Siponimod (BAF312) (C09-1044-295)

InformationSiponimod (BAF312) BAF312 (Siponimod) is a next-generation S1P receptor agonist, selective for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, exhibits >1000-fold selectivity over S1P2, S1P3 and S1P4 receptors. Phase 3.TargetsS1P1 receptor ; S1P5 receptor 0.39 nM(EC50); 0.98 nM(EC50)In vitroBAF312 (Siponimod) is a potent and selective S1P receptor agonist, with EC50 of 0.39 nM and 0.98 nM for S1P1 and S1P5receptors, exhibits >1000-fold selectivity over S1P2, S1P3 and S1P4 receptors. BAF312 (1 h at 1 μM) promotes prominent internalization of S1P1 receptors by 91%.In vivoBAF312 effectively suppresses encephalomyelitis (EAE) in rats by internalizing S1P1 receptors, rendering them insensitive to the egress signal from lymph nodes. BAF312 significantly reduces clinical scores when dosed prophylactically or therapeutically in mice at 0.3 mg/kg.Cell Research(from reference)Cell lines：CHO Concentrations：~1 μM Incubation Time：1 h. Specification: 0.98 Molecular Formula: C29H35F3N2O3 Molecular Weight: 516.6 PubChem CID: 44599207 Isomeric SMILES: CCC1=C(C=CC(=C1)/C(=N/OCC2=CC(=C(C=C2)C3CCCCC3)C(F)(F)F)/C)CN4CC(C4)C(=O)O Related Documents: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/S413720-SCI_41c3cd0bca1f02997865cc541c2f0470.pdf