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

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 1 mg | $60 | In Stock | In Stock | |
| 5 mg | $148 | In Stock | In Stock | |
| 10 mg | $238 | In Stock | In Stock | |
| 25 mg | $429 | In Stock | In Stock | |
| 50 mg | $588 | In Stock | In Stock | |
| 100 mg | $828 | In Stock | In Stock |
| Description | ASP-4058 is a selective, safe, and orally active second-generation agonist of sphingosine phosphate receptors 1 and 5 (S1P1 and S1P5).ASP-4058 ameliorates experimental autoimmune encephalomyelitis in mice. |
| 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.[2] |
| 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.[1] 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.[1] |
| Molecular Weight | 442.31 |
| Formula | C19H12F6N4O2 |
| Cas No. | 952565-91-2 |
| Smiles | C[C@H](Oc1ccc(cc1C(F)(F)F)-c1nc(no1)-c1ccc2nc[nH]c2c1)C(F)(F)F |
| Relative Density. | 1.463 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 70 mg/mL (158.26 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.52 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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