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7,4'-Dimethoxy-3-hydroxyflavone

Cat No.:V127510 Purity: ≥98%
7,4'-Dimethoxy-3-hydroxyflavone is an orally effective PAR4 antagonist.
7,4'-Dimethoxy-3-hydroxyflavone
7,4'-Dimethoxy-3-hydroxyflavone Chemical Structure CAS No.: 13198-99-7
Product category: PKC
This product is for research use only, not for human use. We do not sell to patients.
Size Price
500mg
1g
Other Sizes
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Product Description
7,4'-Dimethoxy-3-hydroxyflavone is an orally potent PAR4 antagonist. 7,4'-Dimethoxy-3-hydroxyflavone inhibits PAR4-mediated human platelet aggregation with an IC50 value of 1.4 μM. 7,4'-Dimethoxy-3-hydroxyflavone inhibits PAR4-mediated human platelet aggregation and PAR4 signaling pathways, including NF-κB, Ca2+/protein kinase C, Akt, ERK, and p38. 7,4'-Dimethoxy-3-hydroxyflavone inhibits vascular PAR4 expression and endothelial dysfunction in streptozotocin (STZ)-induced diabetic mice and improves oxidative stress. 7,4'-Dimethoxy-3-hydroxyflavone prevents thrombosis in mice without affecting bleeding time [1][2].
Biological Activity I Assay Protocols (From Reference)
ln Vitro
7,4'-Dimethoxy-3-hydroxyflavone (DMF-OH) (1-10 μM, 6-48 h) can inhibit high glucose-induced PAR4 expression in the endothelial cells of EA.hy 926 cells [1]. 7,4'-Dimethoxy-3-hydroxyflavone (1-10 μM, 6-48 h) can inhibit high glucose-induced endothelial PAR4 function by eliminating PAR4-mediated Ca2+ response and reducing the Ca2+ response of EA.hy 926 cells to AYPGKF-NH₂ (PAR4 activating peptide) or thrombin [1]. 7,4'-Dimethoxy-3-hydroxyflavone (1-10 μM, 24 h) can inhibit the PAR4-mediated exacerbation of high glucose-induced EA.hy 926 cell endothelial dysfunction [1]. 7,4'-Dimethoxy-3-hydroxyflavone (1-10 μM, 24 h) inhibited PAR4 expression in high glucose-induced EA.hy 926 cells by suppressing ROS-driven NF-κB activation [1]. 7,4'-Dimethoxy-3-hydroxyflavone (1-5 μM, 3-5 min) inhibited PAR4-mediated human platelet aggregation and secretion by suppressing GPIIb/IIIa activation, which is a key step in PAR4-AP-induced platelet aggregation [2]. 7,4'-Dimethoxy-3-hydroxyflavone (1-5 μM, 1-3 min) inhibited downstream signaling pathways of PAR4 in platelets, including Ca2+/protein kinase C, Akt, ERK, and p38 [2]. 7,4'-Dimethoxy-3-hydroxyflavone (5-20 μM, 10 min) inhibited the recruitment of β-arrestin to PAR4 in CHO-K1 cells in a concentration-dependent manner [2]. 7,4'-Dimethoxy-3-hydroxyflavone (5-20 μM, 3 min) enhanced the inhibitory effects of Vorapaxar and Ticagrelor on thrombin-induced platelet aggregation [2]. 7,4'-Dimethoxy-3-hydroxyflavone (5-10 μM, 10 min) reduced thrombus formation in whole blood under flowing conditions [2].
ln Vivo
7,4'-Dimethoxy-3-hydroxyflavone (DMF-OH) (20 mg/kg, gavage, once daily for 21 days) inhibited vascular PAR4 expression and endothelial dysfunction in streptozotocin (STZ)-induced diabetic mice and improved oxidative stress [1]. 7,4'-Dimethoxy-3-hydroxyflavone (1-7.5 mg/kg, intraperitoneal injection, single dose) significantly protected mice from FeCl3-induced carotid artery occlusion without significantly affecting tail bleeding time [2].
Cell Assay
Real-time quantitative PCR[1]
Cell Types: EA.hy926 cells in high glucose (HG) culture.
Tested Concentrations: 1, 3, 10 μM
Incubation Duration: 6 hours
Experimental Results: High glucose-induced F2RL3 expression was inhibited in a concentration-dependent manner, and complete inhibition was achieved at 10 μM.
Western Blot analysis [1]
Cell Types: EA.hy926 cells were cultured under high glucose (HG) conditions.
Tested Concentrations: 10 μM Culture time: 48 hours
Experimental Results: High glucose-induced PAR4 protein expression was inhibited.
Real-time quantitative PCR[1]
Cell Types: EA.hy926 cells cultured in high glucose (HG)
Tested Concentrations: 1, 10 μM
Culture time: 24 hours
Experimental Results: The expression of VCAM1, ICAM1, CCL2, TNF, IL1B and F3 was reduced.
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Immunofluorescence [1]
Cell Types: EA.hy926 cells cultured in high glucose (HG)
Tested Concentrations: 10 μM
Incubation Duration: 48 hours
Experimental Results: Inhibited high glucose-induced ROS generation. Eliminated high glucose-induced NF-κB activation.

Animal Protocol
Animal/Disease Models:Four-week-old male C57BL/6J mice were intraperitoneally injected with STZ (180 mg/kg) [1]
Doses: 20 mg/kg
Route of Administration: Daily gavage for 21 days
Experimental Results: No effect on STZ-induced hyperglycemia and weight loss. Inhibited upregulation of PAR4. Improved aortic wall thickening and disordered arrangement of tunica media smooth muscle cells. Inhibited the increase in expression of pro-inflammatory and procoagulant mediators in the aorta and prevented macrophage infiltration. Prevented the increase in aortic 8-OHdG levels induced by diabetes. Reduced serum MDA levels.
Animal/Disease Models:Male Balb/c mice (20-25 g, 6-8 weeks old) FeCl3-induced arterial thrombosis model [2]
Doses: 1, 3 and 7.5 mg/kg
Route of Administration: Intraperitoneal injection 30 minutes before thrombosis induction
Experimental Results: Prevented thrombosis in mice without affecting bleeding time
References

[1]. 7,4'-dimethoxy-3-hydroxyflavone, a protease-activated receptor 4 (PAR4) inhibitor with antioxidant activity, ameliorates diabetic endothelial dysfunction. Br J Pharmacol. 2025 Jun 12.

[2]. Discovery of 7, 4'-dimethoxy-3-hydroxyflavone as a protease-activated receptor 4 antagonist with antithrombotic activity and less bleeding tendency in mice. Biochem Pharmacol. 2022 Aug;202:115152.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C17H14O5
Molecular Weight
298.29
CAS #
13198-99-7
Appearance
Typically exists as solids at room temperature
SMILES
COC1=CC=C(C=C1)C2=C(C(C3=CC=C(C=C3O2)OC)=O)O
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
Solubility (In Vivo)
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)


Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.3524 mL 16.7622 mL 33.5244 mL
5 mM 0.6705 mL 3.3524 mL 6.7049 mL
10 mM 0.3352 mL 1.6762 mL 3.3524 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

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  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

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