156635-05-1

中文名称 BIBB 515

英文名称 BIBB 515

CAS 156635-05-1

分子式 C22H21ClN2O2

分子量 380.87

MOL 文件 156635-05-1.mol

156635-05-1 结构式

基本信息物理化学性质图谱信息 BIBB 515价格(试剂级) 常见问题列表

基本信息

中文别名

化合物BIBB 515

英文别名

BIBB 515
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

物理化学性质

沸点586.5±50.0 °C(Predicted)

密度1.26±0.1 g/cm3(Predicted)

储存条件-20°C储存

溶解度DMSO:1.38(Max Conc. mg/mL);3.62(Max Conc. mM)
DMF:0.3(Max Conc. mg/mL);0.79(Max Conc. mM)
Ethanol:0.15(Max Conc. mg/mL);0.39(Max Conc. mM)

酸度系数(pKa)4.72±0.50(Predicted)

形态白色固体。

颜色White to off-white

图谱信息

BIBB 515(156635-05-1)核磁图(¹HNMR)

BIBB 515价格(试剂级)

报价日期	产品编号	产品名称	CAS号	包装	价格
2024/08/19	HY-116175	BIBB 515 BIBB 515	156635-05-1	1mg	500元
2024/08/19	HY-116175	BIBB 515 BIBB 515	156635-05-1	5mg	1100元
2024/08/19	HY-116175	BIBB 515 BIBB 515	156635-05-1	10mg	1650元

常见问题列表

生物活性

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。

靶点

2,3-oxidosqualene cyclase (OSC)

体外研究

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.

体内研究

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).