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Fingolimod (FTY720)

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Catalog No.
A8548
S1P受体激动剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 600.00
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100mg
¥ 530.00
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200mg
¥ 880.00
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1g
¥ 2,380.00
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Background

Fingolimod is a mechanistically novel, orally bioavailable therapy for multiple sclerosis (MS) [1].

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 [1, 2].

References:
[1] Chun J, Brinkmann V. A mechanistically novel, first oral therapy for multiple sclerosis: the development of fingolimod (FTY720, Gilenya). Discovery medicine, 2011, 12(64): 213.
[2] Chun J, Hartung H P. Mechanism of action of oral fingolimod (FTY720) in multiple sclerosis. Clinical neuropharmacology, 2010, 33(2): 91.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt343.94
Cas No.162359-56-0
FormulaC19H34ClNO2
SynonymsGilenia; FTY 720; FTY-720
Solubility≥17.2mg/mL in DMSO
Chemical Name2-amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol;hydrochloride
SDFDownload SDF
Canonical SMILESCCCCCCCCC1=CC=C(C=C1)CCC(CO)(CO)N.Cl
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验: [1]

细胞系

MCF-7、MDA-MB-231、Sk-Br-3、HCT-116和SW620细胞

制备方法

该化合物在DMSO中的溶解度大于10 mM,若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。

反应条件

IC50:79.1 μM (MCF-7)、59.9 μM (MDA-MB-231)、72.9 μM (Sk-Br-3)、> 100 μM (HCT-116) 、40.0 μM (SW620),8 hours

实验结果

通过WST-1实验测定fingolimod的IC50值。结果表明,化合物的处理以剂量依赖性方式引起细胞死亡。在测试的所有细胞中,5-7 μM 浓度范围内fingolimod的IC50值相对较低。

动物实验: [2]

动物模型

C57BL/6J小鼠

给药剂量

腹腔注射,0.1 mg/kg体重

实验结果

在注射fingolimod(0.1 mg/kg体重)后30分钟,海马神经元中磷酸化ERK1/2(pERK1/2)的水平显著增加。另外30分钟后,BDNF mRNA水平升高,48小时后海马、皮质和纹状体中的BDNF蛋白水平显著增加。

注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1] Nagaoka Y, Otsuki K, Fujita T, et al. Effects of phosphorylation of immunomodulatory agent FTY720 (fingolimod) on antiproliferative activity against breast and colon cancer cells. Biological and Pharmaceutical Bulletin, 2008, 31(6): 1177-1181.

[2] Deogracias R, Yazdani M, Dekkers M P J, et al. Fingolimod, a sphingosine-1 phosphate receptor modulator, increases BDNF levels and improves symptoms of a mouse model of Rett syndrome. Proceedings of the National Academy of Sciences, 2012, 109(35): 14230-14235.

生物活性

描述 Fingolimod是一种机制新颖的和可口服的疗法,用于多发性硬化症(MS)的治疗。
靶点 S1P1 S1P3 S1P4 S1P5    
IC50            

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