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BAF312, a potent sphingosine-1 receptor (S1P-R) modulator selectively …

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BAF312, a potent sphingosine-1 receptor (S1P-R) modulator selectively targeting

S1P1 and S1P5 receptors

 

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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].

 

Details

Chemical Formula:

 

C29H35F3N2O3

CAS No.:

 

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 200 mM in DMSO

Synonyms:

 

Siponimod

Storage:

 

For longer shelf life, store solid powder or DMSO solution at -20oC desiccated.

 

References

1.

Pan S, et al. Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator. ACS Med Chem Lett. 2013; 4(3): 333–337. 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

 

Ordering information

   

Catalog No.

Product Name

Size

C2233

BAF312

5mg, 25mg & 100mg

     

 

▣ 관련 페이지 ; Cellagen Technology

 

   

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