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

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.

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3-O-Methylquercetin Chemical Structure

3-O-Methylquercetin Chemical Structure

CAS No. : 1486-70-0

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Based on 1 publication(s) in Google Scholar

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Description

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].

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]
In Vitro

3-O-Methylquercetin (1-10 μM; 24 h) inhibits NO production (IC50: 4.23μM) and the expression of iNOS protein and mRNA in a concentration-dependent manner in RAW 264.7 cells treated with LPS (HY-D1056)[1].
3-O-Methylquercetin (1-30 μM; 15 min) can relax the trachea of guinea pig[2].
3-o-methylquercetin (1-100 μM;20-24 h) improves the survival rate of rat cortical cells treated with H2O2[3].

MedChemExpress (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.
In Vivo

3-O-Methylquercetin (3-30 μmol/kg ≈ 0.95-9.5 mg/kg; Intraperitoneal injection; 3 times) shows improvement in airway hyperresponsiveness induced by oobumin (HY-W250978)[4].

MedChemExpress (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.
Molecular Weight

316.26

Formula

C16H12O7

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C(OC)=C(C2=CC=C(O)C(O)=C2)OC3=CC(O)=CC(O)=C13

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (158.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 0.62 mg/mL (1.96 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 0.62 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.2 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 0.62 mg/mL (1.96 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 0.62 mg/mL.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.2 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
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%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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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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.

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Product Name:
3-O-Methylquercetin
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