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Benpyrine

CAS No. : 2550398-89-3

MCE 站：Benpyrine

产品活性：Benpyrine 是一种高度特异性的具有口服活性的 TNF-α 抑制剂，K_D 值为 82.1 μM。Benpyrine 与 TNF-α 紧密结合并阻断其与 TNFR1 的相互作用，IC₅₀ 值为 0.109 ?M。Benpyrine 可用于 TNF-α 介导的炎症和自身免疫性疾病的研究。

研究领域：Apoptosis

作用靶点：TNF Receptor

In Vitro: Benpyrine (5-20 ?M; 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 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-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.

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