1. GPCR/G Protein
  2. LPL Receptor
  3. Siponimod

Siponimod  (Synonyms: BAF-312)

Cat. No.: HY-12355 Purity: 98.88%
COA Handling Instructions

Siponimod (BAF-312) is an orally active and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4, with EC50s of 0.4, 0.98, >10000, >1000, and 750 nM, respectively. Siponimod can be used for multiple sclerosis (MS) research-.

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

Siponimod Chemical Structure

Siponimod Chemical Structure

CAS No. : 1230487-00-9

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10 mM * 1 mL in DMSO USD 75 In-stock
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1 g USD 2200 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

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Description

Siponimod (BAF-312) is an orally active and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4, with EC50s of 0.4, 0.98, >10000, >1000, and 750 nM, respectively. Siponimod can be used for multiple sclerosis (MS) research[1]-[4].

IC50 & Target

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 (compound 32) exhibits selectivity to S1P1 and S1P5, and spares activity on the S1P2, S1P3 and S1P4 receptors[1].
Siponimod (1 mM; 0-1 h) promotes internalization of S1P1 receptors, results 94% S1P1 receptors localized intracellularly at 1 h[2].
Siponimod (0.001 nM-1 μM; 1 h) activates the GIRK channel in atrial myocytes, with an EC50 value of 15.8 nM in CHO cell line CCL-61[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Siponimod (1 g/kg; i.v.; single dose) shows low to moderate in monkey, but high in rat in metabolism studies with liver microsomes. The absolute bioavailability is 50 and 71% in the rat and monkey, respectively, indicating no major presystemic first pass metabolism[1].
Siponimod (0.3, 3 mg/kg; p.o.; once daily; 23 d) suppresses experimental autoimmune encephalomyelitis (EAE) in rats by internalizing S1P1 receptors[2].
Parmacokinetics of Siponimod in rats and monkey[1]

/td> CL (L/h/kg) Vss (L/kg) T1/2 (h) F (%)
Rat 0.36 2.15 6 50
Monkey 0.098/td> 2.12 19 71

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Experimental autoimmune encephalomyelitis (EAE) model in Lewis rats (200-250 g)[2]
Dosage: 0.03, 0.3, 3 mg/kg
Administration: Oral gavage; once daily; 23 days
Result: Decreased peripheral lymphocyte counts by 88% at the Tmax of 8 h postadministration.
Clinical Trial
Molecular Weight

516.60

Formula

C29H35F3N2O3

CAS No.
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, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : ≥ 30 mg/mL (58.07 mM)

*"≥" means soluble, but saturation unknown.

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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

  • 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

  • 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

  • 6.

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

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

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 98.88%

References
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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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Product Name:
Siponimod
Cat. No.:
HY-12355
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