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编 号:F536716
分子式:C19H12F6N4O2
分子量:442.31
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1mg
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5mg
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10mg
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25mg
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生物活性:
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.

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).
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