NB-598 (Maleate)
Names
[ CAS No. ]:
155294-62-5
[ Name ]:
NB-598 (Maleate)
[Synonym ]:
(E)-N-(6,6-dimethyl-2-hepten-4-ynyl)-N-ethyl-3-[4-(3-thienyl)-2-thienylmethyloxy]benzylamine maleate
NB-598 (Maleate)
Biological Activity
[Description]:
NB-598 (Maleate) is a potent and competitive inhibitor of squalene epoxidase (SE), and suppresses triglyceride biosynthesis through the farnesol pathway.
[Related Catalog]:
[In Vitro]
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].
[Kinase Assay]
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]
[Related Small Molecules]
Captisol
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Cyclosporin A
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H2DCFDA
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0MPTP hydrochloride
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GW4869
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Etomoxir
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TD139
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Mitoquinone mesylate
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GSK2795039
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JC-1
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BAPTA-AM
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AP 20187
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Setanaxib (GKT137831)
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D-Luciferin
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Crotaline
Chemical & Physical Properties
[ Molecular Formula ]:
C31H35NO5S2
[ Molecular Weight ]:
565.74300
[ Exact Mass ]:
565.19600
[ PSA ]:
143.55000
[ LogP ]:
7.19500
[ Storage condition ]:
2-8℃