Ibrolipim (NO-1886) | LPL Activator

Cas No.:	133208-93-2
Synonyms:	NO-1886,NO 1886,NO1886
SMILES:	BrC1=CC(C#N)=C(C=C1)NC(C2=CC=C(C=C2)CP(OCC)(OCC)=O)=O
Formula:	C₁₉H₂₀BrN₂O₄P
M.Wt:	451.25
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication:	[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.

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].
Target:	Lipoprotein lipase (LPL)[1][2][3]
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.
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.
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.

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