891859-12-4

Ceralifimod is an agonist of the sphingosine-1-phosphate (S1P) receptors S1P₁ and S1P₅ (K_is = 0.626 and 0.574 nM, respectively). It is selective for S1P₁ and S1P₅ over S1P_2-4 (K_is = >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.

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