1. Neuronal Signaling
  2. Cholinesterase (ChE) Amyloid-β
  3. AChE-IN-94

AChE-IN-94 是一种具有口服活性并且能够穿过血脑屏障的乙酰胆碱酯酶 (AChE) 抑制剂,IC50 为 0.40 μM,Ki 为 0.28 μM。AChE-IN-94 可抑制自发性和 AChE 介导的 1-42 聚集。AChE-IN-94 在 Scopolamine (HY-N0296) 诱导的遗忘模型中可缓解认知/记忆缺陷。AChE-IN-94 可用于阿尔茨海默病 (AD) 的研究。

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AChE-IN-94

AChE-IN-94 Chemical Structure

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查看 Cholinesterase (ChE) 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AChE-IN-94 is an orally active and blood-brain barrier penetrable AChE inhibitor with an IC50 of 0.40 μM and Ki of 0.28 μM. AChE-IN-94 prevents self-induced and AChE-mediated1-42 aggregation. AChE-IN-94 alleviates cognitive/memory deficits in Scopolamine (HY-N0296)-induced amnesic model. AChE-IN-94 can be used for the study of Alzheimer's disease (AD)[1].

IC50 & Target[1]

AChE

0.4 μM (IC50)

AChE

0.28 μM (Ki)

体外研究
(In Vitro)

AChE-IN-94 (Compound LB05) 对乙酰胆碱酯酶 (AChE) 表现出强效的抑制活性,IC50 为 0.40 μM,抑制常数 (Ki) 为 0.28 μM[1]。 AChE-IN-94 (10-50 μM) 以剂量依赖方式从 AChE 的外周阴离子位点 (PAS) 置换碘化丙啶 (PI)[1]。 AChE-IN-94 (5-20 μM, 48 小时) 以浓度依赖方式抑制 Aβ1-42 聚集[1]

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

体内研究
(In Vivo)

AChE-IN-94 (Compound LB05) (5-20 mg/kg, 灌胃,每日一次,连续 7 天) 可改善 Scopolamine (HY-N0296) 诱导的雄性 Wistar 大鼠认知障碍[1]

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

Animal Model: Scopolamine-induced amnesia rat model: Male Wistar rats (160-180 g) were injected with scopolamine (3 mg/kg, i.p.) on the 7th day[1]
Dosage: 5, 10, 20 mg/kg
Administration: p.o., once daily for 7 days
Result: Ameliorated cognitive deficits in a dose-dependent manner.
Restored the percentage of spontaneous alternation (reflecting spatial working memory) and the total number of arm entries (reflecting exploratory activity).
Improved cholinergic function and reduced oxidative stress in the hippocampus.
Decreased AChE activity, reduced malondialdehyde (MDA) levels, and elevated catalase (CAT) activity.
分子量

432.90

Formula

C20H18ClFN4O2S

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 *
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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:
AChE-IN-94
目录号:
HY-175758
需求量: