Cat. No. | Product Name | Target | Signaling Pathways |
---|---|---|---|
T77699 |
EP4-IN-1
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Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
EP4-IN-1 是一种有效的前列腺素 EP4 受体抑制剂,具有潜在的抗肿瘤抗炎和镇痛活性,可用于研究免疫疾病和肿瘤疾病。 | |||
T9622 |
MF-766
|
Prostaglandin Receptor | GPCR/G Protein; Immunology/Inflammation |
MF-766 是高效的、具有口服活性的EP4选择性拮抗剂,Ki 为 0.23 nM。它在功能检测中表现为一种完整的拮抗剂,其 IC50为 1.4 nM (在 10% HS 存在时变成 1.8 nM)。它具有用于癌症和炎症疾病研究的价值。 | |||
T83779 |
EP4 Antagonist 14
Prostaglandin E2 Receptor 4 Antagonist 14,PGE2 Receptor 4 Antagonist 14 |
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EP4 antagonist 14是一种前列腺素E2(PGE2)受体亚型EP4的拮抗剂,其在使用表达人源受体的HEK293细胞的报告基因测定中的IC50值为1.1 nM。它还能抑制PGE2诱导的同种细胞中的β-阿雷斯汀招募(IC50 = 0.9 nM)。EP4 antagonist 14(10 µM)能减少RAW 264.7巨噬细胞中PGE2诱导的mRNA表达,这些mRNA编码Il-4、巨噬细胞甘露糖受体1(Mrc1)、几丁质酶样蛋白3(Chil3)、趋化因子(C-X-C)基序配体1(Cxcl1)、表达在髓样细胞上的触发受体2(Trem2)和精氨酸酶-1(Arg1)。在体内,EP4 antagonist 14(每天30 mg/kg),结合抗PD-1抗体,能够在CT26小鼠结肠癌模型中抑制肿瘤生长并增加CD8+ T细胞对肿瘤的浸润。 | |||
T37996 |
17-phenyl trinor Prostaglandin E2 ethyl amide
17-phenyl trinor Prostaglandin E2 ethyl amide |
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17-phenyl trinor PGE2 ethyl amide is derived from 17-phenyl trinor PGE2, a synthetic analog of PGE2 that acts as an agonist of EP1 and EP3 receptors in mice (Ki = 14 and 3.7 nM, respectively) and EP1, EP3, and EP4 in rats (Ki = 25, 4.3, and 54 nM, respectively). 17-phenyl trinor PGE2 causes contraction of guinea pig ileum at a concentration of 11 μM and is 4.4 times more potent than PGE2 as an antifertility agent in hamsters. Modification of the C-1 carboxyl group to an ethyl amide serves to inc... |