ChemicalBook--->CAS DataBase List--->952565-91-2

952565-91-2

952565-91-2 Structure

952565-91-2 Structure
IdentificationBack Directory
[Name]

ASP-4058
[CAS]

952565-91-2
[Synonyms]

ASP-4058
ASP 4058,ASP4058
[Molecular Formula]

C19H12F6N4O2
[MDL Number]

MFCD31813625
[MOL File]

952565-91-2.mol
[Molecular Weight]

442.31
Chemical PropertiesBack Directory
[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
Hazard InformationBack Directory
[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
Spectrum DetailBack Directory
[Spectrum Detail]

ASP-4058(952565-91-2)1HNMR
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