204067-45-8
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- CAS号:
- 204067-45-8
- 英文名:
- FR194738 free base
- 英文别名:
- FR194738 free base;FR194738 free base,FR-194738 free base;Benzenemethanamine, N-[(2E)-6,6-dimethyl-2-hepten-4-yn-1-yl]-N-ethyl-3-[2-methyl-2-(3-thienylmethoxy)propoxy]-
- 中文名:
- 204067-45-8
- 中文别名:
- 化合物 T11321;化合物FR194738 FREE BASE
- CBNumber:
- CB54797059
- 分子式:
- C27H37NO2S
- 分子量:
- 439.65
- MOL File:
- 204067-45-8.mol
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204067-45-8化学性质
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沸点:
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538.0±50.0 °C(Predicted)
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密度:
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1.051±0.06 g/cm3(Predicted)
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储存条件:
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Store at -20°C
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溶解度:
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Soluble in DMSO
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形态:
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Viscous Liquid
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酸度系数(pKa):
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7.09±0.50(Predicted)
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颜色:
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Colorless to light yellow
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204067-45-8性质、用途与生产工艺
FR194738 free base 是一种角鲨烯环氧化酶 (squalene epoxidase) 抑制剂。在 HepG2 细胞匀浆中, FR194738 抑制角鲨烯环氧酶活性,IC50 值为 9.8 nM。
IC50: 9.8 nM (squalene epoxidase, in HepG2 cell homogenates)
In intact HepG2 cells, FR194738 concentration-dependently inhibits the incorporation of [
14
C]acetate into free cholesterol and cholesteryl ester, with IC
50
s of 4.9 and 8.0 nM, respectively. FR194738 induces intracellular [
14
C]squalene accumulation. FR194738 increases the incorporation of [
14
C]acetate into squalene, an intermediate of cholesterol synthesis. FR194738 potently inhibits squalene epoxidase (SE) in HepG2 cell homogenate and liver microsomes in dogs and rats. The inhibitory effect of FR194738 in comparison to the HMG-CoA reductase inhibitors, Simvastatin, Fluvastatin and Pravastatin, on cholesterol biosynthesis in HepG2 cells is examined. Among these compounds, FR194738 is the most potent, with an IC
50
of 2.1 nM. The IC
50
s of Simvastatin, Fluvastatin and Pravastatin are 40, 28 and 5100 nM, respectively. FR194738 inhibits hamster liver microsomal squalene epoxidase activity in a concentration-dependent manner with an IC
50
of 14 nM.
Serum lipid levels in hamsters after daily administration of FR194738 and Pravastatin for 10 d are measured. FR194738 reduces the serum levels of total, non high density lipoprotein (HDL) and HDL cholesterol, and triglyceride. Treatment of hamsters with FR194738 increases HMG-CoA reductase activity by 1.3-fold at 32 mg/kg compared to the control group and does not significantly change that at 100 mg/kg.
204067-45-8
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下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/08/19 | HY-100303 | 204067-45-8 FR194738 free base | 204067-45-8 | 1 mg | 2285元 |
2024/08/19 | HY-100303 | FR194738 free base | | 5 mg | 5000元 |
204067-45-8, 204067-45-8 相关搜索:
- 抑制剂
- C27H37NO2S
- 化合物FR194738 FREE BASE
- 化合物 T11321
- 204067-45-8
- FR194738 free base,FR-194738 free base
- Benzenemethanamine, N-[(2E)-6,6-dimethyl-2-hepten-4-yn-1-yl]-N-ethyl-3-[2-methyl-2-(3-thienylmethoxy)propoxy]-
- FR194738 free base