1230487-00-9
Chemical Structure
Siponimod
Synonym(s): BAF-312
- CAS No.: 1230487-00-9
- Formula:C29H35F3N2O3
- Molecular Weight:516.60
IUPAC Name: (E)-1-(4-(1-(((4-cyclohexyl-3-(trifluoromethyl)benzyl)oxy)imino)ethyl)-2-ethylbenzyl)azetidine-3-carboxylic acid
InChIKey: KIHYPELVXPAIDH-HNSNBQBZSA-N
SMILES: O=C(C1CN(CC2=CC=C(/C(C)=N/OCC3=CC=C(C4CCCCC4)C(C(F)(F)F)=C3)C=C2CC)C1)O
Biological Activity: Siponimod (BAF-312) is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC50 values of 0.39 nM and 0.98 nM, respectively. Siponimod induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod can be used in research related to multiple sclerosis[1][2][3][4].
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Siponimod | 99.95% | Siponimod (BAF-312) is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC50 values of 0.39 nM and 0.98 nM, respectively. Siponimod induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod can be used in research related to multiple sclerosis. | ||||||||||||||||||||
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Siponimod (Standard) | ≥98% | Siponimod (BAF-312) (Standard) is the analytical standard of Siponimod. This product is intended for research and analytical applications. Siponimod is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC50 values of 0.39 nM and 0.98 nM, respectively. Siponimod induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod can be used in research related to multiple sclerosis. | ||||||||||||||||||||
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Siponimod-d11 | Siponimod-d11 (BAF-312-d11) is deuterium labeled Siponimod (HY-12355). Siponimod is an orally active, blood-brain barrier penetrant dual agonist of S1P1/S1P5, with EC50 values of 0.39 nM and 0.98 nM, respectively. Siponimod induces S1P1 internalization, activates GIRK channels, inhibits lymphocyte egress, reduces peripheral lymphocyte counts, triggers transient bradycardia, prevents synaptic neurodegeneration, promotes remyelination, alleviates demyelination, and prevents the loss of GABAergic interneurons. Siponimod can be used in research related to multiple sclerosis. | |||||||||||||||||||||
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- [1]. Gergely P, et al. The selective sphingosine 1-phosphate receptor modulator BAF312 redirects lymphocyte distribution and has species-specific effects on heart rate. Br J Pharmacol. 2012;167(5):1035-1047. [Content Brief]
- [2]. Pan S, et al. Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator. ACS Med Chem Lett. 2013;4(3):333-337. Published 2013 Jan 4. [Content Brief]
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[3]. McGinley M, Fox RJ. Prospects of siponimod in secondary progressive multiple sclerosis. Ther Adv Neurol Disord. 2018 Jul 17;11:1756286418788013.
[Content Brief] - [4]. Behrangi N, et al. Mechanism of Siponimod: Anti-Inflammatory and Neuroprotective Mode of Action. Cells. 2019;8(1):24. Published 2019 Jan 7. [Content Brief]
