kunming mice (30 g-35 g, 6 weeks)[1].
Dosage: 250 mg/kg
Administration: i.p., once, dissolved in a mixed solvent composed of DMSO (HY-Y0320C), HS-15 (HY-Y1893), castor oil (HY-107799) and normal saline (HY-W460471) (8/5/5/82, V/V/V/V).
Result: Had no mortality or treatment-related abnormalities.
Did not significantly alter the mean body weight.
Resulted in normal tissue architecture in major organs, with no treatment-related lesions observed.
Animal Model: male SD rats (220 g-250 g, 8 weeks)[1].
Dosage: 100 mg/kg
Administration: i.p., once
Result: Maintained sustained concentrations in cerebrospinal fluid (CSF) between 20 min and 2 h.
分子量

420.50

Formula

C24H28N4O3
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

BChE-IN-46 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

BChE-IN-46Cholinesterase (ChE)COXCyclooxygenaseAlzheimer's diseaseBChEblood-brain barrierCOX-2Inhibitorinhibitorinhibit

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目录号：
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