2. GPCR/G Protein NF-κB
  3. P2Y Receptor Keap1-Nrf2
  4. P2Y1 antagonist 4

P2Y1 antagonist 4 是一种选择性的 P2Y1 receptor 拮抗剂，具有出色的血脑屏障渗透性。P2Y1 antagonist 4 抑制 ADP 诱导的兔洗涤血小板中 P2Y1 receptor 介导的细胞质 Ca2+ 增加 (IC50 = 1.95 μM) 和血小板聚集 (IC50 = 3.24 μM)。P2Y1 antagonist 4 显著上调 H2O2 处理的 HT22 细胞中核 Nrf2 蛋白的水平。P2Y1 antagonist 4 在小鼠急性心肌梗死模型中减少心肌梗死面积。P2Y1 antagonist 4 可用于缺血性中风和心肌梗死的研究。

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P2Y1 antagonist 4

P2Y1 antagonist 4 Chemical Structure

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P2Y1 antagonist 4 相关抗体

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查看 P2Y Receptor 亚型特异性产品:

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P2Y1 Receptor P2Y2 Receptor P2Y6 Receptor P2Y12 Receptor P2Y13 Receptor P2Y14 Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

P2Y1 antagonist 4 is a selective P2Y1 receptor antagonist with excellent blood-brain barrier (BBB) penetration. P2Y1 antagonist 4 inhibits P2Y1 receptor-mediated cytosolic Ca2+ increase (IC50 = 1.95 μM) and platelet aggregation (IC50 = 3.24 μM) induced by ADP in rabbit washed platelets. P2Y1 antagonist 4 significantly upregulates the level of nuclear Nrf2 protein in H2O2-treated HT22 cells. P2Y1 antagonist 4 reduces myocardial infarct size in a mouse acute myocardial infarction (MI) model. P2Y1 antagonist 4 can be used for the study of ischemic stroke and myocardial infarction[1].

IC50 & Target[1]

P2Y1 Receptor

 

体外研究
(In Vitro)

P2Y1 antagonist 4 (Compound 12g) 抑制 ADP 诱导的兔洗涤血小板中 P2Y1 受体介导的细胞质 Ca2+ 增加 (IC50 = 1.95 μM) 和血小板聚集 (IC50 = 3.24 μM) [1]。
P2Y1 antagonist 4 (10 μM, 24 小时) 显著提高 H2O2 诱导的氧化应激损伤 HT22 海马神经元的细胞活力 [1]。
P2Y1 antagonist 4 (10 μM, 16 小时) 显著上调 H2O2 处理的 HT22 细胞中核 Nrf2 蛋白的水平 [1]。

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

P2Y1 antagonist 4 相关抗体:
体内研究
(In Vivo)

P2Y1 antagonist 4 (Compound 12g) (5-20 mg/kg，静脉注射，LAD 结扎后立即单次给药，24 小时评估) 可剂量依赖性地减少雄性 C57BL/6 小鼠的心肌梗死面积，并降低血清 CK-MB/LDH 水平[1]。

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

Animal Model: The chest was opened at the fourth costal space of the left chest wall along the left edge of the sternum to expose the heart, and a 7-0 silk thread was threaded through a live knot 2 mm from the left anterior descending coronary artery (LAD) branch for permanent ligation in Male C57BL/6 mice (20-25 g, 5-6 weeks old)[1]
Dosage: 5, 10, 20 mg/kg
Administration: i.v., single dose immediately post-LAD ligation, 24 h evaluation
Result: Reduced myocardial infarct size dose-dependently.
Alleviated myocardial cytolysis and reduces fibrosis.
分子量

446.33

Formula

C21H11F5N4O2
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

P2Y1 antagonist 4 相关分类

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Help & FAQs
  • 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:

P2Y1 antagonist 4P2Y ReceptorKeap1-Nrf2P2Y1 receptorischemic strokemyocardial infarctionNrf2Inhibitorinhibitorinhibit

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