NO-1886

生物活性靶点体外研究体内研究 NO-1886 试剂级价格

NO-1886

CAS号:133208-93-2
英文名:NO-1886
中文名:NO-1886
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

安全信息

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

NO-1886性质、用途与生产工艺

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.