2. GPCR/G Protein NF-κB Immunology/Inflammation Metabolic Enzyme/Protease 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 是一种口服有效的 PAR4 拮抗剂。7,4'-Dimethoxy-3-hydroxyflavone 抑制PAR4 介导的人血小板聚集的 IC50 为 1.4 μM。7,4'-Dimethoxy-3-hydroxyflavone 可抑制 PAR4 介导的人血小板聚集及其相关的信号通路，包括 NF-κB、 Ca2+/蛋白激酶C (PKC)、Akt、ERK 和 p38。7,4'-Dimethoxy-3-hydroxyflavone 在链脲佐菌素 (STZ) (HY-13753) 诱导的糖尿病小鼠模型中能抑制血管 PAR4 表达、改善内皮功能障碍并缓解氧化应激。7,4'-Dimethoxy-3-hydroxyflavone 在不影响出血时间的情况下预防小鼠血栓形成[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 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

7,4'-Dimethoxy-3-hydroxyflavone (1-10 μM, 6-48 h) 可抑制高糖诱导的 EA.hy 926 细胞内皮 PAR4表达，而其他 PAR4 拮抗剂 7,4'-dimethoxyflavone (DMF, 10 μM), YD-3 (HY-111766) (1 μM) 和 BMS-986120 (HY-19837) (BMS; 1 nM) 均无此作用[1]。

7,4'-Dimethoxy-3-hydroxyflavone (1-10 μM, 6-48 h) 能在 EA.hy 926 细胞中阻断高糖诱导的内皮 PAR4 功能，表现为：完全抑制 PAR4 介导的 Ca2+响应和显著降低对 AYPGKF-NH₂ (PAR4激活肽) 或凝血酶的 Ca2+ 响应[1]。

7,4'-Dimethoxy-3-hydroxyflavone (1-10 μM, 24 h) 可阻止 EA.hy 926 细胞中高糖环境下PAR4加剧的内皮功能障碍[1]。

7,4'-Dimethoxy-3-hydroxyflavone (1-10 μM, 24 h) 在 EA.hy 926 细胞中通过抑制 ROS 驱动的 NF-κB 活化，从而抑制高糖诱导的 PAR4 表达[1]。

7,4'-Dimethoxy-3-hydroxyflavone (1-5 μM, 3-5 min) 通过抑制 GPIIb/IIIa 的活化来抑制 PAR4 介导的人血小板聚集和分泌，这是PAR4激活肽引发血小板聚集的关键步骤[2]。

7,4'-Dimethoxy-3-hydroxyflavone (1-5 μM, 1-3 min) 抑制血小板中 PAR4 下游信号通路，包括 Ca2+/ 蛋白激酶 C、Akt、ERK 和 p38[2]。

7,4'-Dimethoxy-3-hydroxyflavone (5-20 μM, 10 min) 在 CHO-K1 细胞中浓度依赖性地抑制 β-抑制蛋白向PAR4 的募集[2]。

7,4'-Dimethoxy-3-hydroxyflavone (5-20 μM, 3 min) 可增强 Vorapaxar (HY-10119) 和Ticagrelor (HY-10064) 抑制凝血酶诱导的血小板聚集的效果[2]。

7,4'-Dimethoxy-3-hydroxyflavone (5-10 μM, 10 min) 在流动条件下减少全血中的血栓形成[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

7,4'-Dimethoxy-3-hydroxyflavone 相关抗体:

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.
体内研究
(In Vivo)

7,4'-Dimethoxy-3-hydroxyflavone (DMF-OH) (20 mg/kg，口服，每日给药持续 21 天) 在 Streptozotocin (STZ) (HY-13753) 诱导的糖尿病小鼠模型中抑制血管 PAR4 表达，改善内皮功能障碍并且减轻氧化应激损伤[1]。

7,4'-Dimethoxy-3-hydroxyflavone (1-7.5 mg/kg, i.p., single dose) 能显著预防 FeCl₃ 诱导的颈动脉闭塞，且不影响尾部出血时间[2]。

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
分子量

298.29

Formula

C17H14O5
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

7,4'-Dimethoxy-3-hydroxyflavone 相关分类

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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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