Benpyrine is a highly specific and orally active TNF-α inhibitor with a K D value of 82.1 μM. Benpyrine tightly binds to TNF-α and blocks its interaction with TNFR1, with an IC 50 value of 0.109 µM. Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research
In Vitro
Benpyrine (5-20 µM; 14 hours; RAW264.7 cells) pretreatment results in a dose-dependent decrease in the phosphorylation of IκBα in RAW264.7 cells (stimulated with 10 ng/mL TNF-α or 1 μg/mL LPS). Benpyrine abolishes the TNF-α-induced nuclear translocation of NF-κB/p65 in RAW264.7 cells. Benpyrine only blocks cell death induced by TNF-α WT and Y 119 A, and increases the cell survival rate up to 80%. Benpyrine does not obviously affect L 57 A- and Y 59 L-induced cytotoxicity in L929 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: RAW264.7 cells Concentration: 5 µM, 10 µM, 20 µM Incubation Time: 14 hours Result: Resulted in a dose-dependent decrease in the phosphorylation of IκBα.
In Vivo
Benpyrine (25-50 mg/kg; oral gavage; daily; for 2 weeks; Balb/c mice) treatment significantly relieves the symptoms of collagen-induced arthritis. Benpyrine dose-dependently decreases the levels of proinflammatory cytokines, such as IFN-γ, IL-1β and IL-6, and increases the concentration of the anti-inflammatory cytokine IL-10 . Endotoxemia murine model shows that Benpyrine (25 mg/kg) could attenuate TNF-α-induced inflammation, thereby reducing liver and lung injury . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Balb/c mice (18-20 g) injected with collagen Dosage: 25 mg/kg, 50 mg/kg Administration: Oral gavage; daily; for 2 weeks Result: Relieved the symptoms of collagen-induced arthritis in mice.
