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  3. NB-598

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 Chemical Structure

NB-598 Chemical Structure

CAS No. : 131060-14-5

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Top Publications Citing Use of Products

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

    449.67

    Formula

    C27H31NOS2

    CAS 号
    性状

    固体

    颜色

    Off-white to light yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 50 mg/mL (111.19 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 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
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,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,请在6个月内使用,-20°C储存时,请在1个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 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

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: 2.5 mg/mL (5.56 mM); 悬浊液; 超声助溶

      此方案可获得 2.5 mg/mL的均匀悬浊液,悬浊液可用于口服和腹腔注射。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.56 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。
    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 98.29%

    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

    NB-598 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,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,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2239 mL 11.1193 mL 22.2385 mL 55.5963 mL
    5 mM 0.4448 mL 2.2239 mL 4.4477 mL 11.1193 mL
    10 mM 0.2224 mL 1.1119 mL 2.2239 mL 5.5596 mL
    15 mM 0.1483 mL 0.7413 mL 1.4826 mL 3.7064 mL
    20 mM 0.1112 mL 0.5560 mL 1.1119 mL 2.7798 mL
    25 mM 0.0890 mL 0.4448 mL 0.8895 mL 2.2239 mL
    30 mM 0.0741 mL 0.3706 mL 0.7413 mL 1.8532 mL
    40 mM 0.0556 mL 0.2780 mL 0.5560 mL 1.3899 mL
    50 mM 0.0445 mL 0.2224 mL 0.4448 mL 1.1119 mL
    60 mM 0.0371 mL 0.1853 mL 0.3706 mL 0.9266 mL
    80 mM 0.0278 mL 0.1390 mL 0.2780 mL 0.6950 mL
    100 mM 0.0222 mL 0.1112 mL 0.2224 mL 0.5560 mL
    Help & FAQs
    • 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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    Inquiry Information

    产品名称:
    NB-598
    目录号:
    HY-16343
    需求量: