Cenerimod

Cenerimod is a sphingosine-1-phosphate receptor 1 (S1P1) modulator with an EC50 value of 1 nM in a [35S]GTP?S binding assay. 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-beta-induced increases in collagen levels in primary mouse skin fibroblasts. 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).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. CAS Number: 1262414-04-9. Molecular Formula: C25H31N3O5. Formula Weight: 453.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 25 mg/ml, DMF:PBS (pH 7.2) (1:2): 0.3 mg/ml, DMSO: 20 mg/ml, Ethanol: 10 mg/ml. lambdamax: 249 nm. SMILES: CC1=C(OC[C@@H](O)CO)C(CC)=CC(C2=NOC(C3=CC(C4CCCC4)=NC(OC)=C3)=N2)=C1. InChi Code: InChI=1S/C25H31N3O5/c1-4-16-10-18(9-15(2)23(16)32-14-20(30)13-29)24-27-25(33-28-24)19-11-21(17-7-5-6-8-17)26-22(12-19)31-3/h9-12,17,20,29-30H,4-8,13-14H2,1-3H3/t20-/m0/s1. InChi Key: KJKKMMMRWISKRF-FQEVSTJZSA-N.