BIBB 515
| 中文名称 | BIBB 515 |
|---|---|
| 中文同义词 | 化合物BIBB 515 |
| 英文名称 | BIBB 515 |
| 英文同义词 | BIBB 515;(4-chlorophenyl)-[4-[[4-(4,5-dihydro-1,3-oxazol-2-yl)phenyl]methylidene]piperidin-1-yl]methanone;Methanone, (4-chlorophenyl)[4-[[4-(4,5-dihydro-2-oxazolyl)phenyl]methylene]-1-piperidinyl]-;BIBB 515,Inhibitor,OSC,inhibit,cyclase,effect,metabolism,LDL,BIBB-515,2,3-oxidosqualene,BIBB515,sterol,cholesterol,lipid-lowering |
| CAS号 | 156635-05-1 |
| 分子式 | C22H21ClN2O2 |
| 分子量 | 380.87 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 156635-05-1.mol |
| 结构式 |  |
BIBB 515 性质
| 沸点 | 586.5±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.26±0.1 g/cm3(Predicted) |
| 储存条件 | Store at -20°C |
| 溶解度 | DMSO:1.38(最大浓度 mg/mL);3.62(最大浓度 mM) DMF:0.3(最大浓度 mg/mL);0.79(最大浓度 mM) 乙醇:0.15(最大浓度 mg/mL);0.39(最大浓度 mM) |
| 形态 | 白色固体。 |
| 酸度系数(pKa) | 4.72±0.50(Predicted) |
| 颜色 | 白色至米白色 |
2,3-oxidosqualene cyclase (OSC)
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 [ 14 C]-acetate incorporation into digitonin precipitable sterols could be demonstrated in HepG2 cells (ED 50 = 4.11 nM). A similar inhibition of OSC activity (ED 50 = 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). |
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-116175 | BIBB 515 BIBB 515 | 156635-05-1 | 1mg | 500元 |
| 2024/04/30 | HY-116175 | BIBB 515 BIBB 515 | 156635-05-1 | 5mg | 1100元 |