An S1P1 modulator (EC50 = 1 nM in a [35S]GTPɣS binding assay); selective for S1P1 over S1P2

Cenerimod – 25 mg

Brand:
Cayman
CAS:
1262414-04-9
Storage:
-20
UN-No:
Non-Hazardous - /

Cenerimod is a sphingosine-1-phosphate receptor 1 (S1P1) modulator with an EC50 value of 1 nM in a [35S]GTPɣS binding assay.{52269} It is selective for S1P1 over S1P2, -3, -4, and -5 (EC50s = >10,000, 228, 2,137, and 36 nM, respectively). Cenerimod (5 µM) decreases TGF-β-induced increases in collagen levels in primary mouse skin fibroblasts.{52270} It inhibits CD4+ T cell, CD8+ T cell, and CD11b+ cell infiltration, reduces IL1b, Il6, and Il13 expression, as well as decreases fibrosis in the skin of a mouse model of sclerodermatous chronic graft versus host disease induced by allogenic bone marrow transplant when administered at a dose of 10 mg/kg per day. Cenerimod (6 mg/kg per day for 32 days) reduces paralysis and spinal cord demyelination in a mouse model of experimental autoimmune encephalitis (EAE).  

 

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Description

An S1P1 modulator (EC50 = 1 nM in a [35S]GTPɣS binding assay); selective for S1P1 over S1P2, -3, -4, and -5 (EC50s = >10,000, 228, 2,137, and 36 nM, respectively); decreases TGF-β-induced increases in collagen levels in primary mouse skin fibroblasts at 5 µM; inhibits CD4+ T cell, CD8+ T cell, and CD11b+ cell infiltration, reduces IL1b, Il6, and Il13 expression, as well as decreases fibrosis in the skin of a mouse model of sclerodermatous chronic graft versus host disease induced by allogenic bone marrow transplant at 10 mg/kg per day; reduces paralysis and spinal cord demyelination in a mouse model of EAE at 6 mg/kg per day for 32 days

Formal name: (2S)-3-[4-[5-(2-cyclopentyl-6-methoxy-4-pyridinyl)-1,2,4-oxadiazol-3-yl]-2-ethyl-6-methylphenoxy]-1,2-propanediol

Synonyms: 

Molecular weight: 453.5

CAS: 1262414-04-9

Purity: ≥95%

Formulation: A crystalline solid

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