1. NF-κB
  2. NF-κB
  3. Schisantherin A

Schisantherin A  (Synonyms: 五味子酯甲; Gomisin-C; Schizantherin-A; Wuweizi ester-A)

目录号: HY-N0694 纯度: 99.87%
COA 产品使用指南

Schisantherin A 是一种木脂素。Schisantherin A 通过 IκBα 降解来抑制 p65-NF-κB 易位进入细胞核。

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Schisantherin A Chemical Structure

Schisantherin A Chemical Structure

CAS No. : 58546-56-8

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥284
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5 mg ¥173
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10 mg ¥259
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25 mg ¥467
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50 mg ¥700
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100 mg ¥1050
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Other Forms of Schisantherin A:

MCE 顾客使用本产品发表的 1 篇科研文献

WB

    Schisantherin A purchased from MCE. Usage Cited in: Life Sci. 2020 Oct 1;258:118161.  [Abstract]

    Western blot analysis shows a significant activation of NF-κB signaling, whereas pre-incubation of SchA (50 μM) could diminish LPS-triggered P65NF-κB phosphorylation. The dose-dependent experiment shows SchA at 25 μM or 50 μM could inhibit the activation of P65NF-κB after LPS stimulation for 3 hours.

    查看 NF-κB 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Schisantherin A is a dibenzocyclooctadiene lignan. Schisantherin A inhibits p65-NF-κB translocation into the nucleus by IκBα degradation.

    IC50 & Target[1]

    p65

     

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A549 IC50
    > 100 μM
    Compound: Gomisin C
    Antiproliferative activity against human A549 cells after 72 hrs by SRB assay
    Antiproliferative activity against human A549 cells after 72 hrs by SRB assay
    [PMID: 18063366]
    A549 GI50
    74.9 μM
    Compound: 1
    Growth inhibition of human A549 cells after 48 hrs by SRB assay
    Growth inhibition of human A549 cells after 48 hrs by SRB assay
    10.1039/C6MD00097E
    DU-145 GI50
    13.3 μM
    Compound: 1
    Growth inhibition of human DU145 cells after 48 hrs by SRB assay
    Growth inhibition of human DU145 cells after 48 hrs by SRB assay
    10.1039/C6MD00097E
    HCT-15 IC50
    > 100 μM
    Compound: Gomisin C
    Antiproliferative activity against human HCT15 cells after 72 hrs by SRB assay
    Antiproliferative activity against human HCT15 cells after 72 hrs by SRB assay
    [PMID: 18063366]
    IMR-32 GI50
    3.6 μM
    Compound: 1
    Growth inhibition of human IMR32 cells after 48 hrs by SRB assay
    Growth inhibition of human IMR32 cells after 48 hrs by SRB assay
    10.1039/C6MD00097E
    K562 IC50
    > 100 μM
    Compound: Gomisin C
    Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
    Antiproliferative activity against human K562 cells after 72 hrs by MTT assay
    [PMID: 18063366]
    MDA-MB-231 GI50
    2.8 μM
    Compound: 1
    Growth inhibition of human MDA-MB-231 cells after 48 hrs by SRB assay
    Growth inhibition of human MDA-MB-231 cells after 48 hrs by SRB assay
    10.1039/C6MD00097E
    MDA-MB-231 IC50
    56.4 μM
    Compound: Gomisin C
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by SRB assay
    [PMID: 18063366]
    PANC-1 GI50
    > 100 μM
    Compound: 1
    Growth inhibition of human PANC1 cells after 48 hrs by SRB assay
    Growth inhibition of human PANC1 cells after 48 hrs by SRB assay
    10.1039/C6MD00097E
    SiHa GI50
    14.7 μM
    Compound: 1
    Growth inhibition of human SiHa cells after 48 hrs by SRB assay
    Growth inhibition of human SiHa cells after 48 hrs by SRB assay
    10.1039/C6MD00097E
    SK-HEP1 IC50
    70.4 μM
    Compound: Gomisin C
    Antiproliferative activity against human SK-HEP1 cells after 72 hrs by SRB assay
    Antiproliferative activity against human SK-HEP1 cells after 72 hrs by SRB assay
    [PMID: 18063366]
    SNU-638 IC50
    44.7 μM
    Compound: Gomisin C
    Antiproliferative activity against human SNU638 cells after 72 hrs by SRB assay
    Antiproliferative activity against human SNU638 cells after 72 hrs by SRB assay
    [PMID: 18063366]
    T47D IC50
    51.2 μM
    Compound: Gomisin C
    Antiproliferative activity against human T47D cells after 72 hrs by SRB assay
    Antiproliferative activity against human T47D cells after 72 hrs by SRB assay
    [PMID: 18063366]
    体外研究
    (In Vitro)

    The concentrations of TNF-α and IL-6 in the supernatant of cells pretreated with 2.5 or 25 mg/L of Schisantherin A are significantly decreased compared to the LPS control group (p<0.05, p<0.01). The potential cytotoxicity of Schisantherin A is evaluated by the MTT assay after incubating cells for 24 h in the absence or presence of LPS, result shows cell viabilities are not affected by the cytokines at concentrations used (0.5, 2.5, 25 mg/L). RAW 264.7 murine macrophage cells are pre-incubated with Schisantherin A for 1 h and then stimulated with 1 mg/L LPS for 12 h. Both LPS and samples are untreated in control group. After the cell culture media are collected, nitrite and PGE2 levels are determined, and Schisantherin A is found to reduce NO and PGE2 production in a dose-dependent manner[1].

