FR194738 free base 抑制 HepG2 细胞匀浆中的角鲨烯环氧酶活性,IC50 为 9.8 nM。
产品描述
FR194738 free base inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC50 of 9.8 nM.
体外活性
FR194738 free base potently inhibits squalene epoxidase in HepG2 cell homogenate and liver microsomes in dogs and rats. FR194738 free base inhibits hamster liver microsomal squalene epoxidase activity in a concentration-dependent manner with an IC50 of 14 nM[2]. In intact HepG2 cells, FR194738 free base inhibits the incorporation of [14C]acetate into free cholesterol and cholesteryl ester in a concentration-dependent manner(IC50s = 4.9 and 8.0 nM). FR194738 free base induces intracellular [14C]squalene accumulation and increases the incorporation of [14C]acetate into squalene[3].
体内活性
FR194738 free base reduces the serum levels of total, non high density lipoprotein and high density lipoprotein cholesterol, and triglyceride. In hamsters, FR194738 free base(32 mg/kg) increases HMG-CoA reductase activity by 1.3-fold[2].
Cas No.
204067-45-8
分子式
C27H37NO2S
分子量
439.65
储存和溶解度
DMSO:90mg/mL (204.7mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years