产品描述:
Ponesimod is a potent agonist of sphingosine-1-phosphate receptor 1 (S1P1/EDG-1; IC50s = 6, >10,000, 2,068, 1,956, and 142 nM for S1P1-S1P5, respectively, in a radioligand binding assay).{38368} It selectively activates S1P1 in a GTPγS assay (EC50s = 5.7, >10,000, 105, 1,108, and 59.1 nM, for S1P1-S1P5, respectively). Ponesimod (3-100 mg/kg) reduces the number of circulating lymphocytes in rats in a dose-dependent manner. It reduces edema, protein extravasation, neutrophil activity, and skin levels of the proinflammatory cytokines IL-1β, IL-6, IFN-γ, and TNF-α in a mouse model of delayed-type hypersensitivity at a dose of 30 mg/kg.{38369} Ponesimod (30 mg/kg) also prevents footpad swelling in a rat model of adjuvant-induced arthritis.