ep4 receptor

L-798106 (CM9) 是一种具有选择性和高效性的前列腺素类 EP3 受体拮抗剂 ，抑制 EP4，EP1 和 EP2 受体，抑制动脉粥样硬化中促炎细胞因子的水平，可减弱 PGE2 诱导的咳嗽。

L 888607 is an effective and selective CRTH2 agonist (Ki: 0.8 nM).

EP4 receptor antagonist 1 是一种有效的特异性前列腺素 EP4受体拮抗剂，对人和小鼠 EP4受体的 IC50分别为6.1 nM 和16.2 nM。 EP4 receptor antagonist 1 可用于癌症免疫治疗的研究。

EP4 receptor agonist 3 是一种 EP4 受体激动剂，用于研究 DSS 小鼠结肠炎模型。

EP4 receptor antagonist 7 (Compound 14) 是一种针对前列腺素 E2 (PGE2) 的 EP4 受体亚型的拮抗剂，其IC50值为1.1 nM。在HEK293细胞中，它抑制PGE2诱导的β-阻滞蛋白的募集，IC50为0.9 nM。在RAW 264.7巨噬细胞中，EP4 receptor antagonist 7 能降低PGE2诱导的IL-4、Mrc1、Chil3、Cxcl1、Trem2和Arg1等mRNA的表达。在CT26小鼠结肠癌模型中，该化合物与抗PD-1抗体联合使用可抑制肿瘤生长并增加CD8+ T细胞对肿瘤的浸润。

EP4 receptor antagonist 5 是一种高效且选择性的前列腺素 EP4 受体拮抗剂，能够减轻弗氏佐剂 (CFA) 模型中的炎症。

EP4 receptor antagonist 3 is a highly potent and specific inhibitor of the EP4 receptor. It is intended for research purposes in studying EP4 receptor-mediated diseases such as acute and chronic pain, osteoarthritis, rheumatoid arthritis, and cancer.

EP4 receptor antagonist 4 是一种EP4受体激动剂 (human pEC50 = 6.3)。

EP4 receptor antagonist 2 (compound 2-13) 是一种 EP4 受体的有效激动剂 (IC50: 7.8 nM)，具有抗肿瘤作用。

EP4 receptor agonist 2（compound 31）是一种有效的EP4 receptor激动剂，其EC50值为0.8 nM；而对EP2、EP3、EP4的Ki值分别为>100000、38000、3.1 nM。

Prostaglandin E2 (PGE2) 是一种天然激素样物质，参与平滑肌的收缩与松弛、血管的扩张与收缩、血压调节及炎症调节等多种生理功能，可用于诱导神经病理性疼痛模型。

CJ-42794 (CJ-042794)是前列腺素受体 EP4的选择性拮抗剂, 抑制[3H]-PGE2与 EP4受体结合的平均 pKi 为8.5, 对 EP4选择性比 EP1, EP2和 EP3高200多倍。

KAG-308 is an effective selective and orally active agonist of the EP4 receptor (Ki: 2.57 nM and EC50: 17 nM for human EP4 receptor), more selective over EP1, EP2, EP3, and IP receptor. KAG-308 suppresses colitis and promotes histological mucosal healing,

The prostaglandin E receptor 4 (EP4) is one of four G protein-coupled receptors that mediate the actions of prostaglandin E2 . Binding of PGE2 to the EP4 receptor causes an increase in intracellular cyclic AMP, which plays important roles in bone formation and resorption, cancer, and atherosclerosis. KMN-80 is a substituted γ-lactam (pyrrolidinone) derivative of PGE1 that acts as a selective and potent agonist of EP4 with an IC50 value of 3 nM (IC50 = 1.4 μM for EP3 and > 10 μM for all other prostanoid receptors). In functional assays it has been shown to stimulate secreted alkaline phosphatase gene reporter activity in EP4-transfected HEK293 cells with an EC50 value of 0.19 nM, demonstrating >5,000 and 50,000-fold selectivity against EP2 and TP, respectively. KMN-80 can induce the differentiation of bone marrow stem cells from both young and aged rats into osteoblasts in vitro (EC50s = 20 and 153 nM, respectively) and exhibits favorable tolerability up to at least 10 μM, whereas the EP4 agonist L-902,688 is highly cytotoxic at similar concentrations in these cells. KMN-80 has been used to repair calvarial defects in an in vivo rat craniomaxillofacial reconstruction model (rate of reduction in defect size equivalent to BMP-2 treated rats) and to promote bone formation in a rat incisor tooth socket model.

CAY10580 is a potent and selective prostaglandin EP 4 receptor agonist ( K i =35 nM).

MK-2894 是一种具有口服活性、选择性和高效性的前列腺素受体 4 (EP4 receptor，Ki=0.56 nM，IC50=2.5 nM) 的拮抗剂。MK-2894 具有抗炎活性，可用于研究和类风湿性关节炎相关的炎症。

Aganepag, a potent Prostanoid EP2 receptor agonist, exhibits remarkable selectivity with an EC50 of 0.19 nM, demonstrating no activity at the EP4 receptor. Its applications are primarily in the fields of wound healing, scar reduction, scar prevention, and the treatment and prevention of wrinkles.

L-161982 是选择性的 EP4 受体拮抗剂，可抑制 PGE2 诱导的 HCA-7 细胞 ERK 磷酸化和细胞增殖并可以缓解胶原诱导的小鼠关节炎。

L-902688 is an orally active EP4 receptor agonist (Ki: 0.38 nM; EC50: 0.6 nM). L-902688 displays >4,000-fold selective for EP4 over other EP and prostanoid receptors.

TP-16是一种新型高效且具有选择性的 EP4 拮抗剂，可阻断IMCs的功能，增强细胞毒性T细胞介导的体内肿瘤消除。

Rebamipide (OPC12759) 是一种粘膜保护剂，可诱导COX-2表达，增加PGE2水平，并以 COX-2 依赖性方式增强胃粘膜防御。

GSK726701A is a new type of prostaglandin E2 receptor 4 (EP4) partial agonist (pEC50: 7.4).

BAY-1316957 is a highly potent and selective EP4 receptor antagonist. With an IC50 of 15.3 nM. Good oral bioavailability[1].

MF498 is a novel and selective E prostanoid receptor 4 (EP4 receptor) antagonist, displayed a strong binding affinity for the EP4 receptor (Ki: 0.7 nM).