Benpyrine

2550398-89-3

308.34

10 mM in DMSO

Apoptosis

Benpyrine is a highly specific and orally active TNF-alpha inhibitor with a KD value of 82.1 uM. Benpyrine tightly binds to TNF-alpha and blocks its interaction with TNFR1, with an IC50 value of 0.109 uM. Benpyrine has the potential for TNF-alpha mediated inflammatory and autoimmune disease research.
IC50 & Target: KD: 82.1 uM (TNF-alpha)
In Vitro: Benpyrine (5-20 uM; 14 hours; RAW264.7 cells) pretreatment results in a dose-dependent decrease in the phosphorylation of IkappaBalpha in RAW264.7 cells (stimulated with 10 ng/mL TNF-alpha or 1 ug/mL LPS). Benpyrine abolishes the TNF-alpha-induced nuclear translocation of NF-kappaB/p65 in RAW264.7 cells.

Benpyrine only blocks cell death induced by TNF-alphaWT and Y119A, and increases the cell survival rate up to 80%. Benpyrine does not obviously affect L57A- and Y59L-induced cytotoxicity in L929 cells.
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-gamma, IL-1beta 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-alpha-induced inflammation, thereby reducing liver and lung injury.