2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor NF-κB Immunology/Inflammation Apoptosis Autophagy
  3. RAR/RXR Reactive Oxygen Species Apoptosis Autophagy
  4. Bigelovin

Bigelovin 是可从朝阳花中分离得到的一种倍半萜内酯，是选择性的视黄素 X 受体 α (retinoid X receptor α) 的激动剂。Bigelovin 可通过诱导凋亡和自噬来发挥抗肿瘤活性。Bigelovin 通过抑制 ROS 的生成来调节 mTOR 信号通路。

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Bigelovin Chemical Structure

Bigelovin Chemical Structure

CAS No. : 3668-14-2

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规格 价格 是否有货 数量
1 mg ￥965
In-stock
5 mg ￥2375
In-stock
10 mg ￥3525
In-stock
50 mg   询价  
100 mg   询价  

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Bigelovin 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Bigelovin, a sesquiterpene lactone isolated from Inula hupehensis, is a selective retinoid X receptor α agonist. Bigelovin suppresses tumor growth through inducing apoptosis and autophagy via the inhibition of mTOR pathway regulated by ROS generation[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 ED50
4.9 μM
Compound: Bigelovin
Agonist activity at human RXR-alpha expressed in HEK293 cells coexpressing with pCMX-beta-gal after 24 to 48 hrs by luciferase reporter gene assay
Agonist activity at human RXR-alpha expressed in HEK293 cells coexpressing with pCMX-beta-gal after 24 to 48 hrs by luciferase reporter gene assay
[PMID: 24959987]
HMEC-1 IC50
2679.2 nM
Compound: Bigelovin
Inhibition of HMEC1 cells growth measured after 48 hrs by MTT assay
Inhibition of HMEC1 cells growth measured after 48 hrs by MTT assay
[PMID: 23231968]
HMEC-1 IC50
946.2 nM
Compound: Bigelovin
Inhibition of HMEC1 cells growth measured after 48 hrs
Inhibition of HMEC1 cells growth measured after 48 hrs
[PMID: 23231968]
MCF-10A IC50
26 μM
Compound: 14
Cytotoxicity against human MCF10A cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human MCF10A cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 24044895]
MCF7 IC50
2.1 μM
Compound: 14
Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 24044895]
MDA-MB-231 IC50
2.3 μM
Compound: 14
Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as growth inhibition after 72 hrs by MTT assay
[PMID: 24044895]
RAW264.7 IC50
0.9 μM
Compound: 13
Antiinflammatory action in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production treated 30 mins before LPS challenge measured after 24 hrs by griess reaction
Antiinflammatory action in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production treated 30 mins before LPS challenge measured after 24 hrs by griess reaction
[PMID: 21894898]
体外研究
(In Vitro)

Bigelovin (0 -20 μM，24-72 h) 显著抑制肝癌细胞的细胞活力并诱导细胞凋亡和自噬[1]。
Bigelovin 显著增加p62、LC3B-II，Beclin-1 和 p62 水平的相应降低呈时间依赖性[1]。
Bigelovin 诱导细胞死亡涉及抑制由 ROS 产生调节的 mTOR 通路[1]。

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

Bigelovin 相关抗体:

Cell Viability Assay[1]

Cell Line: HepG2 and SMMC-7721 cells.
Concentration: 0-20 μM.
Incubation Time: 24, 48, 72 h.
Result: Significantly reduced the cell viability of HepG2 and SMMC-7721 cells in a dose- and time dependent manner.
No significant difference observed in cell viability of normal liver cell lines, LO2 and LX2, after BigV treatment for 24, 48 or 72 h.

Western Blot Analysis[1]

Cell Line: HepG2 and SMMC-7721 cells.
Concentration: 0-10 μM.
Incubation Time: 24 h.
Result: The expression of Bcl-2 was decreased, whereas Bax was increased after treatment with BigV. Moreover, Caspase-9, -3 and PARP cleavage were activated significantly after BigV treatment.
体内研究
(In Vivo)

Bigelovin (BigV，5，10，20 mg/kg) 在 HepG2 异种移植肿瘤模型中发挥抗肿瘤活性[1]。

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

Animal Model: HepG2 xenograft model based on the male athymic BALB/c nude mice (5-6 weeks old, 18-22 g)[1].
Dosage: 5, 10, 20 mg/kg.
Administration: Intravenous injection every 2 days.
Result: The tumor growth rate was significantly slower in BigV treated groups in a dose-dependent manner, along with the reduced tumor weight.
No significant alteration of body weight and hepatic enzyme levels (AST, ALT and LDH) in serum was observed after BigV administration.
Western blot findings of tumor tissues indicated the activation of apoptosis and autophagy characterized by the increase of cleaved Caspase-3 and PARP, as well as LC3BII levels.
The inactivation of mTOR was also observed in tumor tissues isolated from BigV-treated mice.
分子量

304.34

Formula

C17H20O5
CAS 号
性状

固体

颜色

White to off-white

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 100 mg/mL (328.58 mM; 超声助溶 (<60°C); 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 3.2858 mL 16.4290 mL 32.8580 mL
5 mM 0.6572 mL 3.2858 mL 6.5716 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 (protect from light)。-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

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 (8.21 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。

    以 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (8.21 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。

    以 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。

    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

只
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）。

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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: 99.92%

COA (287 KB) HNMR (270 KB) LCMS (87 KB)

产品使用指南 (1538 KB)
参考文献

Bigelovin 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 (protect from light)。-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 3.2858 mL 16.4290 mL 32.8580 mL 82.1450 mL
5 mM 0.6572 mL 3.2858 mL 6.5716 mL 16.4290 mL
10 mM 0.3286 mL 1.6429 mL 3.2858 mL 8.2145 mL
15 mM 0.2191 mL 1.0953 mL 2.1905 mL 5.4763 mL
20 mM 0.1643 mL 0.8214 mL 1.6429 mL 4.1072 mL
25 mM 0.1314 mL 0.6572 mL 1.3143 mL 3.2858 mL
30 mM 0.1095 mL 0.5476 mL 1.0953 mL 2.7382 mL
40 mM 0.0821 mL 0.4107 mL 0.8214 mL 2.0536 mL
50 mM 0.0657 mL 0.3286 mL 0.6572 mL 1.6429 mL
60 mM 0.0548 mL 0.2738 mL 0.5476 mL 1.3691 mL
80 mM 0.0411 mL 0.2054 mL 0.4107 mL 1.0268 mL
100 mM 0.0329 mL 0.1643 mL 0.3286 mL 0.8214 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.

Keywords:

Bigelovin3668-14-2RAR/RXRReactive Oxygen SpeciesApoptosisAutophagyRetinoic acid receptorsRetinoid X receptorsInhibitorinhibitorinhibit

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