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Siponimod

Catalog No. T6403 CAS 1230487-00-9

Synonyms: BAF-312

BAF312 (Siponimod), a next-generation <a href="/target/S1P_Receptor" style="display: inline; color: #c13a36">S1P Receptor</a> 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, CAS 1230487-00-9

Pack Size	Availability	Price/USD
2 mg	In stock	$ 50.00
5 mg	In stock	$ 64.00
10 mg	In stock	$ 94.00
25 mg	In stock	$ 176.00
50 mg	In stock	$ 262.00
1 mL * 10 mM (in DMSO)	In stock	$ 73.00

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Purity: 97.08%

Purity: 99.29%

Purity: 99.13%

Purity: 97.79%

Purity: 98%

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Chemical Properties

Storage & Solubility Information

Description	BAF312 (Siponimod), 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	516.605
Formula	C29H35F3N2O3
CAS No.	1230487-00-9

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: 41 mg/mL (79.4 mM)

DMSO: 93 mg/mL (180 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References 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.

Citations

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：

Bioactive Compounds Library Max Clinical Compound Library FDA-Approved Drug Library Fluorochemical Library Immunology/Inflammation Compound Library ReFRAME Related Library Pediatric Drug Library Anti-Cancer Compound Library Approved Drug Library NO PAINS Compound Library

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GLPG2938 ONO-7300243 GSK2018682 Ki16198 SLF1081851 Ki16425 PF-543 CYM-5541

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Keywords

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

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