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156635-05-1

中文名稱 BIBB 515
英文名稱 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 結(jié)構(gòu)式 156635-05-1 結(jié)構(gòu)式

基本信息

中文別名
化合物BIBB 515
英文別名
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

物理化學性質(zhì)

沸點586.5±50.0 °C(Predicted)
密度1.26±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
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)
酸度系數(shù)(pKa)4.72±0.50(Predicted)
形態(tài)白色固體。
顏色White to off-white
BIBB 515價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-116175BIBB 515
BIBB 515
156635-05-11mg500元
2024/11/08HY-116175BIBB 515
BIBB 515
156635-05-15mg1100元
2024/11/08HY-116175BIBB 515
BIBB 515
156635-05-110mg1650元

常見問題列表

生物活性
BIBB 515 是一種有效的,選擇性的和口服活性的 2,3-氧化角鯊烯環(huán)化酶 (OSC) 抑制劑,在大鼠和小鼠中的 ED50 值分別為 0.2-0.5 mg/kg 和 0.36-33.3 mg/kg (1-5 小時)。BIBB 515 主要通過抑制低密度脂蛋白 (LDL) 的產(chǎn)生來發(fā)揮降脂作用。
靶點

2,3-oxidosqualene cyclase (OSC)

體外研究

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.

體內(nèi)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).
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