2. Metabolic Enzyme/Protease
  3. Cytochrome P450
  4. Bergamottin

Bergamottin  (Synonyms: 5-Geranoxypsoralen; Bergamotine; Bergaptin)

目录号: HY-N2194 纯度: 99.97%
COA 产品使用指南

摩尔计算器

Bergamottin 是一种有效的竞争性 CYP1A1 抑制剂，Ki 为 10.703 nM。

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Bergamottin Chemical Structure

Bergamottin Chemical Structure

CAS No. : 7380-40-7

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规格 价格 是否有货 数量
1 mg ￥419
In-stock
5 mg ￥1300
In-stock
10 mg ￥2300
In-stock
25 mg ￥4900
In-stock
50 mg   询价  
100 mg   询价  

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Customer Review

Bergamottin 相关抗体

Top Publications Citing Use of Products

查看 Cytochrome P450 亚型特异性产品:

查看所有亚型
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Bergamottin is a potent and competitive CYP1A1 inhibitor with a Ki of 10.703 nM.

IC50 & Target[1]

CYP1A1

10.703 nM (Ki)

CYP1A1

0.192 μM (IC50)

CYP1A2

5.077 μM (IC50)

CYP2B2

4.535 μM (IC50)

CYP2B1

9.495 μM (IC50)

体外研究
(In Vitro)

Bergamottin is a competitive inhibitor of CYP1A1. Bergamottin inhibits CYP1A1, CYP1A2, CYP2B1, and CYP2B2 with IC50s of 0.192±0.029 μM, 5.077±0.31 μM, 9.495±0.979 μM, 4.535±0.092 μM, respectively[1]. Bergamottin has potent antiproliferative effects on the A549 cells. Bergamottin shows both concentration-dependent as well as time‑dependent growth inhibitory effects against these cells. Bergamottin also inhibits the clonogenic activity of the A549 cancer cells by reducing the number of cancer colony forming cells. A reduction in clonogenicity also follows the concentration dependence on Bergamottin[2].

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

Bergamottin 相关抗体:
体内研究
(In Vivo)

The anticancer efficacy of Bergamottin under in vivo conditions using female BALB/c nude mice (a total of 20 mice are used) is determined. Tumors are induced in the mice by injecting non-small cell lung cancer A549 cells (1×106 cells/mouse). After tumor formation, the mice are sacrificed and tumors are removed and their weights and volumes are calculated. The results show that 25, 50 and 100 mg/kg Bergamottin injection reduce the tumor weight from 1.61 g in the PBS-treated group (control) to 1.21, 0.42 and 0.15 g, respectively. Tumor weight in the nude mice is reduced much more significantly in the highest-concentration Bergamottin group (100 mg/kg body weight) compared with the vehicle group (P<0.05). Likewise, 25, 50 and 100 mg/kg Bergamottin injection reduces the tumor volume from 2.2 cm3 in the PBS-treated group (control) to 1.71, 1.1 and 0.51 cm3, respectively. The periodic measurement of the tumor xenograft volume indicates that the tumor volume in the nude mice is reduced considerably in the highest-concentration Bergamottin group (100 mg/kg body weight) compared with the vehicle group (P<0.05)[2].

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

338.40

Formula

C21H22O4
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
In Vitro: 

DMSO 中的溶解度 : 50 mg/mL (147.75 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 2.9551 mL 14.7754 mL 29.5508 mL
5 mM 0.5910 mL 2.9551 mL 5.9102 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

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 (7.39 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。

    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。

    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 (7.39 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。

    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

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: 99.97%

COA (265 KB) HNMR (261 KB) LCMS (99 KB)

产品使用指南 (1538 KB)
参考文献
Kinase Assay
[1]

CYP1A1 Supersomes and different concentrations of 7-ethoxyresorufin (ER) are used to determine CYP1A1 enzymatic kinetics. A typical Michaelis-Menten curve is found. The final reaction mixture contains: 1 pmol CYP1A1, 0.5 mM NADPH, different ER concentrations and 0, 4, 8 and 16 nM of Bergamottin (BG). The reaction is started with the addition of NADPH. Kinetic constants are obtained by a nonlinear regression analysis of experimental data fitted to Michaelis-Menten equation with competitive-type inhibition. Kinetic analysis is also shown by using the Lineweaver-Burk, Dixon and replot of the slopes of the Dixon plot[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[2]

Inhibition of cell proliferation by Bergamottin is measured by the MTT assay. Briefly, the human lung adenocarcinoma cancer A549 cells are plated in 96-well culture plates (1×105 cells/well). After 24 h of incubation, the cells are treated with Bergamottin (0, 5, 10, 25, 50, 75 and 100 μM) for 24 and 48 h, MTT solution (10 mg/mL) is then added to each well. After a 4-h incubation, the formazan precipitate is dissolved in 100 μL DMSO, and then the absorbance is measured in an automated microplated reader at 570 nm. The cell viability ratio is calculated. Cytotoxicity is expressed as the concentration of Bergamottin needed to inhibit cell growth by 50% (IC50 value)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[2]

Mice[2]
Female BALB/c nude mice (six weeks old) (a total of 20 are obtained) are maintained with water and food ad libitum in a pathogen-free environment with a 12 h light and 12 h dark cycle in an animal care facility. Human non‑small cell lung carcinoma A549 cells (2×106 cells/mouse) are injected into the right axilla of the nude mice (5 mice/group) to create tumors in the mice. Subsequent to tumor development, the mice are divided into 4 groups and treated with Bergamottin injected intraperitoneally. The control group in the study is treated with an equal amount of PBS while the other three groups are treated with 25, 50 and 100 mg/kg of Bergamottin. Afterwards, the mice are sacrificed after 18 days, and the tumor weight and volume of each mouse are evaluated. Tumor length and width are measured using a Vernier caliper and the tumor volume (TV) is calculated[2].

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

Bergamottin 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 2.9551 mL 14.7754 mL 29.5508 mL 73.8771 mL
5 mM 0.5910 mL 2.9551 mL 5.9102 mL 14.7754 mL
10 mM 0.2955 mL 1.4775 mL 2.9551 mL 7.3877 mL
15 mM 0.1970 mL 0.9850 mL 1.9701 mL 4.9251 mL
20 mM 0.1478 mL 0.7388 mL 1.4775 mL 3.6939 mL
25 mM 0.1182 mL 0.5910 mL 1.1820 mL 2.9551 mL
30 mM 0.0985 mL 0.4925 mL 0.9850 mL 2.4626 mL
40 mM 0.0739 mL 0.3694 mL 0.7388 mL 1.8469 mL
50 mM 0.0591 mL 0.2955 mL 0.5910 mL 1.4775 mL
60 mM 0.0493 mL 0.2463 mL 0.4925 mL 1.2313 mL
80 mM 0.0369 mL 0.1847 mL 0.3694 mL 0.9235 mL
100 mM 0.0296 mL 0.1478 mL 0.2955 mL 0.7388 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:

Bergamottin7380-40-75-Geranoxypsoralen Bergamotine BergaptinCytochrome P450CYPsInhibitorinhibitorinhibit

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