规格

价格

库存

数量

10 mg

¥ 156

现货

25 mg

¥ 229

现货

50 mg

¥ 319

现货

100 mg

¥ 457

现货

500 mg

¥ 1,250

现货

1 mL x 10 mM (in DMSO)

¥ 497

现货

生物活性

产品描述	Fingolimod hydrochloride (FTY720) , a novel immune modulator, is a sphingosine 1-phosphate (S1P) antagonist (IC50: 0.033 nM in K562 and NK cells).
靶点活性	S1P:0.033 nM (K562 and NK cells)
体外活性	K562细胞和NK细胞的培养物在2μM S1P和递增浓度的Fingolimod (FTY720)存在下孵育。FTY720不同浓度的添加阻断了S1P的抑制效应，其IC50值计算为0.033 nM。S1P与FTY720的组合未影响iDCs表面这些分子的表达。此外，单独孵育10 nM FTY720对共刺激分子的表达无影响[1]。FTY720能够减少体外的兴奋毒性神经元死亡。FTY720在LPS激活的小胶质细胞中负向调节p38 MAPK，而对JNK1/2激活无影响[2]。
体内活性	免疫调节剂Fingolimod的给药增加了血清S1P水平，改善了受损的心脏收缩功能，并激活了心脏中的PI3K途径。当使用S1P受体2（S1P2）拮抗剂或PI3K抑制剂后，Fingolimod的心脏保护效果被消除。缺乏鞘氨醇激酶-2的小鼠具有较高的内源性S1P水平，并且与野生型小鼠相比，LPS/PepG诱导的受损心脏收缩功能得到了减轻[3]。在NOD/SCIDγc(-/-)小鼠中使用人类ALL异种移植物，三种Ph(+)人类ALL异种移植物对Fingolimod的反应显示出在早期治疗开始时疾病总体减少了80±12%。相比之下，使用四种不同的人类Ph(-) ALL异种移植物对Fingolimod的治疗并未能减少白血病，与对照组相比没有差异[4]。
细胞实验	DCs or NK cells were incubated at a cell concentration of 1 × 10^6 cells/ml with either media or with 2 μM S1P, 10 nM SEW2871, 10 nM FTY720 or their combinations. DCs were also incubated with 1 μg/ml LPS. After 24 h incubation, the cells were harvested and the cell suspensions were centrifuged at 1,000 × g for 10 min before the supernatants were collected. Detection of the levels of various cytokines and chemokines was carried utilizing the Multi-Analyte ELISArray Kit as described by the manufacturers' user manual [1].
动物实验	This study was carried out on 2-month-old male C57BL/6J mice or sphingosine kinase-2 deficient (SPHK-2?/?) mice weighing 25–30?g, receiving a standard diet and water ad libitum. C57BL/6J wild-type or SPHK-2?/? mice received i.p.-injections of LPS (9?mg/kg)/PepG (1?mg/kg) or its vehicle (0.9% saline). Sham mice were not subjected to LPS/PepG but were otherwise treated in the same way. At 1?h after LPS/PepG challenge, mice were treated with FTY720 (0.1?mg/kg i.v.) or its vehicle (10% DMSO). To elucidate the role of different S1P receptors in the observed effects of FTY720, mice received (45?min after LPS/PepG and 15?min prior to FTY720) the selective phosphatidylinositol 3 (PI3)-kinase inhibitor LY294002 (0.3?mg/kg i.v.) or the selective S1P2 receptor antagonist JTE 013 (1?mg/kg i.v.) or (1?h after LPS/PepG) the selective S1P1 receptor agonist SEW2871 (1?mg/kg i.v.) or vehicle (10% DMSO) [3].
别名	盐酸芬戈莫德, FTY720 HCl, Fingolimod (FTY720) HCl

化学信息

分子量	343.93
分子式	C₁₉H₃₄ClNO₂
CAS No.	162359-56-0
Smiles	Cl.CCCCCCCCc1ccc(CCC(N)(CO)CO)cc1
密度	1.016g/cm3

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

实际储存温度请以COA为准

溶解度信息

H2O: 34.4 mg/mL (100.02 mM), Sonication is recommended.

DMSO: 102 mg/mL (296.57 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.82 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

H2O/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.9076 mL	14.5378 mL	29.0757 mL	145.3784 mL
5 mM	0.5815 mL	2.9076 mL	5.8151 mL	29.0757 mL
10 mM	0.2908 mL	1.4538 mL	2.9076 mL	14.5378 mL
20 mM	0.1454 mL	0.7269 mL	1.4538 mL	7.2689 mL
50 mM	0.0582 mL	0.2908 mL	0.5815 mL	2.9076 mL
100 mM	0.0291 mL	0.1454 mL	0.2908 mL	1.4538 mL

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

Fingolimod hydrochloride

Fingolimod hydrochloride

产品介绍

引用文献

计算器

体内实验配液计算器

剂量转换

关键词

Fingolimod hydrochloride

Fingolimod hydrochloride