FR194738 是一种角鲨烯环氧酶抑制剂,在 HepG2 细胞匀浆中的 IC50 为 9.8 nM。
产品描述
FR194738 is an inhibitor of squalene epoxidase with an IC50 of 9.8 nM in HepG2 cell homogenates.
体外活性
FR194738 inhibits cholesterol biosynthesis in HepG2 cells (IC50 = 2.1 nM)[1]. FR194738 concentration-dependently inhibits hamster liver microsomal squalene epoxidase activity (IC50 = 14 nM)[2]. FR194738 inhibits the incorporation of [14C]acetate in intact HepG2 cells into free cholesterol (IC50 = 4.9 nM) and cholesteryl ester (IC50 = 8.0 nM) in a concentration-dependent manner. FR194738 induces intracellular [14C]squalene accumulation and increases the incorporation of [14C]acetate into squalene[3].
体内活性
FR194738 (32 and 100 mg/kg) reduces the serum levels of total, non HDL and HDL cholesterol, and triglyceride and increases HMG-CoA reductase activity by 1.3-fold at a dose of 32 mg/kg[2].
Cas No.
204067-52-7
分子式
C27H38ClNO2S
分子量
476.11
别名
FR194738
储存和溶解度
DMSO:200 mg/mL (420.1 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years