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Siponimod (BAF312)

Name: Siponimod (BAF312)
Brand: Selleck Chemicals
SKU: S7179
Rating: 5 (9 reviews)

Catalog No.S7179

For research use only.

BAF312 (Siponimod) is a next-generation S1P receptor agonist, selective for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, exhibits >1000-fold selectivity over S1P2, S1P3 and S1P4 receptors. Phase 3.

CAS No. 1230487-00-9

Selleck's Siponimod (BAF312) has been cited by 9 Publications

1 Customer Review

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S1P Receptor Signaling Pathway Map

Biological Activity

Description

Targets

S1P1 receptor ^[1]	S1P5 receptor ^[1]
0.39 nM(EC50)	0.98 nM(EC50)

In vitro

BAF312 (Siponimod) is a potent and selective S1P receptor agonist, with EC50 of 0.39 nM and 0.98 nM for S1P₁ and S1P₅receptors, exhibits >1000-fold selectivity over S1P₂, S1P₃ and S1P₄ receptors. ^[1]BAF312 (1 h at 1 μM) promotes prominent internalization of S1P1 receptors by 91%.^[2]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID

CHO	Ml[xSpVv[3Srb36gZZN{[Xl?	NX;4Npo3OTJyIH3pcpM>	NILkUm5C\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJHMyWDFicnXj[ZB1d3JidILhcpNn\WO2ZXSgbY4hS0iRIHPlcIx{KGmwY4XiZZRm\CCob4KgNVAhfG9iMUWgcYlveyCycnnvdkB1dyCJVGDnZY1u[TN3UzDh[IRqfGmxbjDt[YF{fXKnZDDh[pRmeiBzMkCgcYlveyCkeTDHWHBo[W2vYUO1V{BjcW6maX7nJIF{e2G7LDDFR\|UxRTBwMECwOO69VQ>?	NVniUId2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA3PzBpPkK0PVAxPjdyPD;hQi=>
CHO	MnuwSpVv[3Srb36gZZN{[Xl?		MWPB[49vcXO2IHHjeIl3cXS7IHH0JIh2dWGwIGOxVFUhemWlZYD0c5Ih\XiycnXzd4VlKGmwIFPIU{Bk\WyuczDifUBcOzWVXVfUVIdidW2jUzDibY5lcW6pIHHzd4F6NCCHQ{WwQVAvODByOUlOwG0>	MV68ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zPDF{NUi4OEc,OjRzMkW4PFQ9N2F-
CHO	MWPGeY5kfGmxbjDhd5NigQ>?		NVfUVpZ2SWexbnnzeEBi[3Srdnn0fUBifCCqdX3hckBUOVB2IILlZ4VxfG:{IHX4dJJme3OnZDDpckBEUE9iY3XscJMh[nliW{O1V31IXFCpYX3tZXMh[mmwZHnu[{Bie3OjeTygSWM2OD1yLke1{txO	NIDvRVE9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{NEGyOVg5PCd-MkSxNlU5QDR:L3G+
CHO	MV;GeY5kfGmxbjDhd5NigQ>?	MnLYNVIxKG2rboO=	NIrsXItC\2:waYP0JIFkfGm4aYT5JIF1KGi3bXHuJHMyWDNicnXj[ZB1d3JidILhcpNn\WO2ZXSgbY4hS0iRIHPlcIx{KGmwY4XiZZRm\CCob4KgNVAhfG9iMUWgcYlveyCycnnvdkB1dyCJVGDnZY1u[TN3UzDh[IRqfGmxbjDt[YF{fXKnZDDh[pRmeiBzMkCgcYlveyCkeTDHWHBo[W2vYUO1V{BjcW6maX7nJIF{e2G7LDDFR\|UxRTYQvF2=	NV;hVXUyRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC\|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkS5NFA3PzBpPkK0PVAxPjdyPD;hQi=>

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Assay

Methods	Test Index	PMID

Western blot	p-ERK / ERK / p-AKT / AKT	26856814
Immunofluorescence	Vimentin / S1PR1	26856814

In vivo

BAF312 effectively suppresses encephalomyelitis (EAE) in rats by internalizing S1P₁ receptors, rendering them insensitive to the egress signal from lymph nodes. ^[1] BAF312 significantly reduces clinical scores when dosed prophylactically or therapeutically in mice at 0.3 mg/kg. ^[3]

Protocol (from reference)

Kinase Assay:^[1]	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: ^[1]	Cell lines: CHO Concentrations: ~1 μM Incubation Time: 1 h Method: 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.
Animal Research:^[1]	Animal Models: encephalomyelitis (EAE) model rat Dosages: 0.03, 0.3 and 3 mg/kg Administration: oral gavage

References

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight	516.6
Formula	C₂₉H₃₅F₃N₂O₃
CAS No.	1230487-00-9
Storage	3 years	-20°C	powder
Storage	2 years	-80°C	in solvent
Smiles	CCC1=C(C=CC(=C1)C(=NOCC2=CC(=C(C=C2)C3CCCCC3)C(F)(F)F)C)CN4CC(C4)C(=O)O

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In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Molarity Calculator

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Clinical Trial Information

NCT Number	Recruitment	Interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05376579	Recruiting	Other: siponimod	Active Secondary Progressive Multiple Sclerosis	Novartis Pharmaceuticals\|Novartis	June 17 2022	--
NCT04895202	Recruiting	Other: Siponimod	Secondary Progressive Multiple Sclerosis With Inflammatory Disease Activity	Novartis Pharmaceuticals\|Novartis	November 19 2021	--
NCT03623243	Active not recruiting	Drug: Siponimod	Multiple Sclerosis\|Relapsing Multiple Sclerosis\|Advancing Multiple Sclerosis	Novartis Pharmaceuticals\|Novartis	February 14 2019	Phase 3
NCT02029274	Terminated	Drug: BAF312\|Drug: Placebo	Active Dermatomyositis	Novartis Pharmaceuticals\|Novartis	August 25 2013	Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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