TNF-α-IN-2 是一种有效和具有口服活性的肿瘤坏死因子 α (TNFα) 抑制剂，在 HTRF 分析中的 IC₅₀ 值为 25 nM。结合时，TNF-α-IN-2 会使 TNFα 三聚体变形，当三聚体与 TNFR1 结合时会导致异常信号传导。TNF-α-IN-2 可用于类风湿关节炎的研究。

TNF-α-IN-2 is a potent and orally active inhibitor of tumor necrosis factor alpha (TNFα), with an IC 50 of 25 nM in the HTRF assay. TNF-α-IN-2 distorts the TNFα trimer upon binding, leading to aberrant signaling when the trimer binds to TNFR1. TNF-α-IN-2 can be used for the research of rheumatoid arthritis.

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CD40 25 nM (IC50)

TNF-α-IN-2 (compound 42) (30 min) inhibits the E-selectin expression induced by soluble TNFα in HUVECs, with an IC50 of 30 nM. has not independently confirmed the accuracy of these methods. They are for reference only.

TNF-α-IN-2 (5-25 mg/kg; p.o. 1 h before TNF stimulation) inhibits TNF-induced IL-6 in mice.
TNF-α-IN-2 (2-10 mg/kg; p.o. twice daily for 10 d) dose dependently reduces both the clinical score as well as the levels of inflammatory cytokines and leukocyte cell surface receptors in mice.
TNF-α-IN-2 (0.5 mg/kg; i.v.) exhibits long t 1/2 (6.2 h), low CL (6.6 mL/min?kg), and V ss (3.2 L/kg) in mice.
TNF-α-IN-2 (2 mg/kg; p.o.) exhibits good oral bioavailability (58%), C max (0.47 μM), and AUC tot (5.9 μM?h) in mice. has not independently confirmed the accuracy of these methods. They are for reference only.

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Powder -20°C 3 years；4°C 2 years

[1]. Xiao HY, et, al. Biologic-like In Vivo Efficacy with Small Molecule Inhibitors of TNFα Identified Using Scaffold Hopping and Structure-Based Drug Design Approaches. J Med Chem. 2020 Dec 1.

In Vitro: DMSO : 100 mg/mL (202.05 mM; Need ultrasonic)配制储备液