1. Anti-infection
  2. Fungal Parasite Bacterial
  3. 5,7,3',4'-Tetramethoxyflavone

5,7,3',4'-Tetramethoxyflavone, an orally active polymethoxyflavones (PMFs) that can be isolated from M. exotica, possesses various bioactivities, including anti-fungal, anti-malarial, anti-mycobacterial, and anti-inflammatory activities. 5,7,3',4'-Tetramethoxyflavone exhibits chondroprotective activity by targeting β-catenin signaling.

For research use only. We do not sell to patients.

5,7,3',4'-Tetramethoxyflavone Chemical Structure

5,7,3',4'-Tetramethoxyflavone Chemical Structure

CAS No. : 855-97-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Solution
10 mM * 1 mL in DMSO In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

5,7,3',4'-Tetramethoxyflavone, an orally active polymethoxyflavones (PMFs) that can be isolated from M. exotica, possesses various bioactivities, including anti-fungal, anti-malarial, anti-mycobacterial, and anti-inflammatory activities. 5,7,3',4'-Tetramethoxyflavone exhibits chondroprotective activity by targeting β-catenin signaling[1].

IC50 & Target

Plasmodium

 

Cellular Effect
Cell Line Type Value Description References
RAW264.7 IC50
3.13 μM
Compound: 3y
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated PGE2 production by ELISA
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated PGE2 production by ELISA
[PMID: 28408221]
RAW264.7 IC50
32.5 μM
Compound: 3y
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated NO production by ELISA
Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-stimulated NO production by ELISA
[PMID: 28408221]
RAW264.7 IC50
73.94 μM
Compound: 3y
Cytotoxicity against mouse RAW264.7 cells by MTT assay
Cytotoxicity against mouse RAW264.7 cells by MTT assay
[PMID: 28408221]
In Vitro

5,7,3',4'-Tetramethoxyflavone (5-20 μg/mL, 24 h) inhibits the expression of EP2, EP4, bcatenin and COX-2 gene in chondrocytes[1].
5,7,3',4'-Tetramethoxyflavone (5-20 μg/mL, 48 h) inhibits the protein expression of EP/cAMP/PKA signaling pathway and β-catenin signaling pathway in chondrocytes[1].
5,7,3',4'-Tetramethoxyflavone (5-20 μg/mL, 4 h) protects chondrocytes from apoptosis through regulating IRE1α[2].
5,7,3',4'-Tetramethoxyflavone (5-20 μg/mL, 4 h) reverses the expression pattern of endoplasmic reticulum (ER) stress genes due to IRE1α deficiency[2].

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

Cell Line:
Concentration:
Incubation Time:
Result:

Western Blot Analysis[2]

Cell Line: Chondrocytes
Concentration: 5-20 μg/mL
Incubation Time: 4 h
Result: Increased the protein level of Bcl-2 and XBP1s.
Decreased the expression of pro-apoptotic factors CHOP/caspase-3 and stress kinase JNK.
In Vivo

5,7,3',4'-Tetramethoxyflavone (25-100 mg/kg, i.g.) exhibits chondroprotective activity in rats[1].
5,7,3',4'-Tetramethoxyflavone (5-20 mg/kg; i.v., p.o.) has the absolute bioavailability of 14.3 % in rats[3].
1.19
Pharmacokinetic Analysis in Sprague-dawley Rats Model[3]

Route Dose (mg/kg) AUC (min μg/mL) AUC/Dose (min/mL) t1/2 (h) Tmax (h) Cmax (ng/mL) Bioavailability (%)
i.v. 5 161.49 ± 58.78 0.1154 ± 0.0420 62.85 ± 27.92 / / 14.3
p.o. 50 231.43 ± 71.87 0.0165 ± 0.0051 273.76 ± 90.23 190.34 ± 24.50 0.79 ± 0.30 /

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

Animal Model: Rat knee OA model[1]
Dosage: 25-100 mg/kg
Administration: i.g.
Result: Decreased the contents of IL-1b, TNF-a, and PGE2 in a dose-dependent manner.
Decreases the expression of the inflammatory cytokines in rat knee osteoarthritis (OA) synovial fluid (SF) lavages.
Inhibited chondrocytes hypertrophy and decreased the cartilage thickness.
Exhibited down regulation of b-catenin in a dose-dependent manner.
Molecular Weight

342.35

Formula

C19H18O6

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C=C(C2=CC=C(OC)C(OC)=C2)OC3=C1C(OC)=CC(OC)=C3

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 6.67 mg/mL (19.48 mM; ultrasonic and warming and heat to 60°C; 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 2.9210 mL 14.6049 mL 29.2099 mL
5 mM 0.5842 mL 2.9210 mL 5.8420 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 (protect from light). 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)

Mass
=
Concentration
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Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: ≥ 0.67 mg/mL (1.96 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 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: ≥ 0.67 mg/mL (1.96 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (6.7 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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
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).

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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

Purity: 99.15%

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 (protect from light). 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 2.9210 mL 14.6049 mL 29.2099 mL 73.0247 mL
5 mM 0.5842 mL 2.9210 mL 5.8420 mL 14.6049 mL
10 mM 0.2921 mL 1.4605 mL 2.9210 mL 7.3025 mL
15 mM 0.1947 mL 0.9737 mL 1.9473 mL 4.8683 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:
5,7,3',4'-Tetramethoxyflavone
Cat. No.:
HY-N7030
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