1. Metabolic Enzyme/Protease Immunology/Inflammation
  2. Phosphodiesterase (PDE) NO Synthase
  3. 3-O-Methylquercetin

3-O-Methylquercetin  (Synonyms: 3-O-甲基槲皮素)

目录号: HY-N1860 纯度: 99.98%
COA 产品使用指南

3-O-Methylquercetin 是 cAMP 和 cGMP-磷酸二酯酶 (PDE) 的抑制剂,IC50 分别为 13.8 μM 和 14.3 μM。3-O-Methylquercetin 是 β-分泌酶的抑制剂,IC50 为 6.5 μM。3-O-Methylquercetin 可以对抗氧化损伤导致的神经元死亡,具有神经保护的作用。3-O-Methylquercetin 对脊髓灰质炎病毒、柯萨奇病毒和人鼻病毒具有较强的抗病毒活性。3-O-Methylquercetin 具有抗炎和松弛气管的作用,可用于炎症疾病和哮喘的研究。

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3-O-Methylquercetin Chemical Structure

3-O-Methylquercetin Chemical Structure

CAS No. : 1486-70-0

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

3-O-Methylquercetin is an inhibitor of cAMP and CGMP-phosphodiesterase (PDE) with IC50 at 13.8 μM and 14.3 μM, respectively. 3-O-Methylquercetin is an inhibitor of β-secretase with an IC50 of 6.5 μM. 3-O-Methylquercetin has a neuroprotective effect against neuronal death caused by oxidative damage. 3-O-Methylquercetin has strong antiviral activity against poliovirus, coxsackie virus and human rhinovirus. 3-O-Methylquercetin has anti-inflammatory and trachea-relaxing effects and can be used in the study of inflammatory diseases and asthma[1][2][3][4][5][6].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
8.14 μM
Compound: 2a
Anticancer activity against human A549 cells by HTS assay
Anticancer activity against human A549 cells by HTS assay
[PMID: 25139569]
Calu-1 IC50
> 50 μM
Compound: 2a
Anticancer activity against human Calu1 cells by HTS assay
Anticancer activity against human Calu1 cells by HTS assay
[PMID: 25139569]
HeLa IC50
6.09 μM
Compound: 2a
Anticancer activity against human HeLa cells by HTS assay
Anticancer activity against human HeLa cells by HTS assay
[PMID: 25139569]
HepG2 2.2.15 CC50
2.1 μM
Compound: Table 3, R9C1
Cytotoxicity against human HepG2(2.2.15) cells after 8 days by MTT assay
Cytotoxicity against human HepG2(2.2.15) cells after 8 days by MTT assay
[PMID: 21401115]
HOP-62 IC50
35.54 μM
Compound: 2a
Anticancer activity against human HOP62 cells by HTS assay
Anticancer activity against human HOP62 cells by HTS assay
[PMID: 25139569]
LOX IMVI IC50
> 50 μM
Compound: 2a
Anticancer activity against human LOXIMVI cells by HTS assay
Anticancer activity against human LOXIMVI cells by HTS assay
[PMID: 25139569]
M14 IC50
> 50 μM
Compound: 2a
Anticancer activity against human M14 cells by HTS assay
Anticancer activity against human M14 cells by HTS assay
[PMID: 25139569]
Monocyte IC50
47 μM
Compound: 3-O-methyl quercetin
Inhibition of TNFalpha expression in LPS-stimulated human monocytes treated 30 mins before LPS challenge measured after 14 hrs by ELISA
Inhibition of TNFalpha expression in LPS-stimulated human monocytes treated 30 mins before LPS challenge measured after 14 hrs by ELISA
[PMID: 10096854]
NCI-H1299 IC50
46.81 μM
Compound: 2a
Anticancer activity against human H1299 cells by HTS assay
Anticancer activity against human H1299 cells by HTS assay
[PMID: 25139569]
NCI-H157 IC50
18.67 μM
Compound: 2a
Anticancer activity against human NCI-H157 cells by HTS assay
Anticancer activity against human NCI-H157 cells by HTS assay
[PMID: 25139569]
NCI-H1792 IC50
24.09 μM
Compound: 2a
Anticancer activity against human NCI-H1792 cells by HTS assay
Anticancer activity against human NCI-H1792 cells by HTS assay
[PMID: 25139569]
NCI-H1944 IC50
23.64 μM
Compound: 2a
Anticancer activity against human NCI-H1944 cells by HTS assay
Anticancer activity against human NCI-H1944 cells by HTS assay
[PMID: 25139569]
NCI-H460 IC50
9.91 μM
Compound: 2a
Anticancer activity against human H460 cells by HTS assay
Anticancer activity against human H460 cells by HTS assay
[PMID: 25139569]
NCI-H522 IC50
> 50 μM
Compound: 2a
Anticancer activity against human NCI-H522 cells by HTS assay
Anticancer activity against human NCI-H522 cells by HTS assay
[PMID: 25139569]
RAW264.7 IC50
3.5 μg/mL
Compound: 204
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess reagent based assay
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 24 hrs by Griess reagent based assay
[PMID: 31255927]
体外研究
(In Vitro)

