生物活性
Fingolimod (FTY720) HCl是一种1-磷酸-神经鞘氨醇S1P受体拮抗剂，IC50为0.33 nM。S1P 作用于K562细胞，抑制NK细胞裂解。多种浓度 FTY720可逆转S1P的抑制作用，IC50为173 nM。此外, 10 nM FTY720 单独温育时，对共刺激分子的表达没有任何影响。
化学数据
| 分子量 | 343.9 |
| 分子式 | C19H33NO2.HCl |
| CAS号 | 162359-56-0 |
| 纯度 | 99.46% |
| 溶解性（25°C） | DMSO 60 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 | MCF-7 cells |
| 方法 | In Vitro Proliferation Assay Cells were seeded onto 96- well plates at the densities of 3000 cells/well. After 24 h of pre-cultivation, appropriate concentrations of the samples were added and the cells were cultured for 2 d. The relative growth ratio was determined by WST-1 assay using a cell counting kit (Dojindo Laboratories, Kumamoto, Japan) according to the manufacturer’s instructions. The IC50 value was determined from the dose response curve. At least three independent experiments were performed. The proliferation assay that tested the effects of DMS was performed using identical methods. Compounds with or without DMS were added to the wells and the plates were incubated for 78 h at 37 °C in a humidified atmosphere containing 5% CO2 before
the WST-1 assay was conducted. |
| 浓度 | 0~100μM |
| 处理时间 | 2 days |
| 动物实验 |
|---|
| 动物模型 | Six-weekold female NOD.Cg-Prkdcscid Il2rgtm1Wjl/SzJ (NSG) mice with Mino cells |
| 配制 | not mentioned |
| 剂量 | 10 mg/kg daily for 10 days |
| 给药处理 | intraperitoneal injections |
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 | 2.9078 mL | 14.5391 mL | 29.0782 mL |
| 5 mM | 0.5816 mL | 2.9078 mL | 5.8156 mL |
| 10 mM | 0.2908 mL | 1.4539 mL | 2.9078 mL |
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