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BIBB 515

CAS No. : 156635-05-1

MCE 站：BIBB 515

产品活性：BIBB 515 是一种有效的，选择性的和口服活性的 2,3-氧化角鲨烯环化酶 (OSC) 抑制剂，在大鼠和小鼠中的 ED₅₀ 值分别为 0.2-0.5 mg/kg 和 0.36-33.3 mg/kg (1-5 小时)。BIBB 515 主要通过抑制低密度脂蛋白 (LDL) 的产生来发挥降脂作用。

研究领域：Others

作用靶点：Others

In Vitro: Sterol synthesis, 2,3-oxidosqualene cyclase activity, HMGCoA reductase activity, and the specificity of BIBB 51 5 versus 2,3-oxidosqualene cyclase are measured in intact HepG2 cells or cell homogenates.Concentration-dependent inhibition of cholesterol biosynthesis by BIBB 515 as monitored by [¹⁴C]-acetate incorporation into digitonin precipitable sterols could be demonstrated in HepG2 cells (ED₅₀ = 4.11 nM). A similar inhibition of OSC activity (ED₅₀= 8.69 nM) is seen in HepC2 cell homogenates. No inhibition of HMGCoA reductasc could be measured in HepG2 cell homogenates at concentrations of BIBB 515 up to 1 and 10 μM.

In Vivo: BIBB 515 (16.0-148.2 mg/ kg; oral administration; daily; for 40 days; male golden Syrian hyperlipemic hamsters) treatment shows dose-dependent lipid-lowering activity in normolipemic hamsters (-19% for total cholesterol and -32% for VLDL + LDL cholesterol) and in hyperlipemic hamsters (-25% for total cholesterol and -59% for LDL-cholesterol).

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