UCB-9260 是口服活性小分子，通过稳定三聚体的不对称形式抑制肿瘤坏死因子信号传导。它对肿瘤坏死因子的选择性高于其他超家族成员，并与肿瘤坏死因子结合，其Kd值为 13?nM。

UCB-9260 inhibits TNF signaling by stabilizing an asymmetric form of the trimer.

In Hek-293 cells, UCB-9260 (0-10 μM)?inhibits NF-κB with a geometric mean IC50?of 202?nM after TNF (10?pM) stimulation. UCB-9260?inhibits TNF-dependent cytotoxicity with a geometric mean IC50?of 116?nM and a geometric mean IC50?of 120?nM, using human and mouse TNF, respectively.

UCB-9260 (150?mg/kg; p.o.) treatment twice daily?for 7 days shows a significant reduction of the clinical score. In adult male Balb/c mice, UCB-9260?(10-300?mg/kg; p.o.) dose-dependently inhibits human and mouse TNF-induced neutrophil recruitment to the peritoneal compartment.

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C26H25N5O

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DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years