3-O-Methylquercetin (1-10 μM;24 小时) 在 LPS (HY-D1056) 处理的 RAW 264.7 细胞中以浓度依赖性的方式抑制 NO 的生成 (IC50: 4.23 μM) 以及 iNOS 蛋白和 mRNA 的表达[1]
3-O-Methylquercetin (1-30 μM;15 分钟) 对豚鼠气管具有松弛作用[2]
3-O-Methylquercetin (1-100 μM;20-24 小时) 在 H2O2 处理的大鼠皮质细胞中,可提高细胞的存活率[3]

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

Western Blot Analysis[1]

Cell Line: LPS (HY-D1056) treated RAW 264.7
Concentration: 1, 3 and 10 μM
Incubation Time: 24 h
Result: Reduced the level of iNOS in a dose-dependent manner.
体内研究
(In Vivo)

3-O-Methylquercetin (3-30 μmol/kg ≈ 0.95-9.5 mg/kg;腹腔注射;3 次) 在卵清蛋白 (HY-W250978) 诱导的气道高反应性小鼠模型中具有改善作用[4]

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

Animal Model: Ovalbumin (HY-W250978) treated female BALB/c mice aged 8-12 weeks old[4]
Dosage: 3 and 30 μmol/kg ≈ 0.95 and 9.5 mg/kg
Administration: Intraperitoneal injection (i.p.); 3 times
Result: Significantly suppressed the enhanced pause value induced by aerosolized methacholine in sensitized mice after secondary allergen challenge.
Significantly suppressed total inflammatory cells, macrophages, neutrophils, and eosinophils, but not lymphocytes.
Significantly decreased the secretion of TNF-α, and at the highest dose even decreased the secretions of IL-4, IL-5, and TNF-α.
分子量

316.26

Formula

C16H12O7

CAS 号
性状

固体

颜色

Light yellow to yellow

中文名称

3-邻甲基槲皮素;3-O-甲基槲皮素

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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (158.10 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 3.1620 mL 15.8098 mL 31.6196 mL
5 mM 0.6324 mL 3.1620 mL 6.3239 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。-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: 0.62 mg/mL (1.96 mM); 澄清溶液; 超声助溶

    此方案可获得 0.62 mg/mL的澄清溶液。

    1 mL 工作液为例,取 100 μL 6.2 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: 0.62 mg/mL (1.96 mM); 澄清溶液; 超声助溶

    此方案可获得 0.62 mg/mL的澄清溶液。

    1 mL 工作液为例,取 100 μL 6.2 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
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。-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 3.1620 mL 15.8098 mL 31.6196 mL 79.0489 mL
5 mM 0.6324 mL 3.1620 mL 6.3239 mL 15.8098 mL
10 mM 0.3162 mL 1.5810 mL 3.1620 mL 7.9049 mL
15 mM 0.2108 mL 1.0540 mL 2.1080 mL 5.2699 mL
20 mM 0.1581 mL 0.7905 mL 1.5810 mL 3.9524 mL
25 mM 0.1265 mL 0.6324 mL 1.2648 mL 3.1620 mL
30 mM 0.1054 mL 0.5270 mL 1.0540 mL 2.6350 mL
40 mM 0.0790 mL 0.3952 mL 0.7905 mL 1.9762 mL
50 mM 0.0632 mL 0.3162 mL 0.6324 mL 1.5810 mL
60 mM 0.0527 mL 0.2635 mL 0.5270 mL 1.3175 mL
80 mM 0.0395 mL 0.1976 mL 0.3952 mL 0.9881 mL
100 mM 0.0316 mL 0.1581 mL 0.3162 mL 0.7905 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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产品名称:
3-O-Methylquercetin
目录号:
HY-N1860
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