2. GPCR/G Protein Membrane Transporter/Ion Channel
  3. LPL Receptor Potassium Channel
  4. Siponimod hemifumarate

Siponimod hemifumarate  (Synonyms: BAF-312 hemifumarate)

Cat. No.: HY-12355A Purity: 99.64%
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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.

CAS No. : 1234627-85-0

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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Siponimod hemifumarate:

Siponimod hemifumarate Related Antibodies

Top Publications Citing Use of Products

    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.

    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.

    Siponimod hemifumarate purchased from MedChemExpress. Usage Cited in: Vet Microbiol. 2021 Oct:261:109177.

    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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    LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

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    Description

    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[1][2][3][4].

    IC50 & Target[1]

    S1PR1

    0.39 nM (EC50)

    S1PR5

    0.98 nM (EC50)

    S1PR4

    750 nM (EC50)

    S1PR3

    >1000 nM (EC50)

    S1PR2

    >10000 nM (EC50)

    In Vitro

    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 hemifumarate Related Antibodies
    In Vivo

    Siponimod (0.03-3 mg/kg; p.o.; daily; day 11 to day 34 post-immunization) hemifumarate dose-dependently suppresses established chronic experimental autoimmune encephalomyelitis in female DA rats, with significant efficacy observed at doses of 0.3 mg/kg and 3 mg/kg[1].
    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.

    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]
    Dosage: 0.03 mg/kg; 0.3 mg/kg; 3 mg/kg
    Administration: p.o.; daily; day 11 to day 34 post-immunization
    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.
    Animal Model: Lewis rats[2]
    Dosage: 1 mg/kg; 0.14 mg/kg
    Administration: p.o.; single dose
    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.
    Molecular Weight

    574.63

    Formula

    C29H35F3N2O3.1/2C4H4O4
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    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]
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    -20°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.7403 mL 8.7013 mL 17.4025 mL
    5 mM 0.3481 mL 1.7403 mL 3.4805 mL
    View the 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.

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    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

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    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Purity & Documentation
    References

    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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    Siponimod hemifumarate Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Siponimod hemifumarate1234627-85-0BAF-312 hemifumarateLPL ReceptorPotassium ChannelLysophospholipid ReceptorKcsAS1P1S1P5relapsing?remitting multiple sclerosisCHO cellslymphocytesmultiple sclerosisGIRK channelssecondary progressive multiple sclerosisGABAergic interneuronblood-brain barrierInhibitorinhibitorinhibit

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