crth2 (dp2) receptor

CAY10595 是 CRTh2 (DP2) 受体的拮抗剂，Ki 为 10 nM。

AZD1981 是一种有效且特异性的 CRTh2 (DP2) 受体拮抗剂，IC50为 4 nM，用于研究哮喘、绝经后、药代动力学、哮喘患者和药物相互作用等治疗和基础科学的试验。

BI-671800 (AP-761) 是高特异性的前列腺素 D2 受体拮抗剂，对哮喘有研究潜力，对人和小鼠 CRTH2 转染细胞中 PGD2 结合 CRTH2 的 IC50值分别为 4.5 和 3.7 nM。

CAY10471 Racemate (TM30089 Racemate) 是一种高选择性的 CRTH2 DP 2 受体拮抗剂，对 hCRTH2 的Ki 值为 0.6 nM，对其选择性远高于人血栓素 A2 受体 TP 或 PGD2 受体 DP。它对大小鼠的同源 CRTH2 也具有拮抗作用。

AMG-009 是一种具有选择性和高效性的 CRTH2 和 DP 双重拮抗剂，对 CRTH2 的 IC50 值为 3 nM ，对 DP 受体的 IC50 值为 12 nM。

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

MK-8318 is an effective and selective antagonist of the CRTh2 receptor (Ki: 5.0 nM).

CRTH2-IN-1 is a selective prostaglandin D2 receptor DP2 (CRTH2) antagonist, a Ramatroban analog, with an IC50 of 6 nM in the human DP2 binding assay.

15(R)-15-methyl Prostaglandin D2 (15(R)15methyl PGD2) 是一种 PGD2 合成类似物，也是一种具有选择性和强效性的 CRTH2 DP2 受体激动剂，可调节嗜酸性粒细胞 CD11b 表达、肌动蛋白聚合和趋化。

The biological effects of prostaglandin D2 (PGD2) are transduced by at least two 7-transmembrane G protein-coupled receptors, designated DP1 and CRTH2/DP2. In humans, CRTH2/DP2 is expressed on Th2 cells, eosinophils, and basophils where it mediates the chemotactic activity of PGD2. CAY10597, as a racemic mixture, is a potent CRTH2/DP2 receptor antagonist that binds to the human receptor with a Ki value of 37 nM. The R enantiomer is slightly more potent exhibiting Ki values of 23 and 22 nM at the human and murine CRTH2/DP2 receptor, respectively. The R enantiomer of CAY10597 inhibits eosinophil chemotaxis induced by 13,14-dihydro-15-keto-prostaglandin D2 with an IC50 value of 40 nM.

11-Keto Fluprostenol, a potent analog of prostaglandin F2α (PGF2α), primarily interacts with the FP receptor. It is a structurally modified derivative of prostaglandin D2 (PGD2) designed to enhance its potency and extend its half-life. The compound is produced by oxidizing fluprostenol at the C-11 position, which results in 11-keto fluprostenol. This modification allows 11-keto Fluprostenol to exhibit moderate affinity for the CRTH2 DP2 receptor, though it shows negligible activity at the DP1 receptor, distinguishing its action from that of PGD2.