133208-93-2
基本信息
4-((4-溴-2-氰基苯基)氨基甲酰基)苄基膦酸二乙酯
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 Germany | 3 |
常见问题列表
Lipoprotein lipase (LPL)
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. |
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. |