BIBB 515

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BIBB 515 是一种选择性且有效的 OSC 体内抑制剂，在大鼠和小鼠中的 ED50 值分别为 0.2-0.5 和 0.36-33.3 mg/kg。

BIBB 515 is a selective and potent inhibitor of OSC in vivo with an ED50 value of 0.2-0.5 and 0.36-33.3 mg/kg in rats and mice, respectively. 2, 3-Oxidosqualene cyclase (OSC) is an important enzyme in the biosynthesis of animal, plant, and fungal sterols. OSC catalyzes the conversion of (3S)-2, 3-oxidosqualene to lanosterol, a precursor to cholesterol, in mammals and fungi. Total cholesterol was reduced by 19% in normolipemic hamsters at a dose of 55 mg/kg/day for 11 days and 25% in hyperlipemic hamsters at a dose of 148 mg/kg/day for 25 days.

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.

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). Animal Model:Male golden Syrian hyperlipemic hamsters (~100 g) Dosage:16.0 mg/ kg, 49.7 mg/ kg, and 148.2 mg/ kg Administration:Oral administration; daily; for 40 days Result:Dose-dependent lipid-lowering activity was seen in normolipemic hamsters after 11 days treatment (-19% for total cholesterol and -32% for VLDL + LDL cholesterol at 55 mg/kg/day) and in hyperlipemic hamsters after 25 days (-25% for total cholesterol and -59% for LDL-cholesterol at 148 mg/kg/day).

BIBB 515 | BIBB-515 | BIBB515

Others

Other Targets

OSC

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156635-05-1

380.87

C22H21ClN2O2

>98% (HPLC)

In Vitro:?DMSO : 2.5 mg/mL (6.56 mM)

Clc1ccc(cc1)C(=O)N1CCC(CC1)=Cc1ccc(cc1)C1=NCCO1

1-(4-Chlorobenzoyl)-4-((4-(2-oxazolin-2-yl) benzylidene))piperidine

(-20℃)

With Ice Pack

≥ 2 years