1. Membrane Transporter/Ion Channel
  2. Na+/Ca2+ Exchanger
  3. SEA0400

SEA0400 是一种新颖的,具有选择性的 Na+-Ca2+ exchanger 抑制剂,在培养的神经元、星形胶质细胞和小胶质细胞中,能够抑制 Na+-依赖性 Ca2+ 的吸收,IC50 值为 5-33 nM。

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SEA0400 Chemical Structure

SEA0400 Chemical Structure

CAS No. : 223104-29-8

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     可免费申领三个不同产品的试用装。

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1540
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1 mg ¥589
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5 mg ¥1400
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10 mg ¥2240
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25 mg ¥4049
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50 mg ¥5871
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100 mg ¥8219
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200 mg   询价  
500 mg   询价  

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Top Publications Citing Use of Products

    SEA0400 purchased from MCE. Usage Cited in: Cell Signal. 2017 May 20;37:12-30.  [Abstract]

    HUVECs are incubated with the indicated concentrations of a second reverse-mode NCX inhibitor, SEA0400, for 30 min prior to stimulation with OAG (100 μM) for 5 min. ERK1/2 activation is assessed by Western blot.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    SEA0400 is a novel and selective inhibitor of the Na+-Ca2+ exchanger (NCX), inhibiting Na+-dependent Ca2+ uptake in cultured neurons, astrocytes, and microglia with IC50s of from 5 to 33 nM.

    IC50 & Target

    IC50: 5-33 nM (NCX)

    体外研究
    (In Vitro)

    SEA0400 inhibits Na+-dependent 45Ca2+ uptake in cultured neurons, astrocytes, and microglia. IC50 values of SEA0400 are 33 nM (neurons), 5.0 nM (astrocytes), and 8.3 nM (microglia)[1]. SEA0400 prevents sodium nitroprusside (SNP) to increase ERK and p38 MAPK phosphorylation, and production of reactive oxygen species (ROS) in an extracellular Ca2+-dependent manner[2].

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

    体内研究
    (In Vivo)

    SEA0400 (3 mg/kg + 3 mg/kg/h for 2 h, i.v.) attenuates the infarct volume in the cerebral cortex and striatum, does not affect the mean the regional cortical blood flow in anesthetized rats[1]. SEA0400 protects against the dopaminergic neurotoxicity (determined by dopamine levels in the midbrain and striatum, tyrosine hydroxylase immunoreactivity in the substantia nigra and striatum, striatal dopamine release, and motor deficits) in MPTP-treated C57BL/6J mice[3].

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

    分子量

    371.38

    Formula

    C21H19F2NO3

    CAS 号
    性状

    固体

    颜色

    White to khaki

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 32 mg/mL (86.17 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.6927 mL 13.4633 mL 26.9266 mL
    5 mM 0.5385 mL 2.6927 mL 5.3853 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 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    40% PEG300    5% Tween-80    45% Saline

      Solubility: 2.5 mg/mL (6.73 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 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

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

      Solubility: ≥ 2.5 mg/mL (6.73 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: 99.96%

    参考文献
    Kinase Assay
    [1]

    Na+-Ca2+ exchange activity is determined by assaying Na+-dependent 45Ca2+ uptake as reported previously. Briefly, the cells are preincubated in Hanks' balanced saline solution (HBSS) for 20 min, and the medium is switched to HBSS containing 45Ca2+ and incubated for 5 min. To increase intracellular Na+ concentration, 1 mM ouabain plus 20 μM monensin (for astrocytes and microglia) and 10 μM monensin (for neurons) are used. Monensin is added simultaneously with the isotope. Ouabain is added 5 min before monensin in astrocytes and microglia. SEA0400 and KB-R7943 are added 5 min before monensin and present during 45Ca2+ uptake reaction.

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

    Cell Assay
    [1]

    Cells, plated in 96-well plastic tissue culture plates, are incubated at 37°C for 30 min in normal or Ca2+-free HBSS containing 10 μM H2DCF-DA and 0.25 μg/mL Cremophor EL, and then rinsed twice with normal HBSS to remove excess dye. The cells are reperfused in normal HBSS for 1 h, and the conversion of H2DCF-DA to its fluorescent product dichlorofluorescein by ROS, presumably H2O2 and hydroxyl radical, is determined with excitation at 485 nm and emission at 535 nm using a Wallac Multilabel counter. ROS production is expressed as a percentage of control cells. The linearity and sensitivity of ROS assay are confirmed using H2O2 prior to the experiment. SEA0400 at the indicated concentrations is added 10 min before Ca2+ reperfusion and present until assay. 

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

    Animal Administration
    [1]

    Male Sprague-Dawley rats, weighing 289 to 325 g, are anesthetized with 1 to 2% halothane. A catheter is inserted into the femoral artery and connected to a pressure transducer to record blood pressure. Regional cortical blood flow is measured by a laser Doppler flowmeter, with probe placement at 2 mm posterior and 6 mm lateral to the bregma. SEA0400 or its vehicle with an equivalent volume is i.v. injected at 3 mg/kg and then infused at 3 mg/kg/h for 2 h under normal conditions without MCA occlusion.

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

    参考文献

    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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.6927 mL 13.4633 mL 26.9266 mL 67.3165 mL
    5 mM 0.5385 mL 2.6927 mL 5.3853 mL 13.4633 mL
    10 mM 0.2693 mL 1.3463 mL 2.6927 mL 6.7316 mL
    15 mM 0.1795 mL 0.8976 mL 1.7951 mL 4.4878 mL
    20 mM 0.1346 mL 0.6732 mL 1.3463 mL 3.3658 mL
    25 mM 0.1077 mL 0.5385 mL 1.0771 mL 2.6927 mL
    30 mM 0.0898 mL 0.4488 mL 0.8976 mL 2.2439 mL
    40 mM 0.0673 mL 0.3366 mL 0.6732 mL 1.6829 mL
    50 mM 0.0539 mL 0.2693 mL 0.5385 mL 1.3463 mL
    60 mM 0.0449 mL 0.2244 mL 0.4488 mL 1.1219 mL
    80 mM 0.0337 mL 0.1683 mL 0.3366 mL 0.8415 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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    产品名称:
    SEA0400
    目录号:
    HY-15515
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