ASP-4058是一个选择性的、口服活性的鞘氨醇磷酸受体1和5(S1P1andS1P5)的二代激动剂，能改善小鼠实验性自身免疫性脑脊髓炎，具有良好的安全性。
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[1].
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[1].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[1].|| Animal Model:|Male Lewis rats with an induction of EAE[1].|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[1].|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).
[1]. Rie Yamamoto, et al. ASP4058, a Novel Agonist for Sphingosine 1-Phosphate Receptors 1 and 5, Ameliorates Rodent Experimental Autoimmune Encephalomyelitis with a Favorable Safety Profile. PLoS One. 2014 Oct 27;9(10):e110819.
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