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 µM。Benpyrine 可用于 TNF-α 介导的炎症和自身免疫性疾病的研究。

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.

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KD: 82.1 μM (TNF-α)

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 and YA, and increases the cell survival rate up to 80%. Benpyrine does not obviously affect LA- and YL-induced cytotoxicity in L929 cells. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Weiguang Sun, et al. Discovery of an Orally Active Small Molecule TNF-α Inhibitor. J Med Chem. 2020 Jul 15.

In Vitro: DMSO : 12.5 mg/mL (40.54 mM; Need ultrasonic)配制储备液