ASP-4058 is a selective and oral bioactive agonist for S1P1 and S1P5. It ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile.

ASP4058 (p.o., daily for 21 days) reduces the clinical score in a dose-dependent manner and the cumulative clinical score from day 0 to 21 dpi at 0.03, 0.1 and 0.3 mg/kg are 15.5±1.48, 9.50±2.17 and 1.17±1.17, respectively, while that of the vehicle-treated group is 15.5±0.619 in rats. ASP4058 prevents decreases in the body weight of EAE rats. ASP4058 (p.o., daily for day 12 to day 45) maintains the clinical score at a relatively low level and the cumulative clinical scores (18-45 dpi) among the groups treated with 0.1 and 0.3 mg/kg dosages are 6.90±2.85 and 5.60±2.21, respectively in mice. The ED50 values for ASP4058 is 0.063 mg/kg.

952565-91-2

C19H12F6N4O2

442.31

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years