Referencia número: HY-12355

Siponimod

(Synonyms: BAF-312)

11 Cited Publications

Revisión del cliente

Based on 11 publication(s) in Google Scholar

Siponimod (BAF-312) 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 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 can be used in research related to multiple sclerosis.

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Pureza: 99.95%
No. CAS: 1230487-00-9
Fòrmula: C₂₉H₃₅F₃N₂O₃
Peso molecular:516.60

Almacenamiento:

4°C, sealed storage, away from moisture

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

Siponimod Chemical Structure

No. CAS: 1230487-00-9

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Precio

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (11)
Solvente y solubilidad
- In Vitro
- In Vivo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

IC₅₀ & Target

S1PR1

0.39 nM (EC₅₀)

S1PR5

0.98 nM (EC₅₀)

S1PR4

750 nM (EC₅₀)

S1PR3

>1000 nM (EC₅₀)

S1PR2

>10000 nM (EC₅₀)

Ver todos los productos específicos de isoformas LPL Receptor :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	EC₅₀	0.98 nM Compound: 3, BAF312	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	[PMID: 24125884]
CHO	EC₅₀	750 nM Compound: 3, BAF312	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	[PMID: 24125884]
CHO	EC₅₀	5 μM Compound: 32, BAF312, Siponimod	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	[PMID: 24900670]
CHO	EC₅₀	0.0004 μM Compound: 32, BAF312, Siponimod	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	[PMID: 24900670]
CHO	EC₅₀	0.4 nM Compound: 32, BAF312, Siponimod	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	[PMID: 24900670]

In Vitro

Siponimod (10-1000 nM; 4-13 h) 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 regulates microglial function by reducing IL6 secretion in cultured microglia^[4].
Siponimod 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.

In Vivo

Siponimod (0.03-3 mg/kg; p.o.; daily; day 11 to day 34 post-immunization) 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) 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.

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 1230487-00-9
Appearance Solid
Peso molecular 516.60
Fòrmula C₂₉H₃₅F₃N₂O₃
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
Synonyms

BAF-312
Envío

Room temperature in continental US; may vary elsewhere.
Almacenamiento

4°C, sealed storage, away from moisture

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

Publications (11)

All In Vivo Efficacy StudyOthersFlow CytometryHistological Imaging/StainingWB

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Journal Impact Factor

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
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
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
Int J Mol Sci

Structural Characterization, Toxicity Assessment and Molecular Modeling of Forced Degradation Products of Siponimod. [Abstract]

2026 Apr 18;27(8):3630. PMID: 42074265
Sci Rep

Siponimod treatment response shows partial BDNF dependency in multiple sclerosis models. [Abstract]

2024 Aug 1;14(1):17823. PMID: 39090252

Siponimod 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 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.
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
Cell Signal

Characterization of functionally relevant G protein-coupled receptors in endometriotic epithelial cells. [Abstract]

2025 Sep:133:111876. PMID: 40381972
Neurosci Res

Siponimod inhibits microglial inflammasome activation. [Abstract]

2025 Apr:213:138-145. PMID: 39921000

Siponimod 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 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.
Neurosci Res

Anti-inflammatory effects of siponimod on astrocytes. [Abstract]

2022 Nov:184:38-46. PMID: 35940437
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 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.

Solvente y solubilidad

In Vitro:

DMSO : 25 mg/mL (48.39 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.9357 mL

9.6787 mL

19.3573 mL

5 mM

0.3871 mL

1.9357 mL

3.8715 mL

10 mM

0.1936 mL

0.9679 mL

1.9357 mL

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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculadora de molaridad

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.84 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 4

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: 1.67 mg/mL (3.23 mM); Suspended solution; Need ultrasonic

Protocol 5

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: 1.67 mg/mL (3.23 mM); Suspended solution; Need ultrasonic

Protocol 6

Add each solvent one by one: 1% DMSO 99% Saline

Solubility: 0.33 mg/mL (0.64 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (276 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9357 mL	9.6787 mL	19.3573 mL	48.3933 mL
	5 mM	0.3871 mL	1.9357 mL	3.8715 mL	9.6787 mL
	10 mM	0.1936 mL	0.9679 mL	1.9357 mL	4.8393 mL
	15 mM	0.1290 mL	0.6452 mL	1.2905 mL	3.2262 mL
	20 mM	0.0968 mL	0.4839 mL	0.9679 mL	2.4197 mL
	25 mM	0.0774 mL	0.3871 mL	0.7743 mL	1.9357 mL
	30 mM	0.0645 mL	0.3226 mL	0.6452 mL	1.6131 mL
	40 mM	0.0484 mL	0.2420 mL	0.4839 mL	1.2098 mL

Keywords

Siponimod

11 Cited Publications

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Siponimod

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Anti-Infection Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Publications Citing Use of MedChemExpress (MCE) Siponimod

Ver todos los productos específicos de isoformas LPL Receptor

Actividad biológica

Chemical Information

Publications (11)

Solvente y solubilidad

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

Siponimod Related Classifications

HY-12355 Related Classifications