AChE-IN-21

• 常用名: AChE-IN-21
• 英文名: AChE-IN-21
• CAS号: 2413656-04-7
• 分子量: 395.49
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₄H₂₉NO₄
• 熔点: N/A
• 闪点: N/A

AChE-IN-21用途

AChE-IN-21(化合物I-8)是一种有效、选择性和口服活性的AChE抑制剂,IC50为2.66 nM。AChE-IN-21在体外表现出良好的血脑屏障通透性[1]。

AChE-IN-21名称

• 英文名: AChE-IN-21

AChE-IN-21生物活性

• 描述: AChE-IN-21(化合物I-8)是一种有效、选择性和口服活性的AChE抑制剂,IC50为2.66 nM。AChE-IN-21在体外表现出良好的血脑屏障通透性[1]。
• 相关类别:
  研究领域 >> 神经疾病
  信号通路 >> 神经信号通路 >> 疼痛
• 靶点实验:

  EeAChE:2.66 nM (IC50)

  RatBuChE:19.10 μM (IC50)

• 体外研究: AChE-IN-21(化合物I-8)结合到AChE的催化活性位点和外周阴离子位点[1]。
• 体内研究: AChE-IN-21(化合物I-8)(0-25 mg/kg；例如,每天一次,连续7天)显著逆转东莨菪碱诱导的小鼠记忆障碍[1]。动物模型：体重18-22g的昆明小鼠(雌雄各半)[1]剂量：1.0、5.0和25.0mg/kg给药：灌胃给药,每天一次,连续7天结果：明显阻断东莨菪碱(2mg/kg,i.p.)诱导的记忆障碍。
• 参考文献:

  [1]. Luo L, et al. Design, synthesis and evaluation of phthalide alkyl tertiary amine derivatives as promising acetylcholinesterase inhibitors with high potency and selectivity against Alzheimer's disease. Bioorg Med Chem. 2020 Apr 15;28(8):115400.

AChE-IN-21物理化学性质

• 分子式: C₂₄H₂₉NO₄
• 分子量: 395.49

AChE-IN-21靶点实验

查看更多实验

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实验名称：Inhibition of Electrophorus electricus AChE using acetylcholine iodide as substrate i... 来源：ChEMBL 靶标：Acetylcholinesterase External Id：CHEMBL4617663

实验名称：Antioxidant activity assessed as trolox equivalent of AAPH-induced radical scavenging... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4617665

实验名称：Inhibition of BuChE in rat serum at 50 uM using S-butylthiocholine iodide as substrat... 来源：ChEMBL 靶标：Carboxylic ester hydrolase External Id：CHEMBL4617664

实验名称：Inhibition of recombinant human MAO-A expressed in baculovirus infected BTI insect ce... 来源：ChEMBL 靶标：Amine oxidase [flavin-containing] A External Id：CHEMBL4617667

实验名称：Inhibition of HFIP-pretreated self-induced amyloid beta (1 to 42) (unknown origin) ag... 来源：ChEMBL 靶标：Amyloid-beta precursor protein External Id：CHEMBL4617666

实验名称：Permeability of the compound at 100 ug/ml measured after 18 hrs by PAMPA assay 来源：ChEMBL 靶标：N/A External Id：CHEMBL4617669

实验名称：Inhibition of recombinant human MAO-B expressed in baculovirus infected BTI insect ce... 来源：ChEMBL 靶标：Amine oxidase [flavin-containing] B External Id：CHEMBL4617668

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