Bergaptol(Synonyms: 5-Hydroxypsoralen; 4-Hydroxybergapten)

天然产物 天然产物苯丙素类 Phenylpropanoids

Bergaptol (Synonyms: 5-Hydroxypsoralen; 4-Hydroxybergapten) 纯度: 99.44%

Bergaptol 是CYP3A4酶脱苄基作用的抑制剂,它的IC50是24.92 uM. 最近的研究表明它有抗增殖和抗癌性。

Bergaptol(Synonyms: 5-Hydroxypsoralen;  4-Hydroxybergapten)

Bergaptol Chemical Structure

CAS No. : 486-60-2

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10 mM * 1 mL in DMSO ¥2251 In-stock
500 mg ¥2046 In-stock
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5 g   询价  

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生物活性

Bergaptol is a hydroxylated psoralen that acts as a potent inhibitors of debenzylation activity of CYP3A4 enzyme with an IC50 value of 24.92 uM. Recent studies suggest that it may have antiproliferative and anticancer properties. target: CYP3A4 [1] IC50: 24.92 [1] For in vivo enzyme activity analysis, 100 μM bergaptol was added to the cultures for an additional 24 h at 37°C. After centrifugation, the supernatant was used to measure the bergapten yield by high performance liquid chromatography (HPLC).[2]

分子量

202.16

Formula

C11H6O4

CAS 号

486-60-2

中文名称

香柑醇;佛手酚

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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL (247.33 mM)

H2O : 0.67 mg/mL (3.31 mM; Need ultrasonic)

* “≥” 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 4.9466 mL 24.7329 mL 49.4658 mL
5 mM 0.9893 mL 4.9466 mL 9.8932 mL
10 mM 0.4947 mL 2.4733 mL 4.9466 mL

*

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。-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。

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

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2.5 mg/mL (12.37 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (12.37 mM) 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 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
  • [1]. Basavaraj Girennavar et al. Radical scavenging and cytochrome P450 3A4 inhibitory activity of bergaptol and geranylcoumarin from grapefruit. Bioorganic & Medicinal Chemistry.June 2007, Pages 3684-3691

    [2]. Yucheng Zhao et al. Cloning, Functional Characterization, and Catalytic Mechanism of a Bergaptol O-Methyltransferase from Peucedanum praeruptorum Dunn. Front Plant Sci, 2016, 7: 722.