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133208-93-2

中文名称 NO-1886
英文名称 NO-1886
CAS 133208-93-2
分子式 C19H20BrN2O4P
分子量 451.25
MOL 文件 133208-93-2.mol
更新日期 2024/06/07 17:54:49
133208-93-2 结构式 133208-93-2 结构式

基本信息

中文别名
化合物NO-1886
4-((4-溴-2-氰基苯基)氨基甲酰基)苄基膦酸二乙酯
英文别名
NO-1886
OPF 009
ibrolipim
Ibrolipim NO-1886
Lipoprotein Lipase Activator
4-diethoxyphosphorylmethyl-N-(4-bromo-2-cyanophenyl)benzamide
Diethyl 4-[(4-bromo-2-cyanophenyl)carbamoyl]benzylphosphonate
N-(4-bromo-2-cyanophenyl)-4-(diethoxyphosphorylmethyl)benzamide
Diethyl 4-[(4-bromo-2-cyanophenyl)carbamoyl]benzylphosphonate, Ibrolipim, OPF 009
Phosphonic acid, [[4-[[(4-bromo-2-cyanophenyl)amino]carbonyl]phenyl]methyl]-, diethyl ester

物理化学性质

熔点160.5-162.1 °C
储存条件Sealed in dry,2-8°C
溶解度二甲基亚砜:≥20mg/mL
形态粉末
颜色灰白色至淡黄色

安全数据

危险性符号(GHS)
GHS06
警示词危险
危险性描述H301
防范说明P301+P310
危险品标志Xi,T
危险类别码36/37/38-25
安全说明26-36-45
危险品运输编号UN 2811 6.1 / PGIII
WGK Germany3

图谱信息

常见问题列表

生物活性
Ibrolipim (NO-1886) 是一种口服活性的脂蛋白脂肪酶 (LPL) 激活剂。 Ibrolipim 可降低血浆甘油三酸酯,增加高密度脂蛋白胆固醇水平。 Ibrolipim 具有肾保护和降血脂的作用。
靶点

Lipoprotein lipase (LPL)

体外研究

Ibrolipim (0.5-10 μM; 0-24 hours; THP-1 macrophage-derived foam cells) treatment increases ABCA1 and ABCG1 expression at translational levels in a dose-dependent and time-dependent manner .
Ibrolipim (0.5-10 μM; 0-24 hours; THP-1 macrophage-derived foam cells) treatment increases ABCA1 and ABCG1 expression at the transcriptional levels in a dose-dependent and time-dependent manner .
Ibrolipim 5 and 50 μmol/L significantly increases cholesterol efflux from THP-1 macrophage-derived foam cells to apoA-I or HDL. LXRα is also upregulated by the Ibrolipim treatment. LXRα small interfering RNA completely abolishes the promotion effect that is induced by Ibrolipim.

Western Blot Analysis

Cell Line: THP-1 macrophage-derived foam cells
Concentration: 0.5 μM, 5 μM, 10 μM
Incubation Time: 0 hour, 6 hours, 12 hours, 24 hours
Result: Increased ABCA1 and ABCG1 translational levels in a dose-dependent and time-dependent manner.

RT-PCR

Cell Line: THP-1 macrophage-derived foam cells
Concentration: 0.5 μM, 5 μM, 10 μM
Incubation Time: 0 hour, 6 hours, 12 hours, 24 hours
Result: Increased ABCA1 and ABCG1 expression at the transcriptional levels in a dose-dependent and time-dependent manner.
体内研究

Ibrolipim (NO-1886; 100 mg/kg; oral administration; daily; for 8 weeks; female Sprague-Dawley rats) treatment decreases accumulation of visceral fat and suppresses the increase in body weight resulting from the ovariectomy. Ibrolipim decreases the respiratory quotient and increases expression of the fatty acid translocase messenger RNA (mRNA) in the liver, soleus muscle, and mesenteric fat. Ibrolipim also increases the expression of fatty acid-binding protein mRNA in the liver and soleus muscle and the expression of the uncoupling protein 3 (UCP3) mRNA in the heart, soleus muscle, and mesenteric fat, but not in the brown adipose tissue.

Animal Model: Female Sprague-Dawley rats (10-week-old; 200-260 g) with experimental ovariectomy treatment
Dosage: 100 mg/kg
Administration: Oral administration; daily; for 8 weeks
Result: Decreased accumulation of visceral fat and suppressed the increase in body weight resulting from the ovariectomy.
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