Fingolimod
货号：
11975-50mg 基本售价：
4928.0 元 规格：
50 mg
产品信息
概述| 货号 | 11975-50mg |
| 描述 | Sphingosine 1-phosphate (S1P) is an extracellular lipid mediator whose major effects are mediated through four of the S1P receptors (S1P1, S1P3, S1P4, and S1P5). S1P1 plays a key role in the immune system, regulating lymphocyte egress from lymphoid tissues into the circulation. S1P receptors have been shown to influence cell proliferation, morphology, and migration and are also expressed on a wide range of cells that are involved in many biological processes relevant to multiple sclerosis (MS).1 Fingolimod (FTY720 (free base) of Item No. 10006292) is a derivative of the fungal metabolite myriocin, a structural analog of sphingosine. In vivo, fingolimod is phosphorylated to form fingolimod-phosphate, which resembles naturally occurring S1P.2 Fingolimod-phosphate functions as an agonist at S1P1, S1P4, and S1P5 receptors (EC50 values of ~0.3-0.6 nM in vitro) and at 10-fold higher concentrations at S1P3 receptors (EC50 values of ~3 nM) but has no activity at S1P2receptors.3 Fingolimod is a first-in-class orally bioavailable compound that has shown efficacy in advanced clinical trials for the treatment of MS through receptor-mediated actions both on the immune system and in the central nervous system.2 At 0.1-0.3 mg/kg it was shown to be highly effective at inhibiting the development of experimental autoimmune encephalomyelitis, an animal model of human MS, whereas concentrations 10-100-fold higher or in combination with classic immunosuppressants were required to prolong organ graft survival in animals.3 |
| 别名 | FTY720 (free base); |
性能| 供应商 | Cayman |
| 应用文献 |
1.Huwiler, A.,Kolter, T.,Pfeilschifter, J., et al. Physiology and pathophysiology of sphingolipid metabolism and signaling. Biochimica et Biophysica Acta 1485, 63-99 (2000).
2.Chun, J., and Hartung, H.P. Mechanism of action of oral fingolimod (FTY720) in multiple sclerosis. Clin.Neuropharmacol. 33(2), 91-101 (2010).
3.Brinkmann, V.,Billich, A.,Baumruker, T., et al. Fingolimod (FTY720): Discovery and development of an oral drug to treat multiple sclerosis. Nature Reviews.Drug Discovery 9(11), 883-897 (2010).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 307.5 |
| 分子式 | C19H33NO2 |
| CAS号 | 162359-55-9 |
| 稳定性 | ≥ 2 years |
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