ASP-4058

SKU: orb1710380

Description

ASP-4058 is a second-generation, orally bioavailable agonist selectively targeting S1P1 and S1P5 receptors. It demonstrates efficacy in preclinical models, notably ameliorating experimental autoimmune encephalomyelitis (EAE) in mice, supporting its research application in neuroinflammatory and autoimmune disease studies.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 952565-91-2
• MW: 442.31
• Purity: 99.96% (May vary between batches)
• Formula: C₁₉H₁₂F₆N₄O₂
• SMILES: C[C@H](Oc1ccc(cc1C(F)(F)F)-c1nc(no1)-c1ccc2nc[nH]c2c1)C(F)(F)F
• Target: LPL Receptor,S1P Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.52 mM);DMSO:70 mg/mL (158.26 mM)

Bioactivity

• In Vivo:
  ASP4058 (0.1 and 0.3 mg/kg; 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 value for ASP4058 is 0.063 mg/kg. ASP4058 (0.03, 0.1, and 0.3 mg/kg; 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 the vehicle-treated group is 15.5±0.619 in rats.
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• In Vitro:
  ASP4058 (100 nM) significantly reduced FITC-dextran leakage through an endothelial monolayer and suppressed the migration of macrophages across the monolayer in vitro by using a Transwell system.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

ASP 4058, ASP4058, ASP-4058, LPLReceptor, LPL Receptor, S1P Receptor, S1P5, S1PReceptor, S1P1

Compound Identifiers

PubChem CID

16755143