Name | N-(4-bromo-2-cyanophenyl)-4-(diethoxyphosphorylmethyl)benzamide |
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Synonyms |
Ibrolipim
NO 1886 OPF-009 Lipoprotein Lipase Activator |
Description | Ibrolipim (NO-1886) is an orally active lipoprotein lipase (LPL)-promoting agent. Ibrolipim decreases plasma triglycerides, increases high-density lipoprotein cholesterol levels. Ibrolipim has renoprotective and hypolipidemic effects[1][2][3]. |
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Related Catalog | |
Target |
Lipoprotein lipase (LPL)[1][2][3] |
In Vitro | 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 [1]. 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 [1]. 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[1]. Western Blot Analysis[1] 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[1] 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. |
In Vivo | 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[2]. Animal Model: Female Sprague-Dawley rats (10-week-old; 200-260 g) with experimental ovariectomy treatment[2] 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. |
References |
Density | 1.44g/cm3 |
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Boiling Point | 512.5ºC at 760 mmHg |
Molecular Formula | C19H20BrN2O4P |
Molecular Weight | 451.25100 |
Flash Point | 263.7ºC |
Exact Mass | 450.03400 |
PSA | 98.23000 |
LogP | 5.41218 |
Vapour Pressure | 1.29E-10mmHg at 25°C |
Index of Refraction | 1.59 |
Storage condition | 2-8°C |
Symbol |
GHS06 |
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Signal Word | Danger |
Hazard Statements | H301 |
Precautionary Statements | P301 + P310 |
RIDADR | UN 2811 6.1 / PGIII |