2. GPCR/G Protein NF-κB Metabolic Enzyme/Protease Immunology/Inflammation Neuronal Signaling Membrane Transporter/Ion Channel PI3K/Akt/mTOR Stem Cell/Wnt MAPK/ERK Pathway TGF-beta/Smad Epigenetics
  3. Protease Activated Receptor (PAR) NF-κB Reactive Oxygen Species (ROS) Calcium Channel Akt ERK p38 MAPK PKC
  4. 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].

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7,4'-Dimethoxy-3-hydroxyflavone Chemical Structure

7,4'-Dimethoxy-3-hydroxyflavone Chemical Structure

CAS No. : 13198-99-7

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7,4'-Dimethoxy-3-hydroxyflavone Related Antibodies

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NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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ERK ERK1 ERK2 ERK5 ERK8

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PKC PKCα PKCβ PKCγ PKCδ PKCε PKCη PKCζ PKCθ PKCμ PKC-ι ℩ PKCι

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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].

In Vitro

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.

7,4'-Dimethoxy-3-hydroxyflavone Related Antibodies

Real Time qPCR[1]

Cell Line: EA.hy926 cells incubated with high glucose (HG)
Concentration: 1, 3, 10 μM
Incubation Time: 6 h
Result: Inhibited high glucose-induced F2RL3 expression in a concentration-dependent manner, with complete inhibition at 10 μM.

Western Blot Analysis[1]

Cell Line: EA.hy926 cells incubated with high glucose (HG)
Concentration: 10 μM
Incubation Time: 48 h
Result: Abolished the high glucose-induced PAR4 protein expression.

Real Time qPCR[1]

Cell Line: EA.hy926 cells incubated with high glucose (HG)
Concentration: 1, 10 μM
Incubation Time: 24 h
Result: Decreased the expression of VCAM1, ICAM1, CCL2, TNF, IL1B and F3

Immunofluorescence[1]

Cell Line: EA.hy926 cells incubated with high glucose (HG)
Concentration: 10 μM
Incubation Time: 48 h
Result: Prevented the ROS production induced by high glucose.
Abolished high glucose-induced NF-κB activation.
In Vivo

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.

Animal Model: 4 weeks male C57BL/6J mice injected STZ (i.p. 180 mg/kg)[1]
Dosage: 20 mg/kg
Administration: Daily by oral gavage for 21 days
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.
Animal Model: Male Balb/c mice (20-25 g, age 6-8 weeks) model of FeCl3-induced arterial thrombosis[2]
Dosage: 1, 3, and 7.5 mg/kg
Administration: i.p. for 30 min before induction of thrombosis
Result: Prevent thrombosis in mice without affecting bleeding time
Molecular Weight

298.29

Formula

C17H14O5
CAS No.
SMILES

COC1=CC=C(C=C1)C2=C(C(C3=CC=C(C=C3O2)OC)=O)O
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7,4'-Dimethoxy-3-hydroxyflavone Related Classifications

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  • 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.

Keywords:

7,4'-Dimethoxy-3-hydroxyflavone13198-99-7Protease Activated Receptor (PAR)NF-κBReactive Oxygen Species (ROS)Calcium ChannelAktERKp38 MAPKPKCThrombin receptorsNuclear factor-κBNuclear factor-kappaBCa2+ channelsCa channelsPKBProtein kinase BExtracellular signal regulated kinasesProtein kinase CHyperglycemiaROSPAR4AKTP38 MAPKInhibitorinhibitorinhibit

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