hCAI/II-IN-6

• 常用名: hCAI/II-IN-6
• 英文名: hCAI/II-IN-6
• CAS号: 694466-00-7
• 分子量: 388.49
• 密度: N/A
• 沸点: N/A
• 分子式: C₁₉H₂₄N₄O₃S
• 熔点: N/A
• 闪点: N/A

hCAI/II-IN-6用途

hCAI/II-IN-6是一种人体碳酸酐酶(CA)抑制剂。hCAI/II-IN-6对hCA I、hCA II、hCA VII和hCA XII分别选择性抑制Ki值为220、4.9、6.5和＞50000nM的hCA II和hCAⅦ亚型。hCAI/II-IN-6在体内具有抗惊厥活性和抗最大电休克(MES)活性。hCAI/II-IN-6可用于癫痫研究[1]。

hCAI/II-IN-6名称

• 英文名: 694466-00-7

hCAI/II-IN-6生物活性

• 描述: hCAI/II-IN-6是一种人体碳酸酐酶(CA)抑制剂。hCAI/II-IN-6对hCA I、hCA II、hCA VII和hCA XII分别选择性抑制Ki值为220、4.9、6.5和＞50000nM的hCA II和hCAⅦ亚型。hCAI/II-IN-6在体内具有抗惊厥活性和抗最大电休克(MES)活性。hCAI/II-IN-6可用于癫痫研究[1]。
• 相关类别:
  信号通路 >> 代谢酶/蛋白酶 >> 碳酸酐酶
  研究领域 >> 神经疾病
• 体外研究: hCAI/II-IN-6(0-50μM)抑制hCA I、hCA II、hCA VII和hCA XII活性,Ki值分别为220、4.9、6.5和＞50000nM[1]。
• 体内研究: hCAI/II-IN-6(30-100mg/kg；一次性腹腔注射)在体内显示出良好的抗惊厥作用[1]。hCAI/II-IN-6(30 mg/kg；p.o.一次)在体内显示抗MES活性[1]。动物模型：瑞士白化小鼠[1]剂量：30和100 mg/kg给药：腹腔注射；30～100 mg/kg一次。结果：癫痫发作减轻,抗惊厥效果好,在抗惊厥定量研究中ED50为13.7 mg/kg。动物模型：Wistar白化大鼠[1]剂量：30mg/kg给药：口服灌胃；30 mg/kg一次。结果：在给药后1小时内显示出抗MES活性,对癫痫发作有显著保护作用,1小时后作用减弱。
• 参考文献:

  [1]. Mishra CB, et al. Discovery of Benzenesulfonamides with Potent Human Carbonic Anhydrase Inhibitory and Effective Anticonvulsant Action: Design, Synthesis, and Pharmacological Assessment. J Med Chem. 2017 Mar 23;60(6):2456-2469.

hCAI/II-IN-6物理化学性质

• 分子式: C₁₉H₂₄N₄O₃S
• 分子量: 388.49
• InChIKey: VMBFFHZLNCWIEC-UHFFFAOYSA-N
• SMILES: NS(=O)(=O)c1ccc(NC(=O)CN2CCN(Cc3ccccc3)CC2)cc1
• 储存条件: -20°C

hCAI/II-IN-6靶点实验

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实验名称：Fluorescence-based cell-based primary high throughput screening assay to identify pos... 来源：The Scripps Research Institute Molecular Screening Center 靶标：muscarinic acetylcholine receptor M1 [Homo sapiens] External Id：CHRM1_PAM_FLUO8_1536_1X%ACT PRUN

实验名称：Fluorescence polarization-based biochemical high throughput primary assay to identify... 来源：The Scripps Research Institute Molecular Screening Center 靶标：RecName: Full=Sialate O-acetylesterase; AltName: Full=H-Lse; AltName: Full=Sialic acid-specific 9-O-acetylesterase; Flags: Precursor [Homo sapiens] External Id：SIAE_INH_FP_1536_1X%INH PRUN

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