FTY720 hydrochloride 盐酸芬戈莫德

目录号 M1712 所有产品仅供科研使用，严禁用于人或动物的治疗等任何其他用途，不为任何个人提供产品和服务

Fingolimod (FTY720) HCl是一种具有口服活性的1-磷酸鞘氨醇 (S1P) 受体拮抗剂，能与 S1P 受体的所有五种亚型结合，并且对 S1PR1 和 S1PR4 具有更高的亲和力。此外，Fingolimod还能抑制T细胞的迁移，从而减少自身免疫反应，可用于多发性硬化症（MS）的相关研究。

别名：Fingolimod hydrochloride

规格	价格	库存状态
Free Sample (0.5-1 mg)	¥ 0	中国库存现货
100mg	¥ 530	中国库存现货
200mg	¥ 800	中国库存现货
500mg	¥ 1400	中国库存现货
1g	¥ 1800	中国库存现货

其他规格数量报价？

质量标准及产品资料

纯度： 99.46%
COA
MSDS
H-NMR
HPLC

产品信息

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。Fingolimod hydrochloride 被鞘氨醇激酶磷酸化，特别是被 SK2 磷酸化，然后可与 S1PR1、3、4 和 5 结合。Fingolimod hydrochloride 诱导 S1P1 的内在化，因此抑制 S1P 的活性。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。

使用AbMole产品发表的文献

Phytomedicine. 2023 Dec 5.

Huangqi-Guizhi-Wuwu Decoction regulates differentiation of CD4+ T cell and prevents against experimental autoimmune encephalomyelitis progression in mice
Am J Chin Med. 2023 Jun 30;44942.

Total Flavonoids of Astragalus Inhibit Activated CD4T Cells and Regulate Differentiation of Th17/Th1/Treg Cells in Experimental Autoimmune Encephalomyelitis Mice by JAK/STAT and NFκ B Signaling Pathways
Signal Transduct Target Ther. 2022 May 17;7(1):159.

Intranasal administration of a recombinant RBD vaccine induces long-term immunity against Omicron-included SARS-CoV-2 variants
Eur J Pharmacol. 2022 Sep 15;931:175185.

Anemoside B4 ameliorates experimental autoimmune encephalomyelitis in mice by modulating inflammatory responses and the gut microbiota
J Nat Prod. 2020 May 20.

Anti-inflammatory Efficacy of Combined Natural Alkaloid Berberine and S1PR Modulator Fingolimod at Low Doses in Ulcerative Colitis Preclinical Models
Pulm Circ. 2020 Feb 10;10(1).

Sphingosine-1-phosphate Receptor-Independent Lung Endothelial Cell Barrier Disruption Induced by FTY720 Regioisomers
Neuropharmacology. 2019 Nov 1;158:107701.

FTY720-Mitoxy reduces toxicity associated with MSA-like α-synuclein and oxidative stress by increasing trophic factor expression and myelin protein in OLN-93 oligodendroglia cell cultures.
Neuropharmacology. 2017 May 1;117:149-157.

FTY720 (Fingolimod) reverses a-synuclein-induced downregulation of brain-derived neurotrophic factor mRNA in OLN-93 oligodendroglial cells
Powder Diffraction. 2015;205-210.

Crystal structure of fingolimod hydrochloride, C19H34ClNO2

产品使用成果展示

	数据来源	Neuropharmacology (2017). Figure 6. FTY720 (AbMole BioScience, Kowloon, Hong Kong, China)
	方法	Immunoblots
	细胞系/动物模型	OLN-93 cells
	浓度	160 nM
	处理时间	12 h
	实验结果	On immunoblots we noted that 12 h of 160 nM FTY720 treatment of OLN-93 cells produced a significant increase in global acetylation of histone 3 (AcH3)

	数据来源	Neuropharmacology (2017). Figure 4. FTY720 (AbMole BioScience, Kowloon, Hong Kong, China)
	方法	qPCR
	细胞系/动物模型	OLN-93 cells
	浓度	160 nM
	处理时间	12 h
	实验结果	Empty vector transfected cells expressed BDNF (Fig. 4A, lane 1) and 12 h treatments with 160 nM FTY720 significantly increased BDNF expression in all stably transfected aSyn OLN-93 cell lines (Fig. 4A, lanes 3, 5 and 7), visualized on agarose gels showing the BDNF amplicons generated by qPCR.

	数据来源	Neuropharmacology (2017). Figure 2. FTY720 (AbMole BioScience, Kowloon, Hong Kong, China)
	方法	qPCR
	细胞系/动物模型	OLN-93 cells
	浓度	160 nM
	处理时间	12 h
	实验结果	Similar to our earlier assessment in neuronal cells (Vargas-Medrano et al., 2014), we found that using 160 nM FTY720 treatment of OLN-93 cells for 12 h significantly increased BDNF expression as measured using qPCR (Fig. 2, dark gray whisker box).

实验参考

体外实验*
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

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

体内实验*
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

*上述方法来自公开文献，仅供相同目的实验参考。如实验目的、材料、方法不同，请参考其他文献。

化学性质

分子量	343.9
分子式	C19H33NO2.HCl
CAS号	162359-56-0
溶解性（25°C）	DMSO > 60 mg/mL Water 50 mg/mL
储存条件	粉末型式 -20°C 3年；4°C 2年溶于溶剂 -80°C 6个月；-20°C 1个月
运输方式	冰袋运输，根据产品的不同，可能会有相应调整。

储备液配制

*下述溶液配置方法仅为基于分子量计算出的理论值。不同产品在配置溶液前，需考虑其在不同溶剂中的溶解度限制。

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

不同实验动物依据体表面积的等效剂量转换表（参考来源于公开文献）

	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
K_m 系数	3	6	12	8	5	20

动物 A (mg/kg) = 动物 B (mg/kg) ×	动物 B的K_m系数
	动物 A的K_m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K_m系数（3），再除以大鼠的K_m系数（6），得到化合物用于大鼠的等效剂量为10 mg/kg。

参考文献

[1] Cipriani R, et al. J Neuroinflammation. FTY720 attenuates excitotoxicity and neuroinflammation.

[2] Gao et al. Pharmacol Biochem Behav. Fingolimod (FTY720) inhibits neuroinflammation and attenuates spontaneous convulsions in lithium-pilocarpine induced status epilepticus in rat model.

[3] Fazekas F. Wien Med Wochenschr. Fingolimod in the treatment algorithm of relapsing remitting multiple sclerosis: a statement of the Central and East European (CEE) MS Expert Group.

[4] Deogracias et al. Proc Natl Acad Sci U S A. Fingolimod, a sphingosine-1 phosphate receptor modulator, increases BDNF levels and improves symptoms of a mouse model of Rett syndrome.

[5] Gasperini et al. Drug Des Devel Ther. Development of oral agent in the treatment of multiple sclerosis: how the first available oral therapy, fingolimod will change therapeutic paradigm approach.

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