Siponimod (Synonyms: BAF-312)

Name: Siponimod
Brand: MedChemExpress
SKU: HY-12355
Rating: 5.0 (10 reviews)

Cat. No.: HY-12355 Purity: 99.95%: Data Sheet
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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.

For research use only. We do not sell to patients.

CAS No. : 1230487-00-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of Siponimod:

10 Publications Citing Use of MCE Siponimod

In Vivo Efficacy Study

Others

Flow Cytometry

Histological Imaging/Staining

: 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.

: 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.

: Siponimod 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

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

S1PR1

0.39 nM (EC₅₀)

S1PR5

0.98 nM (EC₅₀)

S1PR4

750 nM (EC₅₀)

S1PR3

>1000 nM (EC₅₀)

S1PR2

>10000 nM (EC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
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	0.98 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	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	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]

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.

Clinical Trial

Molecular Weight

516.60

Formula

C₂₉H₃₅F₃N₂O₃

CAS No.

1230487-00-9

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.95%

Select Batch:

Data Sheet (276 KB) SDS (393 KB)

COA (245 KB) HNMR (283 KB) LCMS (134 KB)

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

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

Siponimod Related Classifications

Inflammation/Immunology Infection

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.

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Siponimod (Synonyms: BAF-312)

Customer Review

Other Forms of Siponimod:

Siponimod Related Antibodies

10 Publications Citing Use of MCE Siponimod

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All LPL Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Siponimod Related Antibodies

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Complete Stock Solution Preparation Table

Siponimod Related Classifications

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