1. NF-κB Metabolic Enzyme/Protease Cell Cycle/DNA Damage
  2. NF-κB HSP Eukaryotic Initiation Factor (eIF)
  3. Rocaglamide

Rocaglamide  (Synonyms: 楝酰胺; Roc-A; MG-002)

目录号: HY-19356 纯度: 98.61%
COA 产品使用指南

Rocaglamide (Roc-A) 是从楝科植物中分离出来,可用于咳嗽,受伤,哮喘和炎症性皮肤病。Rocaglamide 是 T 细胞中一种有效的 NF-κB 活化抑制剂。Rocaglamide 是一种有效的选择性热休克因子 1 (HSF1) 活化抑制剂,IC50 约为 50 nM。Rocaglamide 还抑制翻译起始因子 eIF4A 的功能。Rocaglamide 还具有抗癌特性。

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Rocaglamide Chemical Structure

Rocaglamide Chemical Structure

CAS No. : 84573-16-0

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥5672
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500 μg ¥1280
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1 mg ¥2050
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5 mg ¥5100
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10 mg ¥8700
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Customer Review

Other Forms of Rocaglamide:

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Top Publications Citing Use of Products

    Rocaglamide purchased from MCE. Usage Cited in: Nat Commun. 2021 Jun 17;12(1):3720.  [Abstract]

    The expression of PRDX3 and stem cell markers is decreased upon rocaglamide A (RocA) treatment in a time-dependent and dose-dependent manner.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Rocaglamide (Roc-A) is isolated from the genus Aglaia and can be used for coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor of NF-κB activation in T-cells. Rocaglamide is a potent and selective heat shock factor 1 (HSF1) activation inhibitor with an IC50 of ~50 nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia[1][2][3].

    IC50 & Target[1]

    eIF4

     

    HSF1

    50 nM (IC50)

    体外研究
    (In Vitro)

    Rocaglamide 增强 TRAIL 诱导的耐药 HCC 细胞凋亡。Rocaglamide 单独处理导致 9% HepG2 和 11% Huh-7 细胞凋亡,TRAIL 处理诱导 16% HepG2 和 17% Huh-7 细胞凋亡。然而,Rocaglamide 和 TRAIL 的组合在 55% HepG2 和 57% Huh-7 细胞中诱导细胞凋亡,这显然不仅仅是相加效应。通过使用结晶紫染色测量细胞生存力获得了类似的结果。Rocaglamide 有可能使高度化学耐药的 HepG2 和 Huh-7 细胞对基于 TRAIL 的疗法敏感[2]

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

    体内研究
    (In Vivo)

    与对照组相比,Rocaglamide 处理组的肿瘤体积为 45±12%。与对照组相比,Rocaglamide 显著抑制肿瘤生长。Rocaglamide 处理不会导致体重下降,并且在处理期间未在小鼠身上观察到明显的毒性迹象,这表明 Rocaglamide 的总体耐受性良好[2]

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

    分子量

    505.56

    Formula

    C29H31NO7

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    楝酰胺

    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
    In Vitro: 

    DMSO 中的溶解度 : 100 mg/mL (197.80 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 1.9780 mL 9.8900 mL 19.7800 mL
    5 mM 0.3956 mL 1.9780 mL 3.9560 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: ≥ 7.5 mg/mL (14.84 mM); 澄清溶液

      此方案可获得 ≥ 7.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 75.0 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% (20% SBE-β-CD in Saline)

      Solubility: ≥ 7.5 mg/mL (14.84 mM); 澄清溶液

      此方案可获得 ≥ 7.5 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 75.0 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。
    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: 99.34%

    参考文献
    Cell Assay
    [2]

    HepG2 and Huh-7 cells (1×104/well) are seeded in 96-well plates in complete culture medium and incubated for 24 h. The cells are then exposed to 100 nM Rocaglamide and/or 100 ng/mL TRAIL for 24 h. The control cells are treated with DMSO at a concentration equal to that used for the drug-treated cells. The complete culture medium is then removed and MTT (200 μL, 0.5 mg/mL in 10% FBS-containing DMEM) is added to each well and the plate is incubated for 2 h at 37°C in a humidified incubator. The solution is then removed from the wells and 200 μL DMSO is added to each well prior to agitation. The absorbance at 570 nm is read using a microplate reader (Bio-Tek ELx800). The value for the vehicle-treated cells is considered to indicate 100% viability. Furthermore, a crystal violet assay is carried out. Briefly, the cells (1×105/mL) are seeded in a 12 well plate for 12 h, and treated with TRAIL (0-100 ng/mL) and/or RocA(1-100 nM) for 12 h. The treated cells are washed with phosphate-buffered saline (PBS), fixed with 4% paraformaldehyde for 15 min, and stained using crystal violet for a further 30 min[2].

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

    Animal Administration
    [2]

    Mice[2]
    The Huh-7 cells (3×106), suspended in 100 μL mix (equal volumes of DMEM and Matrigel), are implanted subcutaneously into the right flank of 10 female SCID mice (6-week-old) and then randomly divided into two equal groups, one of which received an intraperitoneal injection of Rocaglamide (2.5 mg/kg in 80 μL olive oil; n=5) and the other, used as a vehicle control, received olive oil alone (n=5). These treatments are performed once daily for 32 days and the tumor volumes and body weights of the animals are measured twice a week. The tumor volumes (mm3) are calculated using the following formula: Tumor volume=LS2/2, where L is the longest diameter and S is the shortest. At the end of the experiments, the mice are sacrificed and tumor samples are harvested, fixed in formalin and embedded in paraffin as tissue sections for immunohistochemical analysis.

    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 1.9780 mL 9.8900 mL 19.7800 mL 49.4501 mL
    5 mM 0.3956 mL 1.9780 mL 3.9560 mL 9.8900 mL
    10 mM 0.1978 mL 0.9890 mL 1.9780 mL 4.9450 mL
    15 mM 0.1319 mL 0.6593 mL 1.3187 mL 3.2967 mL
    20 mM 0.0989 mL 0.4945 mL 0.9890 mL 2.4725 mL
    25 mM 0.0791 mL 0.3956 mL 0.7912 mL 1.9780 mL
    30 mM 0.0659 mL 0.3297 mL 0.6593 mL 1.6483 mL
    40 mM 0.0495 mL 0.2473 mL 0.4945 mL 1.2363 mL
    50 mM 0.0396 mL 0.1978 mL 0.3956 mL 0.9890 mL
    60 mM 0.0330 mL 0.1648 mL 0.3297 mL 0.8242 mL
    80 mM 0.0247 mL 0.1236 mL 0.2473 mL 0.6181 mL
    100 mM 0.0198 mL 0.0989 mL 0.1978 mL 0.4945 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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    目录号:
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