2. GPCR/G Protein Immunology/Inflammation
  3. Prostaglandin Receptor Interleukin Related
  4. EP4 receptor antagonist 7

EP4 receptor antagonist 7 (Compound 14) 是前列腺素 E2 (PGE2) 受体亚型 EP4 的拮抗剂，IC50 值为 1.1 nM。EP4 receptor antagonist 7 在 HEK293 细胞中抑制 PGE2 诱导的 β-阻滞蛋白募集，IC50 值为 0.9 nM。EP4 receptor antagonist 7 在 RAW 264.7 巨噬细胞中降低 PGE2 诱导的 IL-4、巨噬细胞甘露糖受体 1 (Mrc1)、几次质酶样蛋白 3 (Chil3)、趋化因子 (C-X-C) 基序配体 1 (Cxcl1)、髓样细胞上表达的触发受体 2 (Trem2) 和精氨酸酶1 (Arg1) mRNA的表达。在 CT26 小鼠结肠癌模型中，EP4 receptor antagonist 7 联合抗 PD-1 抗体抑制肿瘤生长并增加 CD8+ T 细胞向肿瘤的浸润。

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EP4 receptor antagonist 7 Chemical Structure

EP4 receptor antagonist 7 Chemical Structure

CAS No. : 3035217-40-1

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EP4 receptor antagonist 7 相关抗体

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生物活性

EP4 receptor antagonist 7 (Compound 14) is an antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4 with an IC50 value of 1.1 nM. EP4 receptor antagonist 7 inhibits PGE2-induced β-arrestin recruitment in HEK293 cells with an IC50 value of 0.9 nM. EP4 receptor antagonist 7 decreases PGE2-induced expression of mRNA encoding IL-4, macrophage mannose receptor 1 (Mrc1), chitinase-like protein 3 (Chil3), chemokine (C-X-C) motif ligand 1 (Cxcl1), triggering receptor expressed on myeloid cells 2 (Trem2), and arginase-1 (Arg1), in RAW 264.7 macrophages. EP4 receptor antagonist 7 combined with an anti-PD-1 antibody inhibits tumor growth and increases infiltration of CD8+ T cells into tumors in a CT26 murine colon cancer model[1].

分子量

453.41

Formula

C24H18F3N3O3
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.
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EP4 receptor antagonist 7 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

EP4 receptor antagonist 73035217-40-1Prostaglandin ReceptorInterleukin RelatedILPGE2β-arrestinHEK293 cellsIL-4Mrc1Chil3Cxcl1Trem2Inhibitorinhibitorinhibit

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