A S1P1 receptor modulator
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Cenerimod

Item No. 29665

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
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(Learn about Variance in Solubility)
DMF: 25 mg/mlDMF:PBS (pH 7.2) (1:2): 0.3 mg/mlDMSO: 20 mg/mlEthanol: 10 mg/ml
λmax
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $80

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    10 mg

    $149

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    25 mg

    $332

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    Product Description

    Cenerimod is a sphingosine-1-phosphate receptor 1 (S1P1) modulator with an EC50 value of 1 nM in a [35S]GTPɣS binding assay.1 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.2 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 encephalomyelitis (EAE).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Piali, L., Birker-Robaczewska, M., Lescop, C., et al. Cenerimod, a novel selective S1P1 receptor modulator with unique signaling properties. Pharmacol. Res. Perspec. 5(6), e00370 (2017).

    2. Kano, M., Kobayashi, T., Date, M., et al. Attenuation of murine sclerodermatous models by the selective S1P1 receptor modulator cenerimod. Sci. Rep. 9(1), 658 (2019).