ASP-4058

Research use only, not for human use.

ASP-4058 is a selective, safe, and orally active second-generation agonist of sphingosine phosphate receptors 1 and 5 (S1P1 and S1P5).

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.

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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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GPCR/G Protein

S1P Receptor

S1P Receptor | LPL Receptor

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952565-91-2

442.31

C19H12F6N4O2

>98% (HPLC)

In Vitro:?DMSO : ≥ 50 mg/mL (113.04 mM)

C[C@H](Oc1ccc(cc1C(F)(F)F)-c1nc(no1)-c1ccc2nc[nH]c2c1)C(F)(F)F

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(-20℃)

With Ice Pack

≥ 2 years