1. GPCR/G Protein
  2. LPL Receptor

ASP-4058 

Cat. No.: HY-111021
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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.

For research use only. We do not sell to patients.

ASP-4058 Chemical Structure

ASP-4058 Chemical Structure

CAS No. : 952565-91-2

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  • Technical Information

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  • References

Description

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].

IC50 & Target

S1P1 and S1P5[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
Molecular Weight

442.31

Formula

C₁₉H₁₂F₆N₄O₂

CAS No.

952565-91-2

SMILES

C[[email protected]](OC1=CC=C(C2=NC(C3=CC=C4N=CNC4=C3)=NO2)C=C1C(F)(F)F)C(F)(F)F

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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ASP-4058
Cat. No.:
HY-111021
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ASP-4058

Cat. No.: HY-111021