| 中文名称 |
ELOVL6-IN-1
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| 英文名称 |
ELOVL6-IN-1
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| 英文别名 |
3-(2,5-Dihydro-3-methyl-5-oxo-1-phenyl-1H-pyrazol-4-yl)-3,5,6,7-tetrahydro-5,5-dimethyl-1-phenyl-3-(trifluoromethyl)-1H-indole-2,4-dione;ELOVL6-IN-1;5,5-dimethyl-3-(5-methyl-3-oxo-2-phenyl-1H-pyrazol-4-yl)-1-phenyl-3-(trifluoromethyl)-6,7-dihydroindole-2,4-dione
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| Cas No. |
1185736-98-4
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| 分子式 |
C27H24F3N3O3
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| 分子量 |
495.49
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| 包装储存 |
Powder -20°C 3 years;In solvent -80°C 6 months
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| 详情描述 |
ELOVL6-IN-1 是一种有效的,具有口服活性和选择性 ELOVL6 抑制剂。ELOVL6-IN-1 对小鼠 ELOVL6 的抑制作用呈剂量依赖性,IC50 值为 0.350 μM。ELOVL6-IN-1 对丙二酰辅酶 a (Ki=994 nM) 和对棕榈酰辅酶 a 具有非竞争性抑制 ELOVL6 作用。
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| 产品详情 |
ELOVL6-IN-1 是一种有效的,具有口服活性和选择性 ELOVL6 抑制剂。ELOVL6-IN-1 对小鼠 ELOVL6 的抑制作用呈剂量依赖性,IC50 值为 0.350 μM。ELOVL6-IN-1 对丙二酰辅酶 a (Ki=994 nM) 和对棕榈酰辅酶 a 具有非竞争性抑制 ELOVL6 作用。
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| 生物活性 |
ELOVL6-IN-1 is a potent, orally active and selective ELOVL6 inhibitor. ELOVL6-IN-1 dose-dependently inhibits mouse ELOVL6 activities, with an IC 50 value of 0.350 μM. ELOVL6-IN-1 inhibits ELOVL6 in a noncompetitive manner for malonyl-CoA (K i =994 nM) and palmitoyl-CoA.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
IC50: 0.35 μM (ELOVL6), Ki: 994 nM (ELOVL6)
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| 体外研究(In Vitro) |
ELOVL6-IN-1 has sufficiently lipophilic having the potential to penetrate the intracellular space in a passive diffusion manner. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 体内研究(In Vivo) |
ELOVL6-IN-1 (10 mg/kg; p.o.; 0~2 hours) displays appreciable plasma and liver exposure.
ELOVL6-IN-1 (10 and 30 mg/kg; p.o.; 0~2 hours) reduces the elongation index of the liver lipids.
ELOVL6-IN-1 (100 mg/kg; p.o.; 2 days) reduces the elongation index of the total fatty acids of the liver. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Powder -20°C 3 years;In solvent -80°C 6 months
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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
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| 溶解度数据 |
In Vitro: DMSO : 50 mg/mL (100.91 mM; Need ultrasonic)配制储备液
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[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
1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。
2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。