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Siponimod

Catalog No. T6403   CAS 1230487-00-9
Synonyms: BAF-312

BAF312 (Siponimod (BAF-312)), a next-generation S1P receptor modulator, is specific for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, respectively. The specificity of BAF312 for S1P1 and S1P5 receptors exhibits <1000-fold over S1P2, S1P3 and S1P4 receptors.

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Siponimod Chemical Structure
Siponimod, CAS 1230487-00-9
Pack Size Availability Price/USD Quantity
2 mg In stock $ 33.00
5 mg In stock $ 52.00
10 mg In stock $ 79.00
25 mg In stock $ 142.00
50 mg In stock $ 235.00
100 mg In stock $ 327.00
1 mL * 10 mM (in DMSO) In stock $ 59.00
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Purity: 99.29%
Purity: 99.13%
Purity: 97.79%
Purity: 97.08%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description BAF312 (Siponimod (BAF-312)), a next-generation S1P receptor modulator, is specific for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, respectively. The specificity of BAF312 for S1P1 and S1P5 receptors exhibits >1000-fold over S1P2, S1P3 and S1P4 receptors.
Targets&IC50 S1P5 receptor:0.98 nM(EC50), S1P1 receptor:0.39 nM(EC50)
Kinase Assay GTPγ[35S] binding assay: The cells are homogenized and centrifuged at 26900 × g for 30 min at 4°C. Membranes are re-suspended in 20 mM HEPES (pH 7.4), 100 mM NaCl, 10 mM MgCl2, 1 mM EDTA and 0.1% fat-free BSA at 2–3 mg protein/mL. GTPγ[35S] binding assay is performed with the membranes (75 mg protein /mL in 50 mM HEPES, 100 mM NaCl, 10 mM MgCl2, 20 μg/mL saponin and 0.1% fat-free BSA (pH 7.4), 5 mg/mL with wheat-germ agglutinin-coated scintillation proximity assay-bead, and 10 μM GDP for 10–15 min. The GTPγ[35S]-binding reaction is started by the addition of 200 pM GTPγ[35S]. After 120 min at room temperature, the plates are centrifuged for 10 min at 300 × g and counted.
Cell Research Agonist-mediated internalization of S1P1 receptors in CHO cells analysed by flow cytometry Myc-tag hS1P1 cells are incubated for 1 h with agonist at 37°C in standard culture medium followed by a PBS wash. An aliquot is kept on ice for 3 h, while another aliquot is left for 3 (or 12) h in culture medium (no agonist) at 37°C. The cells are then incubated either with 4 μg/mL monoclonal mouse anti C-myc IgG1 antibody or with isotype control mouse IgG1 for 60 min at 4°C, followed by an incubation with 1 μg/mL of Alexa488-labelled goat anti-mouse secondary conjugates. The cells are subjected to flow cytometry measurements using 10000 viable cells per sample.(Only for Reference)
Synonyms BAF-312
Molecular Weight 516.59
Formula C29H35F3N2O3
CAS No. 1230487-00-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 41 mg/mL (79.4 mM)

DMSO: 93 mg/mL (180 mM)

TargetMolReferences and Literature

1. Gergely P, et al. Br J Pharmacol, 2012, 167(5), 1035-1047. 2. Pan S, et al. ACS Med, Chem, Lett, 2013, 4 (3), 333–337. 3. Lewis ND, et al. J Immunol, 2013, 190(7), 3533-3540. 4. Fauzyah Y, Ono C, Torii S, et al. Ponesimod suppresses hepatitis B virus infection by inhibiting endosome maturation[J]. Antiviral Research. 2020: 104999.

TargetMolCitations

1. Fauzyah Y, Ono C, Torii S, et al. Ponesimod suppresses hepatitis B virus infection by inhibiting endosome maturation. Antiviral Research. 2021 Feb;186:104999

Related compound libraries

This product is contained In the following compound libraries:
Anti-Neurodegenerative Disease Compound Library EMA Approved Drug Library Anti-Cancer Clinical Compound Library GPCR Compound Library Membrane Protein-targeted Compound Library Anti-Cancer Approved Drug Library Drug Repurposing Compound Library Highly Selective Inhibitor Library Anti-Cancer Drug Library Approved Drug Library

Related Products

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Amiselimod hydrochloride LX-2931 Ponesimod MHP PF-543 hydrochloride Peretinoin ML-031 SKI II

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Keywords

Siponimod 1230487-00-9 GPCR/G Protein LPL Receptor S1P Receptor inflammation Lysophospholipid Receptor S1P receptor inhibit neurodegeneration S1P1 agonist progressive multiple sclerosis lymphocytes BAF-312 BAF312 BAF 312 Inhibitor inhibitor

 

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