中文名称: | 盐酸芬戈莫德 促销 | ||||
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英文名称: | Fingolimod HCl | ||||
别名: | 盐酸芬戈莫德 FTY720 2-amino-2-(4-octylphenethyl)propane-1,3-diol hydrochloride | ||||
CAS No: | 162359-56-0 | 分子式: | C19H33NO2.HCl | 分子量: | 343.93 |
CAS No: | 162359-56-0 | ||||
分子式: | C19H33NO2.HCl | ||||
分子量: | 343.93 | ||||
MDL: | MFCD00939512 |
基本信息
产品编号: |
F70007 |
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产品名称: |
Fingolimod HCl |
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CAS: |
162359-56-0 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式: |
溶于液体 |
-80℃ |
6个月 |
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分子量: |
343.93 |
-20℃ |
1个月 |
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化学名: |
FTY720 2-amino-2-(4-octylphenethyl)propane-1,3-diol hydrochloride |
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Solubility (25°C): |
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体外:
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DMSO |
69mg/mL (200.63mM) |
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Water |
69mg/mL (200.63mM) |
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Ethanol |
69mg/mL (200.63mM) |
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体内(现配现用): |
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<1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 |
制备储备液
浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
1mM |
2.9078mL |
14.5391mL |
29.0782mL |
5mM |
0.5816mL |
2.9078mL |
5.8156mL |
10mM |
0.2908mL |
1.4539mL |
2.9078mL |
50mM |
0.0582mL |
0.2908mL |
0.5816mL |
生物活性
产品描述 |
一种S1P拮抗剂,在K562和NK细胞中IC50为0.33nM。 |
靶点 |
S1P receptor |
0.033nM |
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体外研究 |
Fingolimod hydrochloride (FTY720) is a S1P antagonist with an IC50 of 0.033nM in K562 and NK cells.The monocyte-derived immature dendritic cells (iDCs) are pretreated with various concentrations of S1P for various periods of time prior to their incubation with NK cells.Four hours incubation of autologous or allogeneic iDCs with 0.2-20μM of S1P significantly protectes these cells from NK cell lysis.The IC50 values of S1P are calculated at 160nM for autologous iDCs,and 34nM for allogeneic iDCs.Next,the inhibitory effect of S1P is revered by various concentrations of Fingolimod hydrochloride (FTY720) or SEW2871,with an IC50 effect of 173 or 15nM,respectively.The immunomodulator Fingolimod hydrochloride (FTY720) is a structural analogue of S1P and acts in its phosphorylated isoform as an unselective agonist on S1P1 and S1P3-5 and a selective functional antagonist on S1P1.FTY720 enhances serum S1P levels by inhibiting S1P lyase activity.The number of Iba1+cells in ipsilateral CA3 is counted, and the corresponding graph shows a significantly lower number of Iba1+cells in CA3 of the Kainic acid (KA)+FTY720 group than in CA3 of KA group. |
体内研究 |
Administration of the immunomodulator Fingolimod hydrochloride (0.1mg/kg i.v.) increases serum S1P,improves impaired systolic contractility and activates the PI3K-pathway in the heart.Administration of Fingolimod hydrochloride (FTY720) causes a significant rise in serum S1P levels in both sham-operated animals and animals challenged with LPS/PepG (P<0.0001)[.FTY720 attenuates microgliosis,modulates the microglia inflammatory phenotype by reducing LPS-mediated activation of p38 MAPK signalling pathway.Thus,FTY720 shares both direct neuroprotective and anti-inflammatory properties that can contribute to overall neuroprotection.In particular,the potential of FTY720 to switch microglia phenotype from a detrimental to a protective one represents a therapeutic mechanism for attenuating acute and chronic CNS damage. |
推荐实验方法(仅供参考)
细胞实验: |
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Immature dendritic cells (DCs) are left intact or are incubated with 2 μM S1P, 10 nM Fingolimod hydrochloride, 10 nM SEW2871 or the combinations of S1P with these drugs for 4 h. As a control 1 μg/mL LPS is used. The cells are washed and incubated in a 96-well plate (v-bottom, 2×105 cells per well),washed again and resuspended in PBS buffer containing 0.1% sodium azide.They are labeled with 1μg/mL FITC-conjugated mouse anti-human CD80,1μg/mL FITC-conjugated mouse anti-human CD83,1μg/mL FITC-conjugated mouse anti-human CD86,1μg/mL FITC-conjugated mouse anti-human HLAclass I,1μg/mL FITC-conjugated mouse anti-human HLA-DR,1μg/mL FITC-conjugated mouse anti-human HLA-E,or 1μg/mL FITC-conjugated mouse IgG as a control.The cells are washed twice,and examined in the flow cytometer.Markers are set according to the isotype control FITC-conjugated mouse IgG. |
动物实验: |
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Mice This study is carried out on 2-month-old male C57BL/6J mice or sphingosine kinase-2 deficient (SPHK-2-/-) mice weighing 25-30g,receiving a standard diet and water ad libitum.C57BL/6J wild-type or SPHK-2-/-mice receives i.p.-injections of LPS (9mg/kg)/PepG (1mg/kg) or its vehicle (0.9% saline).Sham mice are not subjected to LPS/PepG,but are otherwise treated in the same way.At 1h after LPS/PepG challenge,mice are treated with Fingolimod hydrochloride (0.1mg/kg i.v.) or its vehicle (10% DMSO).To elucidate the role of different S1P receptors in the observed effects of Fingolimod hydrochloride,mice receive (45 min after LPS/PepG and 15 min prior to Fingolimod hydrochloride) the selective PI3K inhibitor LY294002 (0.3mg/kg i.v.) or the selective S1P2 receptor antagonist JTE 013 (1mg/kg i.v.) or (1 h after LPS/PepG) the selective S1P1 receptor agonist SEW2871 (1mg/kg i.v.) or vehicle (10% DMSO). Rat The Sprague-Dawley rats (200 to 250g) are used. Fingolimod hydrochloride is applied icv (1μg/2μL),together with Kainic acid (KA),plus intraperitoneally (ip;1mg/kg) 24h before,and daily,until sacrifice 3 days aftericv.Rats are evaluