Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Fingolimod hydrochloride (FTY720) 是一种新型免疫调节剂,是一种 1-磷酸鞘氨醇(S1P) 拮抗剂,作用于 K562 和 NK 细胞,IC50为 0.033 nM。它诱导 S1P1 的内化,从而抑制 S1P 活性。它被鞘氨醇激酶磷酸化,尤其是被 SK2 磷酸化,从而可与 S1PR1、3、4 和 5 结合
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
100 mg | ¥ 457 | 现货 | ||
200 mg | ¥ 697 | 现货 | ||
500 mg | ¥ 1,258 | 现货 | ||
1 g | ¥ 1,587 | 待询 | ||
1 mL * 10 mM (in DMSO) | ¥ 497 | 现货 |
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 | The cultures of K562 and NK cells were incubated in the presence of 2 μM S1P and increasing concentrations of Fingolimod (FTY720). Addition of various concentrations of FTY720 blocked the inhibitory effect of S1P with an IC50 value calculated at 0.033 nM. The combination of S1P with FTY720 did not affect the expression of these molecules on the surface of iDCs. In addition, 10 nM FTY720 when incubated alone exerted no effect on the expression of co-stimulatory molecules [1]. FTY720 was able to reduce excitotoxic neuronal death in vitro. FTY720 negatively modulates p38 MAPK in LPS-activated microglia, whereas it had no effect on JNK1/2 activation [2]. |
体内活性 | Administration of the immunomodulator FTY720 increased serum S1P, improved impaired systolic contractility and activated the PI3K-pathway in the heart. Cardioprotective effects of FTY720 were abolished following administration of an S1P receptor 2 (S1P2) antagonist or a PI3K inhibitor. Sphingosine kinase-2 deficient mice had higher endogenous S1P levels and the LPS/PepG-induced impaired systolic contractility was attenuated in comparison with wild-type mice [3]. Using human ALL xenografts in NOD/SCIDγc(-/-) mice, three Ph(+) human ALL xenografts responded to FTY720 with an 80 ± 12% reduction in overall disease when treatment was commenced early. In contrast, treatment of mice with FTY720 did not result in reduced leukemia compared to controls using four separate human Ph(-) ALL xenografts [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 | Fingolimod (FTY720) HCl, FTY720, 盐酸芬戈莫德 |
分子量 | 343.93 |
分子式 | C19H34ClNO2 |
CAS No. | 162359-56-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: 34.4 mg/mL (100 mM)
DMSO: 34.4 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
H2O / DMSO | 1 mM | 2.9076 mL | 14.5378 mL | 29.0757 mL | 72.6892 mL |
5 mM | 0.5815 mL | 2.9076 mL | 5.8151 mL | 14.5378 mL | |
10 mM | 0.2908 mL | 1.4538 mL | 2.9076 mL | 7.2689 mL | |
20 mM | 0.1454 mL | 0.7269 mL | 1.4538 mL | 3.6345 mL | |
50 mM | 0.0582 mL | 0.2908 mL | 0.5815 mL | 1.4538 mL | |
100 mM | 0.0291 mL | 0.1454 mL | 0.2908 mL | 0.7269 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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