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Ibrolipim

Ibrolipim用途

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名称

[ CAS 号 ]:
133208-93-2

[ 中文名 ]:
脂蛋白脂肪酶激活剂

[ 英文名 ]:
Ibrolipim

[英文别名 ]:

Ibrolipim
NO 1886
OPF-009
Lipoprotein Lipase Activator

Ibrolipim生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 心血管疾病

信号通路 >> 其他 >> 其他

[ 靶点 ]

Lipoprotein lipase (LPL)[1][2][3]

[体外研究]

Ibrolipim(0.5-10μM；0-24小时；THP-1巨噬细胞源性泡沫细胞)治疗以剂量依赖和时间依赖的方式增加翻译水平上ABCA1和ABCG1的表达[1]。Ibrolipim(0.5-10μM；0-24小时；THP-1巨噬细胞源性泡沫细胞)治疗以剂量依赖和时间依赖的方式增加ABCA1和ABCG1在转录水平的表达[1]。Ibrolipim 5和50μmol/L显著增加THP-1巨噬细胞源性泡沫细胞向apoA-I或HDL的胆固醇流出。LXRα也被Ibrolipim治疗上调。LXRα小干扰RNA完全消除了Ibrolipim的促进作用[1]。Western Blot分析[1]细胞系：THP-1巨噬细胞源性泡沫细胞浓度：0.5μM、5μM、10μM孵育时间：0小时、6小时、12小时、24小时结果：ABCA1和ABCG1翻译水平呈剂量依赖性和时间依赖性增加。RT-PCR[1]细胞系：THP-1巨噬细胞源性泡沫细胞浓度：0.5μM、5μM、10μM孵育时间：0小时、6小时、12小时、24小时结果：ABCA1和ABCG1在转录水平上的表达呈剂量依赖性和时间依赖性。

[体内研究]

Ibrolipim(NO-1886；100mg/kg；口服；每日；连续8周；雌性Sprague-Dawley大鼠)治疗可减少内脏脂肪的积累,并抑制因卵巢切除引起的体重增加。Ibrolipim降低呼吸商,增加肝脏、比目鱼肌和肠系膜脂肪中脂肪酸转位酶信使RNA(mRNA)的表达。Ibrolipim还增加了脂肪酸结合蛋白mRNA在肝脏和比目鱼肌中的表达,以及解偶联蛋白3(UCP3)mRNA在心脏、比目鱼肌和肠系膜脂肪中的表达,但在棕色脂肪组织中没有。动物模型：雌性Sprague-Dawley大鼠(10周龄,200-260g),实验性去卵巢治疗[2]剂量：100mg/kg,口服；每日；8周结果：减少内脏脂肪堆积,抑制去卵巢引起的体重增加。

[参考文献]

[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.

Ibrolipim物理化学性质

[ 密度 ]:
1.44g/cm3

[ 沸点 ]:
512.5ºC at 760 mmHg

[ 分子式 ]:
C₁₉H₂₀BrN₂O₄P

[ 分子量 ]:
451.25100

[ 闪点 ]:
263.7ºC

[ 精确质量 ]:
450.03400

[ PSA ]:
98.23000

[ LogP ]:
5.41218

[ 蒸汽压 ]:
1.29E-10mmHg at 25°C

[ 折射率 ]:
1.59

[ 储存条件 ]:
2-8°C

IbrolipimMSDS

详细MSDS(安全技术说明书)

Ibrolipim安全信息

[ 符号 ]:

GHS06

[ 信号词 ]:
Danger

[ 危害声明 ]:
H301

[ 警示性声明 ]:
P301 + P310

[ 危险品运输编码 ]:
UN 2811 6.1 / PGIII

Ibrolipim文献

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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