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EP4 receptor antagonist 1
EP4 receptor antagonist 1 是一种高效的,竞争性的,选择性前列腺素类 EP4 受体拮抗剂。可用于癌症免疫研究。EP4 receptor antagonist 1 抑制人和小鼠 EP4 受体,IC50 分别为 6.1 nM 和 16.2 nM。对人 EP1,EP2 和 EP3 受体的 IC50 >10 μM。
EP4 receptor antagonist 1 Chemical Structure
CAS No. : 2287259-07-6
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生物活性 |
EP4 receptor antagonist 1 is a highly potent and selective competitive prostanoid EP4 receptor antagonist for cancer immunotherapy. EP4 receptor antagonist 1 inhibits human and mouse EP4 receptor with IC50s of 6.1 nM and 16.2 nM, respectively. IC50s >10 μM for human EP1, EP2,and EP3 receptors[1]. |
IC50 & Target |
IC50: 6.1 nM (human EP4 receptor), 16.2 nM (mouse EP4 receptor)[1] |
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体外研究 (In Vitro) |
The antagonistic effect of EP4 receptor antagonist 1 (Compounds 59) on human EP4 in calcium flux assay with an IC50 of 6.1±0.2 nM in CHO-Gα16 cells overexpressing human EP4 receptor. The antagonistic effect of EP4 receptor antagonist 1 on human EP4 in calcium flux assay with an IC50 of 16.2±1.7 nM in CHO-Gα16 cells overexpressing mouse EP4 receptor[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot Analysis[1]
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体内研究 (In Vivo) |
EP4 receptor antagonist 1 (16, 50, and 150 mg/kg; orally; once daily for two weeks) causes significant inhibition of tumor growth in BALB/c female mice. No significant body weight loss is found in any mouse cohorts. EP4 receptor antagonist 1 is well tolerated in mice at the tested dosage[1]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.
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分子量 |
458.43 |
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Formula |
C23H21F3N4O3 |
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CAS 号 |
2287259-07-6 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
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参考文献 |
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