1. Vitamin D Related/Nuclear Receptor
  2. Estrogen Receptor/ERR
  3. Liquiritigenin

Liquiritigenin  (Synonyms: 甘草素; 4',7-Dihydroxyflavanone)

目录号: HY-N0377 纯度: 99.45%
COA 产品使用指南

Liquiritigenin是从甘草中分离出的黄烷酮,它是一种高度选择性的雌激素受体β (ERβ) 激动剂,用于活化ERE tk-Luc的 EC50 值为36.5 nM。

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Liquiritigenin Chemical Structure

Liquiritigenin Chemical Structure

CAS No. : 578-86-9

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥550
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5 mg ¥500
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10 mg ¥700
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25 mg ¥1320
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50 mg ¥2113
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100 mg ¥2958
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500 mg   询价  

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Customer Review

Other Forms of Liquiritigenin:

查看 Estrogen Receptor/ERR 亚型特异性产品:

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

Liquiritigenin, a flavanone isolated from Glycyrrhiza uralensis, is a highly selective estrogen receptor β (ERβ) agonist with an EC50 of 36.5 nM for activation of the ERE tk-Luc.

IC50 & Target

EC50: 36.5 nM (activation of the ERE tk-Luc)[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 100 μM
Compound: 2
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
Cytotoxicity against human A549 cells after 72 hrs by MTT assay
[PMID: 18440233]
B16 IC50
5 μg/mL
Compound: 6, liquiritigenin
Cytotoxicity against mouse B16 cells after 72 hrs by MTT assay
Cytotoxicity against mouse B16 cells after 72 hrs by MTT assay
[PMID: 15787450]
B16-BL6 IC50
97.7 μM
Compound: 2
Cytotoxicity against mouse B16-BL6 cells after 72 hrs by MTT assay
Cytotoxicity against mouse B16-BL6 cells after 72 hrs by MTT assay
[PMID: 18440233]
CCRF-CEM IC50
> 25 μg/mL
Compound: 6, liquiritigenin
Cytotoxicity against human CEM cells after 72 hrs by MTT assay
Cytotoxicity against human CEM cells after 72 hrs by MTT assay
[PMID: 15787450]
DU-145 IC50
> 100 μM
Compound: 7
Cytotoxicity against human DU145 cells after 72 hrs by MTT assay
Cytotoxicity against human DU145 cells after 72 hrs by MTT assay
[PMID: 20494492]
HCT-116 IC50
37.2 μM
Compound: 7
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay
[PMID: 20494492]
HCT-8 IC50
19.5 μg/mL
Compound: 6, liquiritigenin
Cytotoxicity against human HCT8 cells after 72 hrs by MTT assay
Cytotoxicity against human HCT8 cells after 72 hrs by MTT assay
[PMID: 15787450]
HeLa IC50
> 100 μM
Compound: 2
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
[PMID: 18440233]
HeLa IC50
> 100 μM
Compound: 7
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
Cytotoxicity against human HeLa cells after 72 hrs by MTT assay
[PMID: 20494492]
HL-60 IC50
22.5 μg/mL
Compound: 6, liquiritigenin
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
[PMID: 15787450]
HT-1080 IC50
> 100 μM
Compound: 2
Cytotoxicity against human HT1080 cells after 72 hrs by MTT assay
Cytotoxicity against human HT1080 cells after 72 hrs by MTT assay
[PMID: 18440233]
K562 IC50
> 100 μM
Compound: 7
Cytotoxicity against human K562 cells after 72 hrs by MTT assay
Cytotoxicity against human K562 cells after 72 hrs by MTT assay
[PMID: 20494492]
Lewis lung carcinoma cell line IC50
> 100 μM
Compound: 2
Cytotoxicity against mouse LLC cells after 72 hrs by MTT assay
Cytotoxicity against mouse LLC cells after 72 hrs by MTT assay
[PMID: 18440233]
MCF7 IC50
> 25 μg/mL
Compound: 6, liquiritigenin
Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
[PMID: 15787450]
MDCK CC50
301 μM
Compound: 10
Cytotoxicity against MDCK cells after 72 hrs
Cytotoxicity against MDCK cells after 72 hrs
[PMID: 24313801]
Peritoneal macrophage IC50
85 μM
Compound: kp24
Inhibition of LPS-stimulated nitric oxide production in ddy mouse peritoneal macrophages measured after 20 hrs by Greiss method
Inhibition of LPS-stimulated nitric oxide production in ddy mouse peritoneal macrophages measured after 20 hrs by Greiss method
[PMID: 27955927]
SGC-7901 IC50
92.4 μM
Compound: 7
Cytotoxicity against human SGC7901 cells after 72 hrs by MTT assay
Cytotoxicity against human SGC7901 cells after 72 hrs by MTT assay
[PMID: 20494492]
体外研究
(In Vitro)

