KKL 顾客使用本产品发表的 0 篇科研文献

TNF-α-IN-2 is a potent and orally active inhibitor of tumor necrosis factor alpha (TNFα), with an IC₅₀ 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.

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.

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.

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