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NB-598 Sale

(Synonyms: NB 598;NB598) 目录号 : GC19467

NB-598 是一种强效竞争性角鲨烯环氧酶 (SE) 抑制剂,通过法尼醇途径抑制甘油三酯的生物合成。

NB-598 Chemical Structure

Cas No.:131060-14-5

规格 价格 库存 购买数量
2mg
¥1,275.00
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5mg
¥2,016.00
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10mg
¥3,024.00
现货
50mg
¥9,240.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Kinase experiment:

Caco-2 cells are grown in a 58 cm2 plastic dish with medium A for 13 days. The cells are washed with medium B, and then cultured with medium B including cholesterol-micelle and each compound. The compound is dissolved in Me2SO, and the final concentration of Me2SO is 0.1%(v/v). After 18 hr of incubation, the cells are washed extensively with phosphate-buffered saline (PBS) to remove the compound. Microsomes are prepared as described above. The reaction mixture (0.2 mL) consisted of 0.1 mg microsomes, 0.25% BSA and 40 PM [14C]oleoyl CoA in buffer A. To avoid the effects of endogenous cholesterol, liposome (2 mol of cholesterol: 1 mol of phosphatidylcholine) [15] is added to the reaction mixture. The microsomes are preincubated for 1 hr with or without exogenous cholesterol, and ACAT activity is determined as described above.

References:

[1]. Xia F, et al. Inhibition of cholesterol biosynthesis impairs insulin secretion and voltage-gated calcium channel function in pancreatic beta-cells. Endocrinology. 2008 Oct;149(10):5136-45.
[2]. Horie M, et al. Effects of NB-598, a potent squalene epoxidase inhibitor, on the apical membrane uptake of cholesterol and basolateral membrane secretion of lipids in Caco-2 cells. Biochem Pharmacol. 1993 Jul 20;46(2):297-305.
[3]. Horie M, et al. An inhibitor of squalene epoxidase, NB-598, suppresses the secretion of cholesterol and triacylglycerol and simultaneously reduces apolipoprotein B in HepG2 cells. Biochim Biophys Acta. 1993 May 20;1168(1):45-51.

产品描述

NB-598 is a potent and competitive inhibitor of squalene epoxidase (SE), and suppresses triglyceride biosynthesis through the farnesol pathway.

NB598 (10 μM) causes a 36±7% reduction in total cholesterol level of MIN6 cells. NB598 causes a significant decrease in cholesterol by 49±2%, 46±7%, and 48±2% from PM, ER, and SG, respectively. NB598 dose-dependently inhibits insulin secretion under both basal (1 mM glucose) and glucose-stimulated (16.7 mM glucose) conditions. NB598 at concentrations up to 10 μM does not affect peak outward KV currents or the voltage dependence of activation but increases current inactivation[1]. NB-598 (10 μM) inhibits the synthesis of sterol and sterol ester from [14C]acetate without affecting the synthesis of other lipids such as phospholipids (PL), free fatty acids (FFA) and triacylglycerol (TG). In the absence of exogenous liposomal cholesterol, NB-598 reduces ACAT activity by 31%. NB-598 reduces ACAT activity by 22% even in the presence of a 600 PM concentration of liposomal cholesterol[2]. NB-598 suppresses the secretion of cholesterol and triacylglycerol from HepG2 cells into the medium[3].

References:
[1]. Xia F, et al. Inhibition of cholesterol biosynthesis impairs insulin secretion and voltage-gated calcium channel function in pancreatic beta-cells. Endocrinology. 2008 Oct;149(10):5136-45.
[2]. Horie M, et al. Effects of NB-598, a potent squalene epoxidase inhibitor, on the apical membrane uptake of cholesterol and basolateral membrane secretion of lipids in Caco-2 cells. Biochem Pharmacol. 1993 Jul 20;46(2):297-305.
[3]. Horie M, et al. An inhibitor of squalene epoxidase, NB-598, suppresses the secretion of cholesterol and triacylglycerol and simultaneously reduces apolipoprotein B in HepG2 cells. Biochim Biophys Acta. 1993 May 20;1168(1):45-51.

Chemical Properties

Cas No. 131060-14-5 SDF
别名 NB 598;NB598
化学名 (E)-N-(3-([3,3'-bithiophen]-5-ylmethoxy)benzyl)-N-ethyl-6,6-dimethylhept-2-en-4-yn-1-amine
Canonical SMILES CCN(CC1=CC(OCC2=CC(C3=CSC=C3)=CS2)=CC=C1)C/C=C/C#CC(C)(C)C
分子式 C27H31NOS2 分子量 449.67
溶解度 insoluble in Water;>49.3 mg/mL in EtOH with gentle warming;>54 mg/mL in DMSO with gentle warming 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.2239 mL 11.1193 mL 22.2385 mL
5 mM 0.4448 mL 2.2239 mL 4.4477 mL
10 mM 0.2224 mL 1.1119 mL 2.2239 mL
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