产品描述:
Siponimod is an agonist of sphingosine-1-phosphate receptor 1 (S1P1) and S1P5.{41000,41002} It is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4 (EC50s = 0.39, 0.98, >10,000, >1,000, and 750 nM, respectively, in GTP-γS binding assays).{41000} Siponimod (10 nM) reduces demyelination induced by lysophosphatidylcholine or psychosine (Item Nos. 31594 | 20338) in mouse organotypic cerebellar slice cultures.{41001} It decreases plasma levels of urea and creatinine in a rat model of renal ischemia-reperfusion injury when administered at doses of 10 and 30 mg/kg.{59368} Siponimod (0.3 and 3 mg/kg) reduces disease severity in a rat model of experimental autoimmune encephalomyelitis (EAE).{41000} Formulations containing siponimod have been used in the treatment of multiple sclerosis.