| 描述 |
ELOVL6-IN-1是一种强效、口服活性和选择性ELOVL6抑制剂。ELOVL6-IN-1剂量依赖性地抑制小鼠ELOVL6活性,IC50值为0.350μM。ELOVL6-IN-1对丙二酰辅酶a(Ki=994nm)和棕榈酰辅酶a以非竞争性方式抑制ELOVL6[1]。
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| 相关类别 |
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| 靶点 |
IC50: 0.35 μM (ELOVL6), Ki: 994 nM (ELOVL6)[1]
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| 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]。
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| 体内研究 |
ELOVL6-IN-1(10mg/kg；p、 o。；0~2小时)显示明显的血浆和肝脏暴露[1]。ELOVL6-IN-1(10和30 mg/kg；p、 o。；0~2小时)可降低肝脏脂质的伸长指数[1]。ELOVL6-IN-1(100 mg/kg；p、 o。；2天)降低肝脏总脂肪酸的伸长指数[1]。动物模型：C57BL/6J小鼠剂量：10mg/kg给药：P.o.结果：显示明显的血浆和肝脏暴露。动物模型：C57BL/6J小鼠剂量：10和30mg/kg给药：P.o.结果：降低肝脏脂质的伸长指数。动物模型：C57BL/6J小鼠剂量：100mg/kg给药：P.o.结果：降低肝脏总脂肪酸的伸长指数。
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| 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.
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