CS-2100 is a potent, selective, orally active S1P1 agonist with EC50 of 4.0 nM, over 5000-fold selectivity against S1P3.
CS-2100 demonstrates in vivo immunosuppressive efficacy in rats on host versus graft reaction with ID(50) value of 0.407mg/kg.
CS-2100 (0.1 and 1 mg/kg, oral) decreased significantly lymphocyte counts in rats.
CS-2100 is efficacious in the adjuvant-induced arthritis model in rats (ID50=0.44 mg/kg).
CS-2100 (0.1 and 1 mg/kg) significant decreases in the cumulative EAE scores in the EAE model.
