1234627-85-0

Siponimod (BAF-312) hemifumarate is a potent and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod hemifumarate is selective for S1P1 and S1P5 receptors over S1P2, S1P3, and S1P4 (EC50s of 0.39, 0.98, >10000, >1000, and 750 nM, respectively). Siponimod hemifumarate can be used for multiple sclerosis (MS) research[1][2].

S1PR1: 0.39 nM (EC₅₀); S1PR5: 0.98 nM (EC₅₀); S1PR4: 750 nM (EC₅₀); S1PR3: >1000 nM (EC₅₀); S1PR2: >10000 nM (EC₅₀)

[1] Pan S, et al. Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator. ACS Med Chem Lett. 2013 Jan 4;4(3):333-7. DOI:10.1021/ml300396r
[2] McGinley M, et al. Prospects of siponimod in secondary progressive multiple sclerosis. Ther Adv Neurol Disord. 2018 Jul 17;11:1756286418788013. DOI:10.1177/1756286418788013
[3] Behrangi N, et al. Mechanism of Siponimod: Anti-Inflammatory and Neuroprotective Mode of Action. Cells. 2019 Jan 7;8(1):24. DOI:10.3390/cells8010024