| Bioactivity | Siponimod (BAF-312) is an orally active and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4, with EC50s of 0.4, 0.98, >10000, >1000, and 750 nM, respectively. Siponimod can be used for multiple sclerosis (MS) research[1]-[4]. |
| Invitro | Siponimod (compound 32) exhibits selectivity to S1P1 and S1P5, and spares activity on the S1P2, S1P3 and S1P4 receptors[1].Siponimod (1 mM; 0-1 h) promotes internalization of S1P1 receptors, results 94% S1P1 receptors localized intracellularly at 1 h[2].Siponimod (0.001 nM-1 μM; 1 h) activates the GIRK channel in atrial myocytes, with an EC50 value of 15.8 nM in CHO cell line CCL-61[2]. |
| In Vivo | Siponimod (1 g/kg; i.v.; single dose) shows low to moderate in monkey, but high in rat in metabolism studies with liver microsomes. The absolute bioavailability is 50 and 71% in the rat and monkey, respectively, indicating no major presystemic first pass metabolism[1].Siponimod (0.3, 3 mg/kg; p.o.; once daily; 23 d) suppresses experimental autoimmune encephalomyelitis (EAE) in rats by internalizing S1P1 receptors[2].Parmacokinetics of Siponimod in rats and monkey[1]/td>CL (L/h/kg) |
| Name | Siponimod |
| CAS | 1230487-00-9 |
| Formula | C29H35F3N2O3 |
| Molar Mass | 516.60 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [1]. Gergely P, et al. The selective sphingosine 1-phosphate receptor modulator BAF312 redirects lymphocyte distribution and has species-specific effects on heart rate. Br J Pharmacol. 2012 Nov;167(5):1035-47. [2]. 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. [3]. McGinley M, et al. Prospects of siponimod in secondary progressive multiple sclerosis. Ther Adv Neurol Disord. 2018 Jul 17;11:1756286418788013. [4]. Behrangi N, et al. Mechanism of Siponimod: Anti-Inflammatory and Neuroprotective Mode of Action. Cells. 2019 Jan 7;8(1):24. |
Siponimod
CAS: 1230487-00-9 F: C29H35F3N2O3 W: 516.60
Siponimod (BAF-312) is an orally active and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod is sel
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