An S1P1 receptor modulator; selective for S1P1 and S1P5 over S1P2

Siponimod – 1 mg

Brand:
Cayman
CAS:
1230487-00-9
Storage:
-20
UN-No:
De Minimis - 3077 / 9

Siponimod is an orally bioavailable agonist of the sphingosine-1-phosphate (S1P) receptor that is selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4 (EC50s = 0.39, 0.98, >10,000, >1,000, and 750 nM, respectively, in a radioligand binding assay).{41000,41002} Siponimod activation of the S1P1 receptor leads to receptor internalization, similar to the related compound fingolimod (Item No. 11975), and attenuates psychosine-induced demyelination in organotypic cerebellar slice cultures.{41000,41001} Siponimod (0.3 mg/kg/day) reduces experimental autoimmune encephalomyelitis (EAE) symptoms in rats.{41000} Formulations containing siponimod are in clinical trials for secondary progressive multiple sclerosis.  

 

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Description

An S1P1 receptor modulator; selective for S1P1 and S1P5 over S1P2, S1P3, and S1P4 (EC50s = 0.39, 0.98, >10,000, >1,000, and 750 nM, respectively; binding leads to receptor internalization; attenuates psychosine-induced demyelination in organotypic slice cultures; reduces EAE symptoms in rats at a dose of 0.3 mg/kg/day

Formal name: 1-[[4-[(1E)-1-[[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]imino]ethyl]-2-ethylphenyl]methyl]-3-azetidinecarboxylic acid

Synonyms:  BAF312

Molecular weight: 516.6

CAS: 1230487-00-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Agonists||Research Area|Immunology & Inflammation|Autoimmunity||Research Area|Lipid Biochemistry|Sphingolipids||Research Area|Neuroscience

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