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- Cyclooxygenase (COX)
- EP4 Receptor Antagonist 1
EP4 Receptor Antagonist 1
An EP4 receptor antagonist
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包装价格促销价数量
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1mg￥1150.00920.00- +
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5mg￥4800.003840.00- +
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10mg￥9025.007220.00- +
- 货号: ajcx22426
- CAS: 2287259-07-6
- 别名:
- 分子式: C23H21F3N4O3
- 分子量: 458.4
- 纯度: ＞98%
- 溶解度: DMF: 30 mg/ml,DMSO: 30 mg/ml,DMSO:PBS (pH 7.2) (1:6): 0.14 mg/ml
- 储存: Store at -20°C
- 库存: 现货
Background
EP4 receptor antagonist 1 is an antagonist of the prostaglandin E2 (PGE2) receptor EP4 that has an IC50 value of 6.1 nM in a calcium flux assay using CHO cells co-expressing the human receptor and Gα16.1 It is selective for EP4 over EP1, EP2, and EP3 receptors (IC50s = >10,000 nM for all). EP4 receptor antagonist 1 inhibits PGE2-induced β-arrestin recruitment in HEK293 cells expressing EP4. It reverses ERK phosphorylation induced by PGE2 in CHO cells expressing EP4 and decreases GM-CSF-induced expression of Il1b, Il4ra, Il6, Arg1, Cox2, and Il10 in RAW 264.7 cells when used at a concentration of 10 µM. EP4 receptor antagonist 1 (50 and 150 mg/kg once per day) reduces tumor volume and increases infiltration of CD8+ T cells into tumors in a murine colon carcinoma model.
1.Yang, J.-J., Yu, W.-W., Hu, L.-L., et al.Discovery and characterization of 1 H-1,2,3-triazole derivatives as novel prostanoid EP4 receptor antagonists for cancer immunotherapyJ. Med. Chem.63(2)569-590(2020)
