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 profile In Vivo 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 . 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:Solid IC50& Target:S1P 1 and S1P 5
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ASP-4058
CAS number：952565-91-2 molecular formula：C19H12F6N4O2
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| Chinese alias | - | ||
| English alias | ASP-4058 free base | HY-111021 | 1H-Benzimidazole, 6-(5-(3-(trifluoromethyl)-4-((1S)-2,2,2-trifluoro-1-methylethoxy)phenyl)-1,2,4-oxadiazol-3-yl)- | DB11819 | 952565-91-2 (free base) | 01J7526K2Q | 5-(5-(3-(Trifluoromethyl)-4-(((2S)-1,1,1-trifluoropropan- | ||
| CAS number | 952565-91-2 | molecular formula | C19H12F6N4O2 |
| molecular weight | 442.31 g/mol | Exact mass | - |
| PSA | 76.800 Ų | logp | 5.4 |
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