Siponimod | Sphingosine-1-phosphate receptor agonist

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Siponimod (1230487-00-9) is potent sphingosine-1-phosphate receptor agonist with selectivity for S1P1 (EC50 = 0.4 nM) and S1P5 (EC50 = 1 nM).1,2 FDA approved for the treatment of relapsing forms of multiple sclerosis. Siponimod binds to S1P receptors on B and T cells preventing their release from lymph nodes. It may have positive effects on remyelination of neurons.3

References/Citations:

  1. Pan et al. (2013), Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator; ACS Chem. Lett. 4 333
  2. Gergely et al. (2012), The selective sphingosine-1-phosphate receptor modulator BAF312 redirects lymphocyte distribution and has species-specific effects on heart rate; Br. J. Pharmacol. 167 1035
  3. Wu et al. (2026), Effects of Sphingosine-1 phosphate Modulators on Central Remyelination: A Systemic Review of Animal Models; Cell Mol. Neurobiol. Online ahead of print
1230487-00-9, BAF312, NVP-BAF-312-NX, S-1-P agonist, S-1-P receptor agonist, S1P agonist, siponimod, Siponimod supplier
Alternate Name:
BAF312; NVP-BAF312-NX

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Siponimod (1230487-00-9) is potent sphingosine-1-phosphate receptor agonist with selectivity for S1P1 (EC50 = 0.4 nM) and S1P5 (EC50 = 1 nM).1,2 FDA approved for the treatment of relapsing forms of multiple sclerosis. Siponimod binds to S1P receptors on B and T cells preventing their release from lymph nodes. It may have positive effects on remyelination of neurons.3

References/Citations:

  1. Pan et al. (2013), Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator; ACS Chem. Lett. 4 333
  2. Gergely et al. (2012), The selective sphingosine-1-phosphate receptor modulator BAF312 redirects lymphocyte distribution and has species-specific effects on heart rate; Br. J. Pharmacol. 167 1035
  3. Wu et al. (2026), Effects of Sphingosine-1 phosphate Modulators on Central Remyelination: A Systemic Review of Animal Models; Cell Mol. Neurobiol. Online ahead of print