ep4

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

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。

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 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。

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。

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 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。

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。

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-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.

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

pep4c 可用于生命科学领域的相关研究。其产品编号为 T37701，CAS号为 243843-43-8。

PF-04418948 是一种可口服的，选择性的前列腺素EP2受体拮抗剂，IC50为16 nM。

Prostaglandin E1 (Alprostadil) 是一种前列腺素受体配体，对小鼠 EP1、EP2、EP3、EP4和 IP 的 Ki 值分别为 36、10、1.1、2.1 和 33 nM。它诱导血管舒张并抑制血小板聚集，可作为血管扩张剂用于外周血管疾病的研究。

ONO-AE3-208 (AE 3-208) 是一种 EP4 拮抗剂，可抑制前列腺癌的细胞迁移、侵袭和转移。

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。

TG4-155 是一种脑渗透性 EP2 拮抗剂，对 EP2 和 DP1 具有低纳摩尔的拮抗活性。它作用于 EP2 的 KB 为 2.4 nM，比对 DP1 受体的选择性高 14 倍，比对 EP1、EP3、EP4 和 IP 的选择性比高 550-4750 倍。

E7046 是一种口服有效的特异性 EP4拮抗剂，IC50值为 13.5 nM，Ki 值为 23.14 nM，具有抗肿瘤活性。

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

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,

Butaprost is a chemical compound that functions as a selective agonist for the prostaglandin E receptor (EP2). It exhibits an EC50 of 33 nM and a Ki of 2.4 μM when interacting with the murine EP2 receptor. However, Butaprost demonstrates lower activity against murine EP1, EP3, and EP4 receptors. Furthermore, it effectively attenuates fibrosis by inhibiting the TGF-β Smad2 signaling pathway [1] [2] [3].

MK-2894 sodium salt is a highly potent and selective antagonist of second generation EP4.

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.

16,16-Dimethyl prostaglandin E2 is an orally active vertebrate Hematopoietic stem cells homeostasis critical regulator. It can act through EP2/EP4 and has an interaction with the Wnt pathway.

AAT-008 is a PGE2 receptor EP4 antagonist.

TCS 2510 (CAY10598) 是一种选择性 PGE2 和 EP4 受体激动剂，可增强细胞内 cAMP 浓度和活性 β-caten 的丰度。TCS 2510 抑制TNF-α 产生，可用于研究代谢紊乱带来的疾病。

Grapiprant (AAT-007) 是一种选择性EP4 受体拮抗剂，生理配体为前列腺素 E2(PGE2)，有用于骨关节炎疼痛和炎症的研究潜力。它取代 [3H]-PGE2(1 nM) 与狗的重组EP4 受体结合，IC50为 35 nM，Ki 为 24 nM。

NXT-10796为具口服活性且肠道限制性EP4受体激动剂。

AMX12006为一种口服活性EP4拮抗剂，显示出高度的选择性与有效性，IC50为4.3 nM，并具备细胞毒性和抗肿瘤活性。

ER819762, an antagonist of the prostaglandin E2 EP4 receptor, inhibits Th1 differentiation and Th17 expansion.

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。

BGC201531 (AP-1531) 是一种 EP4 拮抗剂，用于治疗急性偏头痛。

Prostaglandin E2 activates four distinct G protein-coupled receptors, EP1-4. Rivenprost is a potent and selective agonist for the EP4 receptor (Ki = 0.7, 56, 620, and >10,000 nM for EP4, EP3, EP2, and EP1, respectively). It has been used to promote EP4-mediated bone formation, prevent bone loss related to osteoporosis, drive osteoblast differentiation, and stabilize bone implants.[1][2][3][4][5] Rivenprost has also been used to support wound healing.[6]

CP-432 (CP-734432) is an EP4 prostaglandin agonist for the treatment of glaucoma and ocular hypertension.

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。

Treprostinil diethanolamine (UT-15C) 是EP2、DP1和IP 的有效激动剂，对EP2、DP1、IP、EP1、EP4、EP3 和 FPKi 的值分别为 3.6、4.4、32.1、212、826、2505 和 4680 nM。Treprostinil diethanolamine 能够促使 cAMP 的上调，进而维持血管系统内的稳态，并造成人肺动脉的血管扩张。

Travoprost (Fluprostenol isopropyl ester) 是一种异丙基酯前药，是一种高亲和力的，选择性的 FP 前列腺素全受体激动剂。它能够降低眼压，有潜力应用于青光眼和眼高压。

15(R)-Prostaglandin E2, the C-15 epimer of the more physiologically abundant 15(S)-PGE2 (sc-201225) isomer, is produced mainly from arachidonic acid (sc-200770) via the action of COX and PGES enzymes. Present in nearly all cell types, PGE2 interacts with four distinct receptors, EP1 to EP4, leading to a wide range of biological effects. However, 15(R)-Prostaglandin E2 exhibits significantly lower efficacy in most biological assays compared to its 15(S) counterpart. Notably, acid catalyzed epimerization can transform 15(R)-Prostaglandin E2 into the more active 15(S)-Prostaglandin E2 form.

ONO-AE3-208 is an EP4 receptor antagonist with a Ki of 1.3 nM, exhibiting less potent activity against EP3, FP, and TP receptors (Ki values of 30, 790, and 2,400 nM, respectively), while showing no effect on other prostanoid receptors. In wild type mice, treatment with ONO-AE3-208, in conjunction with 3% dextran sodium sulfate, results in severe colitis characterized by epithelial loss, crypt damage, and inflammation, thereby mimicking the effects of EP4 deletion. Further, this compound has been utilized to investigate the role of EP4 signaling in various biological contexts, including immune and autoimmune responses, inflammation, and cancer.

(R)-Vorbipiprant ((R)-CR6086) 作为口服前列腺素 E2 (EP4) 受体拮抗剂，绑定 EP4 受体的能力强，Ki 值为 16.6 nM。该化合物能有效抑制 PGE2 诱导的 cAMP 生成，IC50 值达 22 nM，显示出显著的免疫调节和抗血管生成特性，对小鼠胶原诱导性关节炎的改善效果显著。

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

CR6086 is a novel, potent EP4 antagonist showing favourable immunomodulatory properties, striking DMARD effects in rodents, and anti-inflammatory activity targeted to immune-mediated inflammatory diseases and distinct from the general effects of cyclooxygenase inhibitors. CR6086 showed selectivity and high affinity for the human EP4 receptor (Ki = 16.6 nM) and functioned as a pure antagonist (half-maximal inhibitory concentration, 22 nM) on PGE2-stimulated cAMP production.

15-keto-Prostaglandin E2为内源性代谢产物，通过与STAT3Cys259残基结合，抑制STAT3激活作用。该化合物能够结合并稳定EP2与EP4受体，进而抑制乳腺癌细胞生长与进展，并通过激活PPAR-γ促进真菌生长。

Alprostadil sodium 是一种前列腺素受体配体，对小鼠 EP1、EP2、EP3、EP4和 IP 的 Ki 值分别为 36、10、1.1、2.1 和 33 nM。它诱导血管舒张并抑制血小板聚集，可作为血管扩张剂用于外周血管疾病的研究。

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).