ASP-4058 is a next-generation, selective and oral bioactive agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile.
IC50&Target
S1P1 and S1P5.
体内研究
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 vehicle-treated group is 15.5±0.619 in rats. ASP4058 prevents decreases in 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.
Animal Model:
Male Lewis rats with an induction of EAE.
Dosage:
0.03, 0.1 or 0.3 mg/kg.
Administration:
Oral administration once daily for 21 days.
Result:
Reduced the clinical score in a dose-dependent manner and the cumulative clinical score.
Animal Model:
SJL mice immunized with PLP139-151 and boosted with pertussis toxin developed relapsing-remitting EAE.
Dosage:
0.1 and 0.3 mg/kg
Administration:
Oral administration once daily from day 12 to day 45.
Result:
Maintained the clinical score at a relatively low level and the cumulative clinical scores (18-45 dpi).
分子式
C19H12F6N4O2
分子量
442.31
CAS号
952565-91-2
运输条件
Room temperature in continental US; may vary elsewhere.