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  3. NB-598 hydrochloride

NB-598是鲨烯环氧化酶(SE)竞争性抑制剂,能抑制甘油三酯的生物合成。

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NB-598 hydrochloride Chemical Structure

NB-598 hydrochloride Chemical Structure

CAS No. : 136719-25-0

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Top Publications Citing Use of Products

    NB-598 hydrochloride purchased from MCE. Usage Cited in: J Steroid Biochem Mol Biol. 2015 Aug;152:34-44.  [Abstract]

    GC/MS quantitation of squalene (A) and cholesterol (B) extracted from confluent 6-well plates cell layers from SEBO662 AR+ treated or not (Ctrl) with 10 nM DHT, in the presence or not of the squalene epoxidase inhibitor NB-598 (10 μM). Treatment time is 7 days. Squalene is only detected in NB-598-treated cell layers. DHT significantly increases squalene without significantly modifying cholesterol.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    NB-598 hydrochloride is a potent and competitive inhibitor of squalene epoxidase (SE), and suppresses triglyceride biosynthesis through the farnesol pathway. NB-598 (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

    IC50 & Target

    squalene epoxidase

    体外研究
    (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].

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

    分子量

    486.13

    Formula

    C27H32ClNOS2

    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.

    纯度 & 产品资料
    参考文献
    Kinase Assay
    [2]

    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.

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

    参考文献

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
    NB-598 hydrochloride
    目录号:
    HY-16343A
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