1. MAPK/ERK Pathway Autophagy Metabolic Enzyme/Protease
  2. Carboxylesterase p38 MAPK Autophagy UGT
  3. Bakuchiol

Bakuchiol  (Synonyms: 补骨脂酚; (S)-(+)-Bakuchiol)

目录号: HY-N0235 纯度: 98.53%
COA 产品使用指南

Bakuchiol 是一种可以从补骨脂种子中得到的植物雌激素。Bakuchiol 被证实为多种酶的非竞争性抑制剂,包括 UDP-葡萄糖醛酸基转移酶 2B7 (UGT2B7) 和人羧酸酯酶 2 (hCE2),IC50s 值分别为 40.9 μM 和 7.28 μM。Bakuchiol 在抗炎、抗菌、抗肿瘤以及药物代谢调控等方面具有极大的研究和应用潜力。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Bakuchiol Chemical Structure

Bakuchiol Chemical Structure

CAS No. : 10309-37-2

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥242
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5 mg ¥220
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10 mg ¥350
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25 mg ¥600
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50 mg ¥950
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100 mg ¥1400
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500 mg ¥3588
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Other Forms of Bakuchiol:

查看 p38 MAPK 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Bakuchiol is a phytoestrogen that can be obtained from psoralen seeds. Bakuchiol has been proven to be a non-competitive inhibitor of multiple enzymes, including UDP-glucuronosyltransferase 2B7 (UGT2B7) [2] and human carboxylesterase 2 (hCE2) [3], with IC50s values of 40.9 μM and 7.28 μM, respectively. Bakuchiol exhibits significant research and application potential in areas such as anti-inflammatory[5], antibacterial[4], antitumor[1] therapies, as well as drug metabolism regulation.

IC50 & Target

IC50:40.9 nM (UGT2B7) ; IC50:7.28 nM (hCE2)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
AGS IC50
15.3 μM
Compound: 1
Cytotoxicity against human AGS cells by MTT assay
Cytotoxicity against human AGS cells by MTT assay
[PMID: 18359631]
AGS IC50
6.1 μM
Compound: 1
Inhibition of hypoxia-induced HIF1 activation in human AGS cells by reporter gene assay
Inhibition of hypoxia-induced HIF1 activation in human AGS cells by reporter gene assay
[PMID: 18359631]
BJ EC50
> 36.63 μM
Compound: 1
Cytotoxicity against human BJ cells after 72 hrs by Cell-Titer Glo assay
Cytotoxicity against human BJ cells after 72 hrs by Cell-Titer Glo assay
[PMID: 26922230]
HEK293 EC50
> 36.63 μM
Compound: 1
Cytotoxicity against HEK293 cells after 72 hrs by Cell-Titer Glo assay
Cytotoxicity against HEK293 cells after 72 hrs by Cell-Titer Glo assay
[PMID: 26922230]
HeLa IC50
11 μM
Compound: 1
Cytotoxicity against human HeLa cells by MTT assay
Cytotoxicity against human HeLa cells by MTT assay
[PMID: 18359631]
HepG2 EC50
> 52.0833 μM
Compound: 1
Cytotoxicity against human HepG2 cells after 72 hrs by Cell-Titer Glo assay
Cytotoxicity against human HepG2 cells after 72 hrs by Cell-Titer Glo assay
[PMID: 26922230]
Jurkat EC50
> 49.0196 μM
Compound: 1
Cytotoxicity against human Jurkat cells after 72 hrs by Cell-Titer Glo assay
Cytotoxicity against human Jurkat cells after 72 hrs by Cell-Titer Glo assay
[PMID: 26922230]
NALM-6 EC50
38 μM
Compound: 1
Cytotoxicity against human NALM6 cells after 72 hrs by Cell-Titer Glo assay
Cytotoxicity against human NALM6 cells after 72 hrs by Cell-Titer Glo assay
[PMID: 26922230]
Raji EC50
> 26.0417 μM
Compound: 1
Cytotoxicity against human Raji cells after 72 hrs by Cell-Titer Glo assay
Cytotoxicity against human Raji cells after 72 hrs by Cell-Titer Glo assay
[PMID: 26922230]
RAW264.7 IC50
97.23 μM
Compound: BAK
Cytotoxicity against mouse RAW 264.7 cells assessed as decreased cell viability measured after 24 hrs by MTT assay
Cytotoxicity against mouse RAW 264.7 cells assessed as decreased cell viability measured after 24 hrs by MTT assay
[PMID: 35000392]
SEM EC50
15.2866 μM
Compound: 1
Cytotoxicity against human SEM cells after 72 hrs by Cell-Titer Glo assay
Cytotoxicity against human SEM cells after 72 hrs by Cell-Titer Glo assay
[PMID: 26922230]
体外研究
(In Vitro)

