NO-1886|133208-93-2|-陌孚医药/Medlife

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NO-1886

目录号: PC18735 纯度: ≥98%

CAS No. :133208-93-2

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中文名称

NO-1886

中文别名

4-((4-溴-2-氰基苯基)氨基甲酰基)苄基膦酸二乙酯

英文名称

NO-1886

英文别名

N-(4-Bromo-2-cyanophenyl)-4-(diethoxyphosphorylmethyl)benzamide;N-(4-BROMO-2-CYANOPHENYL)BENZAMIDE;NO-1886;Ibrolipim;Lipoprotein Lipase Activator;NO 1886;OPF-009;Diethyl 4-[(4-bromo-2-cyanophenyl)carbamoyl]benzylphosphonate;OPF 009;4-diethoxyphosphorylmethyl-N-(4-bromo-2-cyanophenyl)benzamide;Diethyl 4-[(4-bromo-2-cyanophenyl)carbamoyl]benzylphosphonate, Ibrolipim, OPF 009

Cas No.

133208-93-2

分子式

C₁₉H₂₀BrN₂O₄P

分子量

451.25

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

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.

性状

Solid

IC50 & Target[1][2]

Lipoprotein lipase (LPL)

体外研究(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 .
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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(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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

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.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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. [Information]

[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. [Information]

[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. [Information]

溶解度数据

体外研究:

DMSO : 125 mg/mL (277.01 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2161 mL	11.0803 mL	22.1607 mL
5 mM	0.4432 mL	2.2161 mL	4.4321 mL
10 mM	0.2216 mL	1.1080 mL	2.2161 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.61 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (4.61 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (4.61 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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