human ep3 receptor

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,

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。

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.

AH 6809 是 EP 和 DP 受体的拮抗剂，对小鼠 EP2受体的 Ki 值为 350 nM，对克隆的人类 EP1，EP2，EP3-III 和 DP 受体的 Ki 值分别为 1217、1150、1597 和 1415 nM。

Tafluprost acid is a selective agonist at the prostaglandin F receptor.

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。

L-644,698 is a selective agonist of human prostanoid DP receptor.

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。

Prostaglandin J2 (PGJ2) 是前列腺素 D2 (PGD2) 的一种内源性代谢物，是一种有效的 PGD2 受体 (DP) 激动剂，对 hDP 和 hCRTH2 的 Ki 分别为 0.9 nM 和 6.6 nM。Prostaglandin J2 刺激细胞内环 AMP 的产生，EC50值为 1.2 nM。Prostaglandin J2 诱导氧化应激和神经细胞凋亡。Prostaglandin J2 诱导泛素化 (Ub) 蛋白的积累 聚集。Prostaglandin J2 具有高度神经毒性，可导致许多神经退行性疾病，包括阿尔茨海默病 (AD) 和帕金森病 (PD)。