target/cox/5

Target 5 在生命科学相关研究中具有广泛的应用。

COX-2 15-LOX-IN-5（Compound 4f）作为一种COX-2 15-LOX双重抑制剂，在脂多糖介导的RAW 264.7巨噬细胞中有效降低NF-κB活化。此外，COX-2 15-LOX-IN-5还表现出显著的抗炎和抗氧化活性。

COX-2 5-LOX-IN-1 (compound 3a), a benzothiophen-2-yl pyrazole carboxylic acid derivative, is a potent and dual inhibitor of COX-2 5-LOX. It exhibits superior analgesic and anti-inflammatory properties compared to Celecoxib and Indomethacin. COX-2 5-LOX-IN-1 displays strong inhibitory activity against COX-1, COX-2, and 5-LOX, with IC50 values of 12.13 μM, 0.4 μM, and 4.96 μM, respectively [1].

COX-2 5-LOX-IN-3 (compound 5b) is a powerful and dual inhibitor of COX-2 and 5-LOX, with IC50 values of 45.73 μM, 5.45 μM, and 4.33 μM for COX-1, COX-2, and 5-LOX, respectively. This compound, COX-2 5-LOX-IN-3, shows promise for the investigation of inflammatory diseases [1].

COX-1 2-IN-5 (compound 2a) 为 COX1 2 双抑制剂，IC50 分别为 2.650 μM 和 0.958 μM，展现抗癌功效。针对肝癌细胞株 HepG2，其抑制作用的 IC50 值为 60.75 μM。

COX 5-LOX-IN-1 (compound 6b) 是有效的COX 5-LOX 双重抑制剂，具有用于炎症性疾病研究的潜力。COX 5-LOX-IN-1 对于 COX-1、COX-2 和 5-LOX 酶的IC50值分别为 1.07、0.55 和 0.28 μM。

COX-2 5-LOX-IN-2 是苯并噻吩-2-基吡唑羧酸衍生物。COX-2 5-LOX-IN-2 (5b) 对COX-2和5-LOX 均有抑制作用。COX-2 5-LOX-IN-2 抑制 COX-1、COX-2 和 5-LOX 的IC50s 分别为 5.40、0.01 和 1.78 μM。COX-2 5-LOX-IN-2 显示出超过塞来昔布和吲哚美辛的镇痛和抗炎活性。

COX/5-LO-IN-1 is a cyclooxygenase and 5-lipoxygenase (5-LO) inhibitor, and used for inflammatory and allergic disease states.

15(R)-HETE, a monohydroxy fatty acid, is synthesized from arachidonic acid via aspirin-acetylated COX-2, leading to the formation of specialized pro-resolving mediators 15(R)-lipoxin A4 and B4 through a transcellular mechanism involving 5-lipoxygenase (5-LO). Additionally, this compound is produced by the cytochrome P450 (CYP) isoform CYP2C9 and can be generated from arachidonic acid by COX-1 in human mast cells, where it accumulates due to its resistance to conversion into 15-KETE by 15-hydroxyprostaglandin dehydrogenase (15-PGDH). As an agonist of PPARβ δ, 15(R)-HETE induces the expression of a target gene in NIH3T3 cells, demonstrating its biological significance.