Siponimod hemifumarate
Based on 10 publication(s) in Google Scholar
Siponimod (BAF-312) hemifumarate is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC50 values of 0.39 nM and 0.98 nM, respectively. Siponimod hemifumarate induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod hemifumarate can be used in research related to multiple sclerosis.
For research use only. We do not sell to patients.
- Purity: 99.64%
- CAS No.: 1234627-85-0
- Formula: C29H35F3N2O3.1/2C4H4O4
- Molecular Weight:574.63
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Storage:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Siponimod hemifumarate
More- Nat Commun. 2024 Sep 6;15(1):7791. [Abstract]
- Theranostics. 2023 Feb 5;13(4):1217-1234. [Abstract]
- Proc Natl Acad Sci U S A. 2019 May 21;116(21):10557-10562. [Abstract]
- Aging Dis. 2023 Jun 1;14(3):966-991. [Abstract]
- Exp Neurol. 2024 Jan:371:114572. [Abstract]
- Sci Rep. 2024 Aug 1;14(1):17823. [Abstract]
- Cell Signal. 2025 Sep:133:111876. [Abstract]
- Vet Microbiol. 2021 Oct:261:109177. [Abstract]
- Neurosci Res. 2025 Apr:213:138-145. [Abstract]
- Neurosci Res. 2022 Nov:184:38-46. [Abstract]
Customer Validation & Images
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Flow Cytometry
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WB
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In Vivo Efficacy Study
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Histological Imaging/Staining
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Others
Biological Activity
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S1PR1 0.39 nM (EC50) |
S1PR5 0.98 nM (EC50) |
S1PR4 750 nM (EC50) |
S1PR3 >1000 nM (EC50) |
S1PR2 >10000 nM (EC50) |
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Cell Line
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Type | Value | Description | References |
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| CHO | EC50 |
0.0004 μM
Compound: 32, BAF312, Siponimod
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Agonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
Agonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
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[PMID: 24900670] |
| CHO | EC50 |
0.98 nM
Compound: 3, BAF312
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Agonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
Agonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
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[PMID: 24125884] |
| CHO | EC50 |
5 μM
Compound: 32, BAF312, Siponimod
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Agonist activity at human S1P3 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
Agonist activity at human S1P3 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
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[PMID: 24900670] |
| CHO | EC50 |
750 nM
Compound: 3, BAF312
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Agonist activity at human S1P4 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
Agonist activity at human S1P4 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
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[PMID: 24125884] |
Siponimod (10-1000 nM; 4-13 h) hemifumarate induces significant and persistent internalization of human S1P1 receptors in CHO cells. Obvious internalization is detectable even at concentrations as low as 10 nM, and the receptors remain localized intracellularly after drug washout[1].
Siponimod hemifumarate regulates microglial function by reducing IL6 secretion in cultured microglia[4].
Siponimod hemifumarate improves oligodendrocyte degeneration by alleviating demyelination in organotypic brain slice cultures[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Siponimod (0.14-1 mg/kg; p.o.; single dose) hemifumarate causes a rapid, dose-dependent reduction in peripheral lymphocyte counts in Lewis rats, with an ED50 of 0.14 mg/kg at 6 hours post-dose, and counts return to normal within 48 hours[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Dark Agouti (DA) (female, 9 weeks old at immunization, 200-250 g, chronic experimental autoimmune encephalomyelitis induced via subcutaneous tail base injection of antigen/adjuvant mix)[1]
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Dosage:0.03 mg/kg; 0.3 mg/kg; 3 mg/kg
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Administration:p.o.; daily; day 11 to day 34 post-immunization
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Result:Reduced area under the curve (AUC) of clinical disease scores from days 12 to 34 compared with vehicle-treated controls.
Showed borderline effect on disease scores at 0.03 mg/kg dose.
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Animal Model:Lewis rats[2]
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Dosage:1 mg/kg; 0.14 mg/kg
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Administration:p.o.; single dose
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Result:Decreased peripheral lymphocyte counts by 88% at 8 hours post-administration.
Returned peripheral lymphocyte counts to normal levels by 48 hours post-administration.
Achieved an ED50 of 0.14 mg/kg for 50% reduction of peripheral lymphocyte counts at 6 hours post-dose.
