1. GPCR/G Protein Neuronal Signaling
  2. Prostaglandin Receptor Amyloid-β
  3. EP2 receptor antagonist-3

EP2 receptor antagonist-3 是一种具有选择性的 EP2 受体 (EP2 receptor) 拮抗剂 (hEP2 SPA实验测定 IC50 为 8 nM;hEP2 cAMP 实验测定 IC5 为 50 nM)。EP2 receptor antagonist-3 可增加巨噬细胞介导的 Amyloid-β 斑块清除。EP2 receptor antagonist-3 在 CD-1 小鼠中显示出适中的清除率和良好的暴露,在小鼠和大鼠中具有良好的中枢神经系统 (CNS) 暴露。EP2 receptor antagonist-3 可用于阿尔茨海默病的研究。

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EP2 receptor antagonist-3

EP2 receptor antagonist-3 Chemical Structure

CAS No. : 1799626-16-6

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  • 生物活性

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  • 参考文献

生物活性

EP2 receptor antagonist-3 is a selective EP2 receptor antagonist (IC50: 8 nM in hEP2 SPA assay, 50 nM in hEP2 cAMP assay). EP2 receptor antagonist-3 increases the macrophage-mediated clearance of Amyloid-β plaques. EP2 receptor antagonist-3 shows moderate clearance and good exposure in CD-1 mice and good CNS exposure in mice and rats. EP2 receptor antagonist-3 can be used for the study of alzheimer’s diseases[1].

体外研究
(In Vitro)

EP2 receptor antagonist-3 (Benzoxazepine 52) 在 SPA 实验中对人、大鼠和小鼠 EP2 受体表现出强效抑制,IC50 值分别为 0.008 μM、0.01 μM 和 0.01 μM,在 cAMP 实验中 IC50 值分别为 0.05 μM、0.03 μM 和 0.004 μM[1]
EP2 receptor antagonist-3 (0.001-3.0 μM, 24 h) 在取自 18 月龄的 Tg2576 小鼠脑切片上表现出对 IC21 介导的 Aβ 斑块吞噬作用的剂量依赖性增加[1]

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

分子量

423.87

Formula

C23H19ClFN3O2

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
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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.

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产品名称:
EP2 receptor antagonist-3
目录号:
HY-176293
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