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204067-45-8

中文名稱 204067-45-8
英文名稱 FR194738 free base
CAS 204067-45-8
分子式 C27H37NO2S
分子量 439.65
MOL 文件 204067-45-8.mol
204067-45-8 結(jié)構(gòu)式 204067-45-8 結(jié)構(gòu)式

基本信息

中文別名
化合物 T11321
化合物FR194738 FREE BASE
英文別名
FR194738 free base
Benzenemethanamine, N-[(2E)-6,6-dimethyl-2-hepten-4-yn-1-yl]-N-ethyl-3-[2-methyl-2-(3-thienylmethoxy)propoxy]-

物理化學(xué)性質(zhì)

沸點(diǎn)538.0±50.0 °C(Predicted)
密度1.051±0.06 g/cm3(Predicted)
儲(chǔ)存條件-20°C儲(chǔ)存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)7.09±0.50(Predicted)
形態(tài)Viscous Liquid
顏色Colorless to light yellow

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
防范說(shuō)明P261-P305+P351+P338

常見(jiàn)問(wèn)題列表

生物活性
FR194738 free base 是一種角鯊烯環(huán)氧化酶 (squalene epoxidase) 抑制劑。在 HepG2 細(xì)胞勻漿中, FR194738 抑制角鯊烯環(huán)氧酶活性,IC50 值為 9.8 nM。
靶點(diǎn)

IC50: 9.8 nM (squalene epoxidase, in HepG2 cell homogenates)

體外研究

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.

體內(nèi)研究

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.

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