TNF-α-IN-29 

TNF-α-IN-29 is an orally active and selective TNF-α inhibitor, with IC₅₀ values of 123.0 nM against human targets, and a human K_d of 45.9 nM. TNF-α-IN-29 blocks TNF-α-TNFR1 protein-protein interactions and inhibits TNF-α-mediated inflammatory signaling pathways. TNF-α-IN-29 exhibits anti-inflammatory effects in a mouse model of collagen-induced arthritis and promotes articular cartilage repair. TNF-α-IN-29 can be used for the research of rheumatoid arthritis^[1].

TNF-α-IN-29 (XS-18) 可与人 TNF-α 蛋白强结合，其 FP-IC₅₀ 为 123.0 nM，K_d 为 45.9 nM；还可抑制 TNF-α 与 TNFR1 之间的蛋白-蛋白相互作用，IC₅₀ 为 36.4 nM。
TNF-α-IN-29 (最长 60 min) 在人肝微粒体中具有更强的体外代谢稳定性，半衰期为 63.6 min^[1]。
TNF-α-IN-29 (1.37-1000 nM; 1.5 h preincubated with TNF-α, 24 h incubated with cells) 可中和 TNF-α 诱导的 L929 细胞凋亡^[1]。
TNF-α-IN-29 (先与 TNF-α 预孵育 20 分钟，再与细胞孵育 18 小时) 可抑制 NF-κB-TA-Luc HEK293 细胞中 TNF-α 诱导的 NF-κB 激活，其 IC₅₀ 为 126.9 nM，且在 20 μM 浓度下仅表现出极低的细胞毒性^[1]。
TNF-α-IN-29 (5-10 μM; 72 h incubated with cells, 15 min stimulated with TNF-α) 可通过降低 IκBα 磷酸化阻断 MH7A 细胞中 TNF-α 介导的 NF-κB 通路激活，并抑制 IL-6 mRNA 的表达^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

TNF-α-IN-29 (XS-18) (小鼠中 500-1000 mg/kg；大鼠中 250-500 mg/kg；口服) 在小鼠 7 天急性毒性试验和大鼠 14 天亚急性毒性试验中，与对照组相比未表现出显著的体重变化^[1]。
TNF-α-IN-29 (5-50 mg/kg；口服；每日 2 次；连续 14 天) 在 CIA 小鼠模型中表现出剂量依赖性的抗类风湿性关节炎活性，其中 50 mg/kg 剂量在减轻关节炎症、修复软骨损伤和抑制促炎细胞因子 (IL-6 和 TNF-α) 表达方面的疗效优于 Tofacitinib (HY-40354)^[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

582.02

C₂₉H₂₇ClF₃N₇O

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Sun Z, et al. Identification of an Orally Bioavailable Quinoline-Based Small-Molecule Tumor Necrosis Factor α (TNF-α) Inhibitor Featuring a Spirocyclic Scaffold. J Med Chem. Published online March 31, 2026.  [Content Brief]