Siponimod (BAF312)

For research use only.

Catalog No.S7179

7 publications

Siponimod (BAF312) Chemical Structure

CAS No. 1230487-00-9

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.

Selleck's Siponimod (BAF312) has been cited by 7 publications

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  • Immunoblot of KMH2 cells following 1 h pre-treatment with increasing concentrations of Ozanimod or Siponimod.

    Leukemia, 2018, 32(1):214-223. Siponimod (BAF312) purchased from Selleck.

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Biological Activity

Description 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.
S1P1 receptor [1] S1P5 receptor [1]
0.39 nM(EC50) 0.98 nM(EC50)
In vitro

BAF312 (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. [1]BAF312 (1 h at 1 μM) promotes prominent internalization of S1P1 receptors by 91%.[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
CHO NHTCXoJHfW6ldHnvckBie3OjeR?= MX2xNlAhdWmwcx?= Ml;pRYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDTNXAyKHKnY3XweI9zKHS{YX7z[oVkfGWmIHnuJGNJVyClZXzsd{BqdmO3YnH0[YQh\m:{IEGwJJRwKDF3IH3pcpMheHKrb4KgeI8hT1SSZ3HtcYE{PVNiYXTkbZRqd25ibXXhd5Vz\WRiYX\0[ZIhOTJyIH3pcpMh[nliR2TQ[4FudWF|NWOgZolv\GmwZzDhd5NigSxiRVO1NF0xNjByMEVOwG0> NFzhVlA9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEmwNFY4OCd-MkS5NFA3PzB:L3G+
CHO M4XNWWZ2dmO2aX;uJIF{e2G7 MnTQRYdwdmm|dDDhZ5Rqfmm2eTDheEBpfW2jbjDTNXA2KHKnY3XweI9zKGW6cILld5Nm\CCrbjDDTG8h[2WubIOgZpkhYzN3U23HWHBo[W2vYWOgZolv\GmwZzDhd5NigSxiRVO1NF0xNjByMEm4{txO NX;5[3hXRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkSxNlU5QDRpPkK0NVI2QDh2PD;hQi=>
CHO NG\sW2lHfW6ldHnvckBie3OjeR?= NEXlcldC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJHMyWDRicnXj[ZB1d3JiZYjwdoV{e2WmIHnuJGNJVyClZXzsd{BjgSCdM{XTYWdVWGejbX3hV{BjcW6maX7nJIF{e2G7LDDFR|UxRTBwN{ZOwG0> MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF{NUi4OEc,OjRzMkW4PFQ9N2F-
CHO MXrGeY5kfGmxbjDhd5NigQ>? MoL5NVIxKG2rboO= NVfyeHh6SWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBUOVB|IILlZ4VxfG:{IITyZY5{\mWldHXkJIlvKEOKTzDj[YxteyCrbnP1ZoF1\WRiZn;yJFExKHSxIEG1JI1qdnNicILpc5IhfG9iR2TQ[4FudWF|NWOgZYRlcXSrb36gcYVie3W{ZXSgZYZ1\XJiMUKwJI1qdnNiYomgS3RR\2GvbXGzOXMh[mmwZHnu[{Bie3OjeTygSWM2OD13zszN M33ZblxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ2OUCwOlcxLz5{NEmwNFY4ODxxYU6=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
p-ERK / ERK / p-AKT / AKT ; 

PubMed: 26856814     

Agonism of S1PR1/5 promotes pERK and pAkt signalling in mouse and human astrocytes. BAF312 at concentrations shown induced pERK after 10 min (n = 3) and pAKT after 30 min treatments (n = 4) a in mouse astrocytes and b in human astrocytes. Data presented as ±SEM (n = 3-4), one-way ANOVA and Newman-Keuls multiple comparison post-test. *p < 0.05, **p < 0.01, ***p < 0.001.

Vimentin / S1PR1 ; 

PubMed: 26856814     

BAF312 induces internalisation of the S1PR1. Mouse astrocytes were serum starved for 4 h and then treated for 1 h with BAF312 (10 nM, 100 nM, 1 μM) or pFTY (1 μM). BAF312 at 1 μM concentration induced internalisation of S1PR1.

In vivo BAF312 effectively suppresses encephalomyelitis (EAE) in rats by internalizing S1P1 receptors, rendering them insensitive to the egress signal from lymph nodes. [1] BAF312 significantly reduces clinical scores when dosed prophylactically or therapeutically in mice at 0.3 mg/kg. [3]


Kinase Assay:[1]
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GTPγ[35S] binding assay:

The cells are homogenized and centrifuged at 26900 × g for 30 min at 4°C. Membranes are re-suspended in 20 mM HEPES (pH 7.4), 100 mM NaCl, 10 mM MgCl2, 1 mM EDTA and 0.1% fat-free BSA at 2–3 mg protein/mL. GTPγ[35S] binding assay is performed with the membranes (75 mg protein /mL in 50 mM HEPES, 100 mM NaCl, 10 mM MgCl2, 20 μg/mL saponin and 0.1% fat-free BSA (pH 7.4), 5 mg/mL with wheat-germ agglutinin-coated scintillation proximity assay-bead, and 10 μM GDP for 10–15 min. The GTPγ[35S]-binding reaction is started by the addition of 200 pM GTPγ[35S]. After 120 min at room temperature, the plates are centrifuged for 10 min at 300 × g and counted.
Cell Research: [1]
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  • Cell lines: CHO
  • Concentrations: ~1 μM
  • Incubation Time: 1 h
  • Method: Agonist-mediated internalization of S1P1 receptors in CHO cells analysed by flow cytometry Myc-tag hS1P1 cells are incubated for 1 h with agonist at 37°C in standard culture medium followed by a PBS wash. An aliquot is kept on ice for 3 h, while another aliquot is left for 3 (or 12) h in culture medium (no agonist) at 37°C. The cells are then incubated either with 4 μg/mL monoclonal mouse anti C-myc IgG1 antibody or with isotype control mouse IgG1 for 60 min at 4°C, followed by an incubation with 1 μg/mL of Alexa488-labelled goat anti-mouse secondary conjugates. The cells are subjected to flow cytometry measurements using 10000 viable cells per sample.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: encephalomyelitis (EAE) model rat
  • Dosages: 0.03, 0.3 and 3 mg/kg
  • Administration: oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 100 mg/mL warmed (193.57 mM)
Ethanol 44 mg/mL warmed (85.17 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 516.6


CAS No. 1230487-00-9
Storage powder
in solvent
Synonyms N/A
Smiles CCC1=C(C=CC(=C1)C(=NOCC2=CC(=C(C=C2)C3CCCCC3)C(F)(F)F)C)CN4CC(C4)C(=O)O

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04895202 Not yet recruiting Other: Siponimod Secondary Progressive Multiple Sclerosis With Inflammatory Disease Activity Novartis Pharmaceuticals|Novartis August 25 2021 --
NCT03623243 Recruiting Drug: Siponimod Multiple Sclerosis Relapsing MS Advancing Multiple Sclerosis Novartis Pharmaceuticals|Novartis February 14 2019 Phase 3
NCT02029274 Terminated Drug: BAF312|Drug: Placebo Active Dermatomyositis Novartis Pharmaceuticals|Novartis August 25 2013 Phase 2
NCT01904214 Completed Drug: BAF312 Renal Impairment Novartis Pharmaceuticals|Novartis July 2013 Phase 1

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S1P Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID