生物活性
BAF312 (Siponimod) is a next-generation S1P receptor modulator, selective for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, exhibits >1000-fold selectivity over S1P2, S1P3 and S1P4 receptors.
化学数据
| 分子量 | 516.6 |
| 分子式 | C29H35F3N2O3 |
| CAS号 | 1230487-00-9 |
| 纯度 | >99% |
| 溶解性（25°C） | DMSO ≥ 30 mg/mL |
| 储存和运输条件 | 固体粉末： -20°C 冷藏长期储存
常温运输及临时存放 |
实验操作 来自于公开的文献，仅供相同实验参考（如实验材料、目的不同，请参考其他文献）
| 细胞实验 |
|---|
| 细胞系 | CHO cells |
| 方法 | Agonist-mediated internalization of S1P1 receptors in CHO cells analysed by flow cytometry
Myc-tag hS1P1 cells were incubated for 1 h with agonist at 37°C in standard culture medium followed by a PBS wash. An aliquot was kept on ice for 3 h, while another aliquot was left for 3 (or 12) h in culture medium (no agonist) at 37°C. The cells were then incubated either with 4 μg·mL–1 monoclonal mouse anti C-myc IgG1 (Roche Applied Science, Mannheim, Germany) antibody or with isotype control mouse IgG1 (Pharmingen, BD Biosciences, Basel, Switzerland) for 60 min at 4°C, followed by an incubation with 1 μg·mL–1 of Alexa488-labelled goat anti-mouse secondary conjugates (Molecular Probes, Juro Supply, Luzern, Switzerland). The cells were subjected to flow cytometry measurements using 10000 viable cells per sample. |
| 浓度 | 1 μM |
| 处理时间 | 1h |
| 动物实验 |
|---|
| 动物模型 | EAE model in the DA rat |
| 配制 | 1% aqueous carboxy-methylcellulose (C-4888, Sigma Chemical Co, St Louis, MO) |
| 剂量 | 0.03, 0.3 and 3 mg/kg once daily |
| 给药处理 | oral gavage |
不同实验动物依据体表面积的等效剂量转换表（数据来源于FDA指南）
| 小鼠 | 大鼠 | 兔 | 豚鼠 | 仓鼠 | 狗 |
| 重量 (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| 体表面积 (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km系数 | 3 | 6 | 12 | 8 | 5 | 20 |
| 动物 A (mg/kg) = 动物 B (mg/kg) × | 动物 B的Km系数 |
| 动物 A的Km系数 |
例如，依据体表面积折算法，将化合物用于小鼠的剂量20 mg/kg 换算成大鼠的剂量，需要将20 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。
储备液配制
以下数据基于产品分子量，对于特殊产品，请参照COA中的储备液配制条件和说明进行操作。
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9357 mL | 9.6787 mL | 19.3573 mL |
| 5 mM | 0.3871 mL | 1.9357 mL | 3.8715 mL |
| 10 mM | 0.1936 mL | 0.9679 mL | 1.9357 mL |
