An agonist of S1P1 and S1P5 receptors
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Ceralifimod

Item No. 24159

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[[3,4-dihydro-6-[(2-methoxy-4-propylphenyl)methoxy]-1-methyl-2-naphthalenyl]methyl]-3-azetidinecarboxylic acid
CAS Number
891859-12-4
Synonyms
  • ONO-4641
Molecular Formula
C27H33NO4
Formula Weight
435.6
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 5 mg/mlDMSO: 5 mg/mlDMSO:PBS (pH 7.2)(1:9): 0.1 mg/mlEthanol: slightly soluble
λmax
280 nm
SMILES
CCCC1=CC=C(COC2=CC(CCC(CN3CC(C(O)=O)C3)=C4C)=C4C=C2)C(OC)=C1
InChi Code
InChI=1S/C27H33NO4/c1-4-5-19-6-7-22(26(12-19)31-3)17-32-24-10-11-25-18(2)21(9-8-20(25)13-24)14-28-15-23(16-28)27(29)30/h6-7,10-13,23H,4-5,8-9,14-17H2,1-3H3,(H,29,30)
InChi Key
QDDQIPUKAXBMBX-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

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    Product Description

    Ceralifimod is an agonist of the sphingosine-1-phosphate (S1P) receptors S1P1 and S1P5 (Kis = 0.626 and 0.574 nM, respectively).1 It is selective for S1P1 and S1P5 over S1P2-4 (Kis = >5,450, >5,630, and 28.8 nM, respectively). Ceralifimod induces calcium influx in CHO-K1 cells overexpressing S1P1 (EC50 = 1 nM) and cAMP accumulation in CHO-K1 cells overexpressing S1P1 or S1P5 (EC50s = 0.027 and 0.33 nM, respectively). In vivo, ceralifimod (0.03 and 0.1 mg/kg) reduces paw edema in a rat model of collagen induced arthritis (CIA). It also delays disease onset and inhibits lymphocyte infiltration of the spinal cord in a rat model of experimental autoimmune encephalomyelitis (EAE) and prevents disease relapse in a non-obese diabetic mouse model of relapsing-remitting EAE.2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kurata, H., Kusumi, K., Otsuki, K., et al. Discovery of a 1-methyl-3,4-dihydronaphthalene-based sphingosine-1-phosphate (S1P) receptor agonist ceralifimod (ONO-4641). A S1P1 and S1P5 selective agonist for the treatment of autoimmune disease. J. Med. Chem. 60(23), 9508-9530 (2017).

    2. Komiya, T., Sato, K., Shioya, H., et al. Efficacy and immunomodulatory actions of ONO-4641, a novel selective agonist for sphingosine 1-phosphate receptors 1 and 5, in preclinical models of multiple sclerosis. Clin. Exp. Immunol. 171(1), 54-62 (2013).