Liquiritigenin 在转染有 ERβ 而不是 ERα 的 U2OS 细胞中产生 ERE tk-Luc 的剂量反应激活。Liquiritigenin 对 ERβ 而非 ERα 产生剂量依赖性激活和 CECR6、NKG2E 和 NKD 的时间依赖性增加。Liquiritigenin 的 ERβ 选择性是由于将共激活剂类固醇受体共激活剂 2 选择性募集到靶基因。Liquiritigenin 对 ERαERβ 表现出相似的结合亲和力,并导致 SRC-2 选择性地募集到 ERβ 细胞中的靶基因[1]。Liquiritigenin 预处理MC3T3-E1细胞可防止MG诱导的成骨细胞 MC3T3-E1 细胞死亡和蛋白加合物、细胞内活性氧、线粒体超氧化物、心磷脂过氧化和 TNF-α 的产生[2]

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

体内研究
(In Vivo)

在小鼠异种移植模型中,Liquiritigenin 不会刺激 MCF-7 乳腺癌细胞的子宫大小或肿瘤发生[1]。Liquiritigenin 处理可显著降低血清和海马中促炎细胞因子的浓度,包括白细胞介素 (IL)-6、IL-1β 和肿瘤坏死因子 (TNF)-α[3]

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

分子量

256.25

Formula

C15H12O4

CAS 号
性状

固体

颜色

White to light yellow

中文名称

甘草素

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
细胞实验: 

DMSO 中的溶解度 : 125 mg/mL (487.80 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 3.9024 mL 19.5122 mL 39.0244 mL
5 mM 0.7805 mL 3.9024 mL 7.8049 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

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: ≥ 2.42 mg/mL (9.44 mM); 澄清溶液

    此方案可获得 ≥ 2.42 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 24.2 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: ≥ 2.42 mg/mL (9.44 mM); 澄清溶液

    此方案可获得 ≥ 2.42 mg/mL(饱和度未知)的澄清溶液。

    1 mL 工作液为例,取 100 μL 24.2 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

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: 99.49%

参考文献
Kinase Assay
[1]

The relative binding affinity of liquiritigenin to pure full-length ERα and ERβ is determined using ERα and ERβ competitor assay kits. Fluorescence polarization of the fluorophore-tagged estrogen bound to ERα and ERβ in the presence of increasing amounts of competitor ligand or extract is determined using the GENios Pro microplate reader with fluorescein excitation (485 nM) and emission (530 nM) filters[1].

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

Animal Administration
[1]

Mice: MCF-7 (250,000) cells are grafted under the kidney capsule of nude mice. Five mice per group are treated with a continuous infusion using osmotic pumps containing vehicle, E2 (0.4 mg) or liquiritigenin (2 mg) that infused 2.5 μL/h for 1 month. After one month of treatment, the tumors and uteri are removed and analyzed[1].

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 3.9024 mL 19.5122 mL 39.0244 mL 97.5610 mL
5 mM 0.7805 mL 3.9024 mL 7.8049 mL 19.5122 mL
10 mM 0.3902 mL 1.9512 mL 3.9024 mL 9.7561 mL
15 mM 0.2602 mL 1.3008 mL 2.6016 mL 6.5041 mL
20 mM 0.1951 mL 0.9756 mL 1.9512 mL 4.8780 mL
25 mM 0.1561 mL 0.7805 mL 1.5610 mL 3.9024 mL
30 mM 0.1301 mL 0.6504 mL 1.3008 mL 3.2520 mL
40 mM 0.0976 mL 0.4878 mL 0.9756 mL 2.4390 mL
50 mM 0.0780 mL 0.3902 mL 0.7805 mL 1.9512 mL
60 mM 0.0650 mL 0.3252 mL 0.6504 mL 1.6260 mL
80 mM 0.0488 mL 0.2439 mL 0.4878 mL 1.2195 mL
100 mM 0.0390 mL 0.1951 mL 0.3902 mL 0.9756 mL
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  • 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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产品名称:
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目录号:
HY-N0377
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