7,4'-Dimethoxy-3-hydroxyflavone

• Description:

  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].

• 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.

• Shipping Conditions:

  Room temperature

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  PAR4

• CAS Number:

  13198-99-7