NO-1886
|
|
|
- CAS号:
- 133208-93-2
- 英文名:
- NO-1886
- 英文别名:
- OPF 009;NO-1886;ibrolipim;Ibrolipim NO-1886;NO-1886 Ibrolipim;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)amino]carbonyl]phenyl]methyl]phosphonate
- 中文名:
- NO-1886
- 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
- CBNumber:
- CB5497355
- 分子式:
- C19H20BrN2O4P
- 分子量:
- 451.25
- MOL File:
- 133208-93-2.mol
|
|
|
NO-1886化学性质
-
熔点:
-
160.5-162.1 °C
-
|
-
沸点:
-
512.5±50.0 °C(Predicted)
-
|
-
密度:
-
1.44±0.1 g/cm3(Predicted)
-
|
-
储存条件:
-
Sealed in dry,2-8°C
-
|
-
溶解度:
-
DMSO: ≥20mg/mL
-
|
-
形态:
-
powder
-
|
-
酸度系数(pKa):
-
11.51±0.70(Predicted)
-
|
-
颜色:
-
off-white to pale yellow
-
|
NO-1886性质、用途与生产工艺
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。
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.
|
NO-1886
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/04/30 | HY-117549 | Ibrolipim | | 1 mg | 200元 |
| 2024/04/30 | HY-117549 | NO-1886
Ibrolipim | 133208-93-2 | 5mg | 400元 |
133208-93-2, NO-1886 相关搜索:
- 药靶配体
- C19H20BrN2O4P
- 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
- 133208-93-2
- Diethyl [[4-[[(4-bromo-2-cyanophenyl)amino]carbonyl]phenyl]methyl]phosphonate
- NO-1886 Ibrolipim
- obesity,fatty,inhibit,NO 1886,Ibrolipim,acid,NO1886,Inhibitor,lipoprotein,lipase,Antihyperlipidemic,UCP3,LDL-C,LXRα,HDL-C
- Phosphonic acid, [[4-[[(4-bromo-2-cyanophenyl)amino]carbonyl]phenyl]methyl]-, diethyl ester
- N-(4-bromo-2-cyanophenyl)-4-(diethoxyphosphorylmethyl)benzamide
- Ibrolipim NO-1886
- Diethyl 4-[(4-bromo-2-cyanophenyl)carbamoyl]benzylphosphonate, Ibrolipim, OPF 009
- ibrolipim
- 4-diethoxyphosphorylmethyl-N-(4-bromo-2-cyanophenyl)benzamide
- Diethyl 4-[(4-bromo-2-cyanophenyl)carbamoyl]benzylphosphonate
- NO-1886
- Lipoprotein Lipase Activator
- OPF 009