(Rac)-Benpyrine, a racemate of Benpyrine, is a potent and orally active TNF-α inhibitor. (Rac)-Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research.In Vitro: (Rac)-Benpyrine (Compound 001; 5-10 μM; 24 hours) treatment inhibits the expression level of TNF-α downstream pathway protein NF-κB in the nucleus in RAW264.7 macrophages.In Vivo: (Rac)-Benpyrine (Compound 001; 25-50 mg/kg; oral gavage; daily; for 3 weeks; Kunming mice) treatment obviously reduces the inflammatory cytokines IFN-γ, IL-1β and IL-6 in the blood serum, and the anti-inflammatory factor IL-10 is obviously increased, the foot swelling degree of the arthritis part is also obviously slowed down, and the weight index increase caused by the arthritis also has no obvious reduction.