TNF-α-IN-2

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 In Vitro TNF-α-IN-2 (compound 42) (30 min) inhibits the E-selectin expression induced by soluble TNFα in HUVECs, with an IC 50 of 30 nM. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female C57Bl/6 mice Dosage: 5, 25 mg/kg Administration: P.o. 1 h prior to TNF stimulation Result: Inhibited IL-6 moderately at 5 mg/kg while the inhibition at 25 mg/kg was similar to mouse Enbrel, which served as the positive control in the study. Form:Solid IC50& Target:CD40 25 nM (IC 50 )

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