BAF312 (Siponimod) is a potent sphingosine-1 receptor (S1P-R) modulator selectively targeting S1P1 and S1P5 receptors [1]. BAF312 reduces inflammation by sequestering lymphocytes in lymphoid tissues [2]. BAF312 also binds its receptors on neurons, astrocytes and oligodendrocytes and present neuroprotective effects [3]. Siponimod showed neuroprotective effects in the CNS of encephalomyelitis mice and organotypic cultures. is currently under investigation in a clinical trial in secondary progressive multiple sclerosis patients [4].
Technical information:
Chemical Formula: | C29H35F3N2O3 | |
CAS #: | 1230487-00-9 | |
Molecular Weight: | 516.6 | |
Purity: | > 98% | |
Appearance: | White | |
Chemical Name: | (E)-1-(4-(1-(((4-cyclohexyl-3-(trifluoromethyl)benzyl)oxy)imino)ethyl)-2-ethylbenzyl)azetidine-3-carboxylic acid | |
Solubility: | Up to 200mM in DMSO | |
Synonyms: | Siponimod |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage condition: For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.
Reference:
1. | Pan S, et al. Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator. ACS Med Chem Lett. 2013; 4(3): 333337. Pubmed ID: 24900670 |
2. | Hundehege P, et al. The next-generation sphingosine-1 receptor modulator BAF312 (siponimod) improves cortical network functionality in focal autoimmune encephalomyelitis. Neural Regen Res 2019; 14:1950-60 Pubmed ID: 31290453 |
3. | Gentile A, et al. Siponimod (BAF312) prevents synaptic neurodegeneration in experimental multiple sclerosis. J Neuroinflammation. 2016; 13(1): 207. Pubmed ID: 27566665 |
4. | Kappos L, et al. Safety and Efficacy of Siponimod (BAF312) in Patients With Relapsing-Remitting Multiple Sclerosis Dose-Blinded, Randomized Extension of the Phase 2 BOLD Study. JAMA Neurol 2016;73(9):1089-98. Pubmed ID: 31290453 |
Other Information:
Product Specification (pdf)
MSDS (pdf)
Certificate of Analysis is available upon request.