Molecular Formula | C29H35F3N2O3 |
Molar Mass | 516.59 |
Density | 1.24±0.1 g/cm3(Predicted) |
Melting Point | 154 - 157°C |
Boling Point | 602.0±65.0 °C(Predicted) |
Solubility | DMSO: ≥ 30 mg/mL |
Appearance | Solid |
Color | White to Off-White |
pKa | 2.69±0.20(Predicted) |
Storage Condition | Hygroscopic, Refrigerator, under inert atmosphere |
In vitro study | BAF312 (Siponimod) is an effective and selective S1P receptor agonist. The EC50 of S1P 1 and S1P 5 receptors is 0.39 nM and 0.98 nM, which is higher than that of S1P 2, s1P 3 and S1P 4 receptors 1000 multiple-fold selectivity. BAF312 (1 H at 1 μm) promoted significant internalization of 91% of the S1P1 receptor. |
In vivo study | BAF312 effectively inhibits rat encephalomyelitis (EAE) by internalizing the S1P 1 receptor, making it insensitive to the exit signal of lymph nodes. BAF312 at a prophylactic or therapeutic dose of 0.3 mg/kg significantly reduced clinical scores in mice. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.936 ml | 9.679 ml | 19.358 ml |
5 mM | 0.387 ml | 1.936 ml | 3.872 ml |
10 mM | 0.194 ml | 0.968 ml | 1.936 ml |
5 mM | 0.039 ml | 0.194 ml | 0.387 ml |