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BAF-312 fumarate

Names

[ CAS No. ]:
1234627-85-0

[ Name ]:
BAF-312 fumarate

[Synonym ]:
3-Azetidinecarboxylic acid, 1-[[4-[(1E)-1-[[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]imino]ethyl]-2-ethylphenyl]methyl]-, (2E)-2-butenedioate (2:1)
1-{4-[(1E)-N-{[4-Cyclohexyl-3-(trifluoromethyl)benzyl]oxy}ethanimidoyl]-2-ethylbenzyl}-3-azetidinecarboxylic acid (2E)-2-butenedioate (2:1)
MFCD31536984
Siponimod Fumarate

Biological Activity

[Description]:

Siponimod (BAF-312) hemifumarate is a potent and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod hemifumarate is selective for S1P1 and S1P5 receptors over S1P2, S1P3, and S1P4 (EC50s of 0.39, 0.98, >10000, >1000, and 750 nM, respectively). Siponimod hemifumarate can be used for multiple sclerosis (MS) research[1][2].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> LPL Receptor
Research Areas >> Inflammation/Immunology
Research Areas >> Neurological Disease

[Target]

S1PR1:0.39 nM (EC50)

S1PR5:0.98 nM (EC50)

S1PR4:750 nM (EC50)

S1PR3:>1000 nM (EC50)

S1PR2:>10000 nM (EC50)


[References]

[1]. Pan S, et al. Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator. ACS Med Chem Lett. 2013 Jan 4;4(3):333-7.

[2]. McGinley M, et al. Prospects of siponimod in secondary progressive multiple sclerosis. Ther Adv Neurol Disord. 2018 Jul 17;11:1756286418788013.

[3]. Behrangi N, et al. Mechanism of Siponimod: Anti-Inflammatory and Neuroprotective Mode of Action. Cells. 2019 Jan 7;8(1):24.

Chemical & Physical Properties

[ Molecular Formula ]:
C62H74F6N4O10

[ Molecular Weight ]:
1149.262

[ Exact Mass ]:
1148.530884

Related Compounds