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FR194738

CAS No. : 204067-52-7

MCE 站：FR194738

产品活性：FR194738 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。

研究领域：Others

作用靶点：Others

In Vitro: In intact HepG2 cells<, FR194738 concentration-dependently inhibits the incorporation of [¹⁴C]acetate into free cholesterol and cholesteryl ester, with IC₅₀s of 4.9 and 8.0 nM, respectively. FR194738 induces intracellular [¹⁴C]squalene accumulation. FR194738 increases the incorporation of [¹⁴C]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 IC₅₀ of 2.1 nM. The IC₅₀s 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 IC₅₀ of 14 nM.

In Vivo: 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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