Chemical Information
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CAS No. 1234627-85-0
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Appearance Solid
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Molecular Weight 574.63
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Formula C29H35F3N2O3.1/2C4H4O4
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Color White to off-white
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SMILES
O=C(C1CN(CC2=CC=C(/C(C)=N/OCC3=CC=C(C4CCCCC4)C(C(F)(F)F)=C3)C=C2CC)C1)O.OC(/C=C/C(O)=O)=O.[1/2]
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Synonyms
BAF-312 hemifumarate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (10)
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Journal Impact Factor
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Most Recent
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Nat Commun
Astrocyte-derived clusterin disrupts glial physiology to obstruct remyelination in mouse models of demyelinating diseases. [Abstract]2024 Sep 6;15(1):7791. PMID: 39242637 -
Theranostics
First in vivo fluorine-19 magnetic resonance imaging of the multiple sclerosis drug siponimod. [Abstract]2023 Feb 5;13(4):1217-1234. PMID: 36923535 -
Proc Natl Acad Sci U S A
Sphingosine-1-phosphate receptor 1 activation in astrocytes contributes to neuropathic pain. [Abstract]2019 May 21;116(21):10557-10562. PMID: 31068460 -
Aging Dis
Lymphocyte-Related Immunomodulatory Therapy with Siponimod (BAF-312) Improves Outcomes in Mice with Acute Intracerebral Hemorrhage. [Abstract]2023 Jun 1;14(3):966-991. PMID: 37191423 -
Exp Neurol
Assessing neuroprotective effects of diroximel fumarate and siponimod via modulation of pacemaker channels in an experimental model of remyelination. [Abstract]2024 Jan:371:114572. PMID: 37852467 -
Sci Rep
2024 Aug 1;14(1):17823. PMID: 39090252
Siponimod hemifumarate purchased from MedChemExpress. Usage Cited in: Sci Rep. 2024 Aug 1;14(1):17823. [Abstract]
weight loss was averted in Siponimod (0.45 µg/d) treated mice independent of BDNFko.
Siponimod hemifumarate purchased from MedChemExpress. Usage Cited in: Sci Rep. 2024 Aug 1;14(1):17823. [Abstract]
Siponimod (0.45 µg/d) treatment reduces lymphocyte infiltration of white matter in lumbar spinal cord. Represenative hematoxylin and eosin (HE) images of spinal cord sections.
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Cell Signal
Characterization of functionally relevant G protein-coupled receptors in endometriotic epithelial cells. [Abstract]2025 Sep:133:111876. PMID: 40381972 -
Vet Microbiol
Lipid metabolism is a novel and practical source of potential targets for antiviral discovery against porcine parvovirus. [Abstract]2021 Oct:261:109177. PMID: 34391196
Siponimod hemifumarate purchased from MedChemExpress. Usage Cited in: Vet Microbiol. 2021 Oct:261:109177. [Abstract]
The S1P-S1P3 axis is involved in the infection of PPV. PK15 cells were infected with PPV (MOI = 1) and simultaneously incubated with 10 μM Fingolimod hydrochloride (FTY720), 10 μM Siponimod (BAF-312), 10 μM TY-52,156 or not for 24 h. The values of Log copy number and Log TCID50 for 24 h p.i. were done.
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Neurosci Res
2025 Apr:213:138-145. PMID: 39921000
Siponimod hemifumarate purchased from MedChemExpress. Usage Cited in: Neurosci Res. 2025 Apr:213:138-145. [Abstract]
Internalization of S1P1 on microglia treated with siponimod. Representative flow cytometry data showing the internalization of S1P1 on microglia with no treatment (blue) or 1000 nM Siponimod (red).
Siponimod hemifumarate purchased from MedChemExpress. Usage Cited in: Neurosci Res. 2025 Apr:213:138-145. [Abstract]
Western blot and quantification were performed on microglial cell culture lysates and supernatants with or without prior Siponimod (1000 nM) treatment, followed by stimulation with LPS and nigrain.
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Neurosci Res
2022 Nov:184:38-46. PMID: 35940437
Solvent & Solubility
DMSO : 12.5 mg/mL (21.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (278 KB)
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SDS (562 KB)
- English - EN (562 KB)
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- Norwegian - NO (562 KB)
- Español - ES (562 KB)
- Swedish - SV (562 KB)
- Italian - IT (562 KB)
- Portuguese - PT (562 KB)
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Handling Instructions (2659 KB)
References
[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;167(5):1035-1047. [Content Brief]
[2]. Pan S, et al. Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator. ACS Med Chem Lett. 2013;4(3):333-337. Published 2013 Jan 4. [Content Brief]
[3].
McGinley M, Fox RJ. Prospects of siponimod in secondary progressive multiple sclerosis. Ther Adv Neurol Disord. 2018 Jul 17;11:1756286418788013.
[Content Brief]
[4]. Behrangi N, et al. Mechanism of Siponimod: Anti-Inflammatory and Neuroprotective Mode of Action. Cells. 2019;8(1):24. Published 2019 Jan 7. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.7403 mL | 8.7013 mL | 17.4025 mL | 43.5063 mL |
| 5 mM | 0.3481 mL | 1.7403 mL | 3.4805 mL | 8.7013 mL | |
| 10 mM | 0.1740 mL | 0.8701 mL | 1.7403 mL | 4.3506 mL | |
| 15 mM | 0.1160 mL | 0.5801 mL | 1.1602 mL | 2.9004 mL | |
| 20 mM | 0.0870 mL | 0.4351 mL | 0.8701 mL | 2.1753 mL |
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