156635-05-1
基本信息
Methanone, (4-chlorophenyl)[4-[[4-(4,5-dihydro-2-oxazolyl)phenyl]methylene]-1-piperidinyl]-
(4-chlorophenyl)-[4-[[4-(4,5-dihydro-1,3-oxazol-2-yl)phenyl]methylidene]piperidin-1-yl]methanone
物理化學性質(zhì)
DMF:0.3(Max Conc. mg/mL);0.79(Max Conc. mM)
Ethanol:0.15(Max Conc. mg/mL);0.39(Max Conc. mM)
報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
2024/11/08 | HY-116175 | BIBB 515 BIBB 515 | 156635-05-1 | 1mg | 500元 |
2024/11/08 | HY-116175 | BIBB 515 BIBB 515 | 156635-05-1 | 5mg | 1100元 |
2024/11/08 | HY-116175 | BIBB 515 BIBB 515 | 156635-05-1 | 10mg | 1650元 |
常見問題列表
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). |