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) -induced diabetic mice. 7,4'-Dimethoxy-3-hydroxyflavone prevents thrombosis in mice without affecting bleeding time[1][2].

Product Specifications

CAS Number

13198-99-7

UNSPSC

12352005

Target

Akt; Calcium Channel; ERK; NF-κB; p38 MAPK; PKC; Protease Activated Receptor (PAR) ; Reactive Oxygen Species (ROS)

Related Pathways

Epigenetics; GPCR/G Protein; Immunology/Inflammation; MAPK/ERK Pathway; Membrane Transporter/Ion Channel; Metabolic Enzyme/Protease; Neuronal Signaling; NF-κB; PI3K/Akt/mTOR; Stem Cell/Wnt; TGF-beta/Smad

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease; Cardiovascular Disease

Smiles

COC1=CC=C(C=C1)C2=C(C(C3=CC=C(C=C3O2)OC)=O)O

Molecular Formula

C17H14O5

Molecular Weight

298.29

References & Citations

[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.|[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.