tnfα antagonist

TNF-α antagonist is an exocyclic peptide that mimics the critical TNF-α recognition loop on TNF receptor I complex and, thus, prevents ligand interaction with the receptor. By blocking the TNF receptor ligand contact site, this peptide interferes with both activating receptor activator of NF-κB (RANK) and TNF-α's recruitment and activation of osteoclasts. TNF-α antagonist has been used to block bone resorption in the study of systemic bone loss in rheumatoid arthritis and inflammatory bone destruction.

R-7050 (TNF-α Antagonist III) 是一种肿瘤坏死因子受体拮抗剂，对 TNFα具有更高选择性。

Larsucosterol trimethylamine (DUR-928 trimethylamine) 是一种有效的肝 X 受体 (LXR) 拮抗剂，可调节内源性表观遗传，减少肝细胞内的脂质积累，减弱巨噬细胞中脂多糖 （LPS） 和 TNFα 诱导的炎症反应，缓解 LPS 和对乙酰氨基酚 （ATMP） 诱导的多器官损伤。

Dersalazine, a PAF antagonist and TNFα inhibitor, is used potentially for the treatment of ulcerative colitis. It showed anti-inflammatory effect in reactivated colitis in rats, as evidenced by a significant reduction in MPO activity.

ASTX660是一种新型非肽模拟拮抗剂，针对cIAP1 2和XIAP，能有效诱导癌细胞系中TNFα-依赖的凋亡，并抑制肿瘤生长。

IW-927 is a potent and selective TNFα/TNFRc1 interaction antagonist.