Bakuchiol (5-20 μM, 72 h) 通过 MTT 实验发现对 A549 细胞具有选择性的细胞毒性。Bakuchiolb在降低 A549 细胞活力方面比它的同类物质 Resveratrol (HY-16561) 更为有效,它们的 IC50s 值分别为 9.58 μM 和 33.02 μM[1]
Bakuchiol (5-20 μM, 24 h or 36h) 能呈浓度依赖性地将 A549 细胞的细胞周期进程阻滞至 S 期,并诱导活性氧 (ROS) 相关的细胞凋亡[1]
Bakuchiol (0-80 μM, 120 min) 是一种针对 UDP-葡萄糖醛酸基转移酶 2B7 (UGT2B7) 的非竞争性抑制剂,其 Ki 值为 10.7 μM,IC50 值为 40.9 μM[2]
Bakuchiol (30 min) 是一种针对人羧酸酯酶 2 (hCE2) 的强效的非竞争性抑制剂,其 Ki 值为 2.12 μM,IC50 值为 7.28 μM[3]
Bakuchiol (0.9775-3.91 μg/mL, 24 h) 能呈浓度依赖性地增加 T. mentagrophytes 真菌分生孢子的膜通透性[4]
Bakuchiol (3.91 μg/mL, 3 h) 能够引发真菌细胞中 187 % 的活性氧 (ROS) 水平升高[4]

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

Western Blot Analysis[1]

Cell Line: A549 cells, EA.hy926 cells, HUVEC cells and MEF
Concentration: 5, 10, and 20 μM
Incubation Time: 24 hours
Result: Induced caspase 9/3 activaton, p53 and Bax up-regulation, as well as Bcl-2 down-regulation.

Apoptosis Analysis[1]

Cell Line: A549 cells, EA.hy926 cells, HUVEC cells and MEF
Concentration: 5, 10, and 20 μM
Incubation Time: 36 hours
Result: Resulted in typical apoptotic cells (p < 0.05), as determined by Annexin V/propidium iodide staining and flow cytometry.

Cell Cycle Analysis[1]

Cell Line: A549 cells
Concentration: 5, 10, and 20 μM
Incubation Time: 24 hours
Result: Increased S phase cell population accompanied with a concomitant reduction of cells in the G1 phase. Resulted in a less potent effect in S phase arrest than bakuchiol.

Cell Cytotoxicity Assay[1]

Cell Line: A549 cells, EA.hy926 cells, HUVEC cells and MEF
Concentration: 5, 10, and 20 μM
Incubation Time: 72 hours
Result: Inhibited the growth of A549 cells, while the growth rate of other cells were not changed. Exhibited concentration-dependent cytotoxicity in A549 cells, while bakuchiol showed a more potent effect than that of resveratrol with IC50s vales of 9.58 μmol/L and 33.02 μmol/ L, respectively.
体内研究
(In Vivo)

Bakuchiol (10 and 20 mg/kg, p.o.) 可以减轻卵清蛋白(OVA)诱导的过敏性鼻炎 (AR)小鼠的过敏症状,减少炎症反应,改善 T 细胞平衡,减少氧化应激并调节 Igs 水平[5]。

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

Animal Model: OVA -induced AR model (BALB/c mice, 6-week-old) [5]
Dosage: 10 and 20 mg/kg
Administration: Oral route (p.o.)
Result: Reduced the nasal symptoms and decreased the levels of IL-4, IL-5, IL-13, Igs (IgE and IgG1), histamine, IL-10, IL-33, and TNF-α. Reduced PGDA and LTC-4 levels in the nasal lavage fluid (NLF). Decreased the ROS and MDA levels, whereas boosting SOD activity. Decreased the eosinophil count in the nasal tissues and influenced the Th1 and Th2 cell proportions.
Clinical Trial
分子量

256.38

Formula

C18H24O

CAS 号
性状

液体(密度:0.963 g/cm3

颜色

Colorless to yellow

中文名称

补骨脂酚

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°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 : 62.5 mg/mL (243.78 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 3.9005 mL 19.5023 mL 39.0046 mL
5 mM 0.7801 mL 3.9005 mL 7.8009 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    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.17 mg/mL (8.46 mM); 澄清溶液

    此方案可获得 ≥ 2.17 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 21.7 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。
  • 方案 二

    请依序添加每种溶剂: 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.17 mg/mL (8.46 mM); 澄清溶液

    此方案可获得 ≥ 2.17 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 21.7 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)。

*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: 99.25%

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, 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 3.9005 mL 19.5023 mL 39.0046 mL 97.5115 mL
5 mM 0.7801 mL 3.9005 mL 7.8009 mL 19.5023 mL
10 mM 0.3900 mL 1.9502 mL 3.9005 mL 9.7512 mL
15 mM 0.2600 mL 1.3002 mL 2.6003 mL 6.5008 mL
20 mM 0.1950 mL 0.9751 mL 1.9502 mL 4.8756 mL
25 mM 0.1560 mL 0.7801 mL 1.5602 mL 3.9005 mL
30 mM 0.1300 mL 0.6501 mL 1.3002 mL 3.2504 mL
40 mM 0.0975 mL 0.4876 mL 0.9751 mL 2.4378 mL
50 mM 0.0780 mL 0.3900 mL 0.7801 mL 1.9502 mL
60 mM 0.0650 mL 0.3250 mL 0.6501 mL 1.6252 mL
80 mM 0.0488 mL 0.2438 mL 0.4876 mL 1.2189 mL
100 mM 0.0390 mL 0.1950 mL 0.3900 mL 0.9751 mL
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    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:
HY-N0235
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