712346-06-0

• 常用中文名：ELOVL6-IN-3
• 常用英文名：ELOVL6-IN-3
• CAS号：712346-06-0
• 分子式：C₂₇H₂₄F₃N₃O₃
• 分子量：495.49
• 相关类别： 研究领域 神经疾病
• 发布时间：2023-10-23 17:56:41
• 更新时间：2025-09-18 13:58:37
• ELOVL6-IN-1是一种强效、口服活性和选择性的ELOVL6抑制剂。ELOVL6-IN-1剂量依赖性抑制小鼠ELOVL6活性,IC50值为0.350μM。ELOVL6-IN-1对丙二酰辅酶a(Ki=994 nM)和棕榈酰辅酶a以非竞争性方式抑制ELOVL6[1]。

名称

• 英文名: ELOVL6-IN-3

物化性质

• 分子式: C₂₇H₂₄F₃N₃O₃
• 分子量: 495.49

生物活性

• 描述: ELOVL6-IN-1是一种强效、口服活性和选择性的ELOVL6抑制剂。ELOVL6-IN-1剂量依赖性抑制小鼠ELOVL6活性,IC50值为0.350μM。ELOVL6-IN-1对丙二酰辅酶a(Ki=994 nM)和棕榈酰辅酶a以非竞争性方式抑制ELOVL6[1]。
• 相关类别:
  信号通路 >> 其他 >> 其他
  研究领域 >> 神经疾病
• 靶点:

  IC50: 0.35 μM (ELOVL6), Ki: 994 nM (ELOVL6)[1]

• 体外研究: ELOVL6-IN-1具有足够的亲脂性,具有以被动扩散方式穿透细胞内空间的潜力[1]
• 体内研究: ELOVL6-IN-1(10 mg/kg口服；0~2小时) 显示出明显的血浆和肝脏暴露[1] ELOVL6-IN-1(10和 30mg/kg口服；0~2小时)降低肝脂质的延伸指数[1] ELOVL6-IN-1(100 mg/kg口服；2.天) 降低肝脏总脂肪酸的延伸指数[1]
• 参考文献:

  [1]. Shimamura K, et al. 5,5-Dimethyl-3-(5-methyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)-1-phenyl-3-(trifluoromethyl)-3,5,6,7-tetrahydro-1H-indole-2,4-dione, a potent inhibitor for mammalian elongase of long-chain fatty acids family 6: examination of its potential utility as a pharmacological tool. J Pharmacol Exp Ther. 2009;330(1):249-256.

  [2]. Takahashi T, Nagase T, Sasaki T, et al. Synthesis and evaluation of a novel indoledione class of long chain fatty acid elongase 6 (ELOVL6) inhibitors. J Med Chem. 2009;52(10):3142-3145.

  [3]. Zheng Junxia, Wu Zhiwei, Dai Mibei, Xu Zhihui, Li Xiaomei, Zhu Shanshan, Lin Chuyun, Hu Peijian, Zhang Luo, Huang Huarong, Zhao Suqing, Zhang Kun and Sun Pinghua, Quantitative Structure Activity Relationship Studies on a Novel Indolediones as Long Chain Fatty Acid Elongase 6 (ELOVL6) Inhibitors, Letters in Drug Design & Discovery 2011; 8(5) .