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

    体内研究
    (In Vivo)

    Schisantherin A, a dibenzocyclooctadiene lignan isolated from the fruit of Schisandra sphenanthera, has been reported to possess varied beneficial pharmacological effects. Schisantherin A protects lipopolysaccharide-induced acute respiratory distress syndrome in mice through inhibiting NF-κB and MAPKs signaling pathways. Pretreatment with Schisantherin A markedly ameliorates LPS-induced histopathologic changes and decreases the levels of TNF-α, IL-6 and IL-1β in the BALF. In addition, the phosphorylation of NF-κB p65, IκB-α, JNK, ERK and p38 induced by LPS are suppressed by Schisantherin A. The lung wet/dry weight ratio is evaluated at 7 h after the intranasal instillation of LPS. The results show that there are no differences between control group and Schisantherin A (40 mg/kg) group (p>0.05). LPS causes a significant increase in lung wet/dry weight ratio (p<0.01) compared with the control group. Schisantherin A dose-dependently decreases the lung wet/dry weight ratio (p<0.05) compared to those in the LPS group[1].

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

    分子量

    536.57

    Formula

    C30H32O9

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    五味子酯甲

    结构分类
    初始来源
    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
    细胞实验: 

    DMSO 中的溶解度 : ≥ 100 mg/mL (186.37 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 1.8637 mL 9.3184 mL 18.6369 mL
    5 mM 0.3727 mL 1.8637 mL 3.7274 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

    动物实验:

    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 (4.66 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。

      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 (4.66 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: 99.87%

    参考文献
    Cell Assay
    [1]

    The MTT assay is performed to measure cell viability. RAW 264.7 cells are mechanically scraped, seeded in 96-well plates at 4×105 cells/mL, and incubated in a 37°C, 5% CO2 incubator overnight. After 24 h, cells, treated with 50 μL of different concentrations of Schisantherin A (0-25 mg/L) for 1 h are then stimulated with 50 μL LPS for 18 h. Subsequently, 20 μL of 5 mg/mL MTT in FBS-free medium is added to each well, and the cells are incubated for 4 h. MTT is removed and resolved with 150 μL/well DMSO. The optical density is measured at 570 nm using a microplate reader. Concentrations are determined for three wells of each sample, and this experiment done in triplicate[1].

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

    Animal Administration
    [1]

    Mice[1]
    Male BALB/c mice, 6-8 weeks old, are used. All mice are randomly divided into six groups: control group, Schisantherin A (40 mg/kg) group, LPS group, Schisantherin A (10, 20 and 40 mg/kg)+LPS group, and Dexamethasone (DEX)+LPS group. DEX+LPS group is used as a positive control. Schisantherin A and DEX (5 mg/kg) are conducted intraperitoneally. Mice of control and LPS groups are given an equal volume of PBS. One hour later, after slightly anesthetized with an inhalation of diethyl ether, mice are instilled intranasally (i.n.) 10 μg LPS in 50 μL PBS to induce lung injury. Control mice are given 50 μL PBS instead of LPS. All mice are alive after 7 h of LPS treatment[1].

    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 1.8637 mL 9.3184 mL 18.6369 mL 46.5922 mL
    5 mM 0.3727 mL 1.8637 mL 3.7274 mL 9.3184 mL
    10 mM 0.1864 mL 0.9318 mL 1.8637 mL 4.6592 mL
    15 mM 0.1242 mL 0.6212 mL 1.2425 mL 3.1061 mL
    20 mM 0.0932 mL 0.4659 mL 0.9318 mL 2.3296 mL
    25 mM 0.0745 mL 0.3727 mL 0.7455 mL 1.8637 mL
    30 mM 0.0621 mL 0.3106 mL 0.6212 mL 1.5531 mL
    40 mM 0.0466 mL 0.2330 mL 0.4659 mL 1.1648 mL
    50 mM 0.0373 mL 0.1864 mL 0.3727 mL 0.9318 mL
    60 mM 0.0311 mL 0.1553 mL 0.3106 mL 0.7765 mL
    80 mM 0.0233 mL 0.1165 mL 0.2330 mL 0.5824 mL
    100 mM 0.0186 mL 0.0932 mL 0.1864 mL 0.4659 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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