Formulation: A crystalline solid
Formal Name: 1-[[4-[(1E)-1-[[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]imino]ethyl]-2-ethylphenyl]methyl]-3-azetidinecarboxylic acid
Purity: ≥98%
Formula Markup: C29H35F3N2O3
Formula Weight: 516,6
Shelf life (days): 1460
CAS Number: 1230487-00-9
Notes: 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.
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