Siponimod (BAF312)

Catalog No.S7179

For research use only.

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.

Siponimod (BAF312) Chemical Structure

CAS No. 1230487-00-9

Selleck's Siponimod (BAF312) has been cited by 9 Publications

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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.
Targets
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 Ml[xSpVv[3Srb36gZZN{[Xl? NX;4Npo3OTJyIH3pcpM> NILkUm5C\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJHMyWDFicnXj[ZB1d3JidILhcpNn\WO2ZXSgbY4hS0iRIHPlcIx{KGmwY4XiZZRm\CCob4KgNVAhfG9iMUWgcYlveyCycnnvdkB1dyCJVGDnZY1u[TN3UzDh[IRqfGmxbjDt[YF{fXKnZDDh[pRmeiBzMkCgcYlveyCkeTDHWHBo[W2vYUO1V{BjcW6maX7nJIF{e2G7LDDFR|UxRTBwMECwOO69VQ>? NVniUId2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA3PzBpPkK0PVAxPjdyPD;hQi=>
CHO MnuwSpVv[3Srb36gZZN{[Xl? MWPB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIGOxVFUhemWlZYD0c5Ih\XiycnXzd4VlKGmwIFPIU{Bk\WyuczDifUBcOzWVXVfUVIdidW2jUzDibY5lcW6pIHHzd4F6NCCHQ{WwQVAvODByOUlOwG0> MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF{NUi4OEc,OjRzMkW4PFQ9N2F-
CHO MWPGeY5kfGmxbjDhd5NigQ>? NVfUVpZ2SWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBUOVB2IILlZ4VxfG:{IHX4dJJme3OnZDDpckBEUE9iY3XscJMh[nliW{O1V31IXFCpYX3tZXMh[mmwZHnu[{Bie3OjeTygSWM2OD1yLke1{txO NIDvRVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEGyOVg5PCd-MkSxNlU5QDR:L3G+
CHO MV;GeY5kfGmxbjDhd5NigQ>? MnLYNVIxKG2rboO= NIrsXItC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJHMyWDNicnXj[ZB1d3JidILhcpNn\WO2ZXSgbY4hS0iRIHPlcIx{KGmwY4XiZZRm\CCob4KgNVAhfG9iMUWgcYlveyCycnnvdkB1dyCJVGDnZY1u[TN3UzDh[IRqfGmxbjDt[YF{fXKnZDDh[pRmeiBzMkCgcYlveyCkeTDHWHBo[W2vYUO1V{BjcW6maX7nJIF{e2G7LDDFR|UxRTYQvF2= NV;hVXUyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA3PzBpPkK0PVAxPjdyPD;hQi=>
Assay
Methods Test Index PMID
Western blot p-ERK / ERK / p-AKT / AKT 26856814
Immunofluorescence Vimentin / S1PR1 26856814
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]

Protocol (from reference)

Kinase Assay:[1]
  • 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]
  • 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.
Animal Research:[1]
  • Animal Models: encephalomyelitis (EAE) model rat
  • Dosages: 0.03, 0.3 and 3 mg/kg
  • Administration: oral gavage

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 516.6
Formula

C29H35F3N2O3

CAS No. 1230487-00-9
Storage 3 years -20°C powder
2 years -80°C in solvent
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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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05376579 Recruiting Other: siponimod Active Secondary Progressive Multiple Sclerosis Novartis Pharmaceuticals|Novartis June 17 2022 --
NCT04895202 Recruiting Other: Siponimod Secondary Progressive Multiple Sclerosis With Inflammatory Disease Activity Novartis Pharmaceuticals|Novartis November 19 2021 --
NCT03623243 Active not recruiting Drug: Siponimod Multiple Sclerosis|Relapsing Multiple Sclerosis|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

(data from https://clinicaltrials.gov, updated on 2022-08-01)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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