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生物活性
Fingolimod is a FDA approved drug for Multiple sclerosis treatment. It is a folk medicine emerged from Fungi. Fingolimod was firstly found to be a therapeutic agent in organ transplantation. Then Fingolimod was found to have similar structure with natural sphingosine and interact with S1P1, S1P4, S1P5 and S1P3 receptors as high affinity agonist with EC50 values of 0.3-3.1 nM. It plays the role in MS treatment through receptor-mediated actions both on the immune system and in the CNS. Fingolimod can prevent normal lymphocyte egress and reduce the infiltration of autoaggressive lymphocytes into the CNS.
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体外研究
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体内研究
Saline
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激酶实验
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细胞实验
10 nM
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动物实验
5 mg/kg/day, 10 mg/kg/day 腹腔注射
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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）
|  动物 A (mg/kg) = 动物 B (mg/kg)×动物 B的Km系数/动物 A的Km系数 |
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例如，已知某工具药用于小鼠的剂量为88 mg/kg , 则用于大鼠的剂量换算方法：将88 mg/kg 乘以小鼠的Km系数（3），再除以大鼠的Km系数（6），得到该药物用于大鼠的等效剂量44 mg/kg。
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参考文献
[1] Rolin J, et al. Cancer Immunol Immunother. 2010, 59(4), 575-586.
[2] Brinkmann, V., et al. 2002. J. Biol. Chem. 277: 21453-21457.
[3] Mandala, S., et al. 2002. Science. 296: 346-349.
分子式
C19H33NO2.HCl |
分子量
343.9 |
CAS号
162359-56-0 |
储存方式
﹣20 ℃冷藏长期储存。冰袋运输 |
溶剂（常温）
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DMSO
70 mg/mL |
Water
70 mg/mL |
Ethanol
70 mg/mL |
体内溶解度
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Clinical Trial Information ( data from http://clinicaltrials.gov )
注：以上所有数据均来自公开文献，并不保证对所有实验均有效，数据仅供参考。
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