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| | ASP-4058 Basic information |
| Product Name: | ASP-4058 | | Synonyms: | ASP-4058;ASP 4058,ASP4058;1H-Benzimidazole, 6-[5-[3-(trifluoromethyl)-4-[(1S)-2,2,2-trifluoro-1-methylethoxy]phenyl]-1,2,4-oxadiazol-3-yl]-;(S)-3-(1H-Benzo[d]imidazol-6-yl)-5-(3-(trifluoromethyl)-4-((1,1,1-trifluoropropan-2-yl)oxy)phenyl)-1,2,4-oxadiazole | | CAS: | 952565-91-2 | | MF: | C19H12F6N4O2 | | MW: | 442.31 | | EINECS: | | | Product Categories: | | | Mol File: | 952565-91-2.mol |  |
| | ASP-4058 Chemical Properties |
| Boiling point | 581.1±60.0 °C(Predicted) | | density | 1.463±0.06 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | Soluble in DMSO | | form | Solid | | pka | 9.18±0.30(Predicted) | | color | White to off-white |
| | ASP-4058 Usage And Synthesis |
| Uses | 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]. | | 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[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). |
| | References | [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. DOI:10.1371/journal.pone.0110819 |
| | ASP-4058 Preparation Products And Raw materials |
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