ASP-4058 (C09-1102-638)

ASP-4058 is a next-generation, selective and oral bioactive agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P 1 and S1P 5 ) , ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profileIn VivoASP4058 (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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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).Form:SolidIC50& Target:S1P 1 and S1P 5. Specification: 0.99 Molecular Formula: C19H12F6N4O2 Molecular Weight: 442.31 PubChem CID: 16755143 Isomeric SMILES: C[C@@H](C(F)(F)F)OC1=C(C=C(C=C1)C2=NC(=NO2)C3=CC4=C(C=C3)N=CN4)C(F)(F)F