Siponimod (BAF312)
Catalog No.S7179
Molecular Weight(MW): 516.6
BAF312 (Siponimod) is a next-generation S1P receptor modulator, 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.
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Biological Activity
| Description | BAF312 (Siponimod) is a next-generation S1P receptor modulator, 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. | |||||||||
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| 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] |
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| 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
| 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. |
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| Cell Research: [1] |
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| Animal Research:[1] |
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Solubility (25°C)
| In vitro | DMSO | 100 mg/mL warmed (193.57 mM) |
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| 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 |
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| Formula | C29H35F3N2O3 |
| CAS No. | 1230487-00-9 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
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Clinical Trial Information
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
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| NCT03338998 | Recruiting | Drug: BAF312|Drug: Placebo | Hemorrhagic Stroke|Intracerebral Hemorrhage (ICH) | Novartis Pharmaceuticals|Novartis | December 24 2017 | Phase 2 |
| 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 |
| NCT01801917 | Terminated | Drug: Placebo|Drug: BAF312 | Polymyositis | Novartis Pharmaceuticals|Novartis | April 24 2013 | Phase 2 |
| NCT01665144 | Active not recruiting | Drug: BAF312|Drug: Placebo | Secondary Progressive Multiple Sclerosis | Novartis Pharmaceuticals|Novartis | December 20 2012 | Phase 3 |
| NCT01565902 | Completed | Drug: BAF312 | Hepatic Impairment | Novartis Pharmaceuticals|Novartis | October 2012 | Phase 1 |
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.
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