Ibrolipim

[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].

[Related Catalog]:

Research Areas >> Cardiovascular Disease

Signaling Pathways >> Others >> Others

[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]

[1]. Chen SG, et al. Ibrolipim increases ABCA1/G1 expression by the LXRα signaling pathway in THP-1 macrophage-derived foam cells. Acta Pharmacol Sin. 2010 Oct;31(10):1343-9.

[2]. Kano S, et al. NO-1886 (ibrolipim), a lipoprotein lipase-promoting agent, accelerates the expression of UCP3 messenger RNA and ameliorates obesity in ovariectomized rats. Metabolism. 2006 Feb;55(2):151-8.

[3]. Liu Y, et al. Preventive effect of Ibrolipim on suppressing lipid accumulation and increasing lipoprotein lipase in the kidneys of diet-induced diabetic minipigs. Lipids Health Dis. 2011 Jul 16;10:117.

[ Density]:
1.44g/cm3

[ 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

Click to get detail MSDS

[ Symbol ]:

GHS06

[ Signal Word ]:
Danger

[ Hazard Statements ]:
H301

[ Precautionary Statements ]:
P301 + P310

[ RIDADR ]:
UN 2811 6.1 / PGIII

Effects of NO-1886 on inflammation-associated cytokines in high-fat/high-sucrose/high-cholesterol diet-fed miniature pigs.

Eur. J. Pharmacol. 540(1-3) , 139-46, (2006)

Inflammation, closely associated with obesity, is emerging as an important risk factor for the pathophysiological development of atherosclerosis and diabetes mellitus. Fat balance is critical in the a...

NO-1886 suppresses diet-induced insulin resistance and cholesterol accumulation through STAT5-dependent upregulation of IGF1 and CYP7A1.

J. Endocrinol. 1st ed., 204 , 47-56, (2010)

Insulin resistance and dyslipidemia are both considered to be risk factors for metabolic syndrome. Low levels of IGF1 are associated with insulin resistance. Elevation of low-density lipoprotein chole...

Evaluation of induction potency of new drug candidates on CYP1A2 and CYP3A4 using real-time one-step RT-PCR in primary cultures of cryopreserved human hepatocytes.

Drug Metab. Pharmacokinet. 24(5) , 446-50, (2009)

This study evaluates the induction potency of new drug candidates on mRNA levels of CYP1A2 and CYP3A4 in primary cultures of cryopreserved human hepatocytes. Analysis was performed by quantitative rea...

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