7,4'-Dimethoxy-3-hydroxyflavone
7,4'-Dimethoxy-3-hydroxyflavone is an orally active PAR4 antagonist. 7,4'-Dimethoxy-3-hydroxyflavone inhibits PAR4-mediated human platelet aggregation with an IC50 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 prevents vascular PAR4 expression, endothelial dysfunction and ameliorates oxidative stress in Streptozotocin (STZ) (HY-13753)-induced diabetic mice. 7,4'-Dimethoxy-3-hydroxyflavone prevents thrombosis in mice without affecting bleeding time[1][2].
For research use only. We do not sell to patients.
- CAS No.: 13198-99-7
- Formula: C17H14O5
- Molecular Weight:298.29
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
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PAR4 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HL-60 | IC50 |
148 μM
Compound: 7
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Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
Cytotoxicity against human HL60 cells after 72 hrs by MTT assay
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[PMID: 25014747] |
7,4'-Dimethoxy-3-hydroxyflavone prevents (DMF-OH) (1-10 μM, 6-48 h) high glucose-induced endothelial PAR4 expression in EA.hy 926 cells[1].
7,4'-Dimethoxy-3-hydroxyflavone (1-10 μM, 6-48 h) prevents high glucose-induced endothelial PAR4 function by abolishing PAR4-mediated Ca2+ responses and reducing Ca2+ responses to AYPGKF-NH₂ (PAR4-activating peptide) or thrombin in EA.hy 926 cells[1].
7,4'-Dimethoxy-3-hydroxyflavone (1-10 μM, 24 h) prevents high glucose-induced PAR4-induced aggravation of endothelial dysfunction in EA.hy 926 cells[1].
7,4'-Dimethoxy-3-hydroxyflavone (1-10 μM, 24 h) prevents high glucose-induced PAR4 expression through inhibition of ROS driven NF-κB activation in EA.hy 926 cells[1].
7,4'-Dimethoxy-3-hydroxyflavone (1-5 μM, 3-5 min) inhibits PAR4-mediated human platelet aggregation and secretion through inhibiting the activation of GPIIb/IIIa, which is the key step for platelet aggregation caused by PAR4-AP[2].
7,4'-Dimethoxy-3-hydroxyflavone (1-5 μM, 1-3 min) inhibits PAR4 downstream signaling pathways, including Ca2+/protein kinase C, Akt, ERK and p38 in platelet[2].
7,4'-Dimethoxy-3-hydroxyflavone (5-20 μM, 10 min) inhibits β-arrestin recruitment to PAR4 concentration-dependently in CHO-K1 cells[2].
7,4'-Dimethoxy-3-hydroxyflavone (5-20 μM, 3 min) enhances the efficacy of Vorapaxar (HY-10119) and Ticagrelor (HY-10064) in inhibiting thrombin-induced platelet aggregation[2].
7,4'-Dimethoxy-3-hydroxyflavone (5-10 μM, 10 min) decreases thrombus formation in whole blood under flow conditions[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:EA.hy926 cells incubated with high glucose (HG)
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Concentration:1, 3, 10 μM
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Incubation Time:6 h
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Result:Inhibited high glucose-induced F2RL3 expression in a concentration-dependent manner, with complete inhibition at 10 μM.
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Cell Line:EA.hy926 cells incubated with high glucose (HG)
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Concentration:10 μM
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Incubation Time:48 h
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Result:Abolished the high glucose-induced PAR4 protein expression.
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Cell Line:EA.hy926 cells incubated with high glucose (HG)
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Concentration:1, 10 μM
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Incubation Time:24 h
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Result:Decreased the expression of VCAM1, ICAM1, CCL2, TNF, IL1B and F3
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Cell Line:EA.hy926 cells incubated with high glucose (HG)
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Concentration:10 μM
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Incubation Time:48 h
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Result:Prevented the ROS production induced by high glucose.
Abolished high glucose-induced NF-κB activation.
7,4'-Dimethoxy-3-hydroxyflavone (DMF-OH) (20 mg/kg, oral gavage, daily for 21 days) prevents vascular PAR4 expression, endothelial dysfunction and ameliorates oxidative stress in Streptozotocin (STZ) (HY-13753)-induced diabetic mice[1].
7,4'-Dimethoxy-3-hydroxyflavone(1-7.5 mg/kg, i.p., single dose) significantly protects from FeCl3-induced carotid arterial occlusions, without significantly affecting tail bleeding time[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:4 weeks male C57BL/6J mice injected STZ (i.p. 180 mg/kg)[1]
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Dosage:20 mg/kg
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Administration:Daily by oral gavage for 21 days
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Result:Did not affect STZ-induced hyperglycaemia and body weight loss.
Blunted the up-regulation of PAR4.
Improved the aortic wall thickening and irregular arrangement of smooth muscle cells of tunica media.
Blunted the increased expression of proinflammatory and procoagulant mediators in the aorta and prevented macrophage infiltration.
Prevented diabetes-induced increases in aortic 8-OHdG levels.
Reduced the increased serum MDA levels.
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Animal Model:Male Balb/c mice (20-25 g, age 6-8 weeks) model of FeCl3-induced arterial thrombosis[2]
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Dosage:1, 3, and 7.5 mg/kg
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Administration:i.p. for 30 min before induction of thrombosis
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Result:Prevent thrombosis in mice without affecting bleeding time
Chemical Information
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CAS No. 13198-99-7
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Molecular Weight 298.29
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Formula C17H14O5
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SMILES
COC1=CC=C(C=C1)C2=C(C(C3=CC=C(C=C3O2)OC)=O)O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Tsai JY, et al. 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. [Content Brief]
[2]. ] Lin YT, et al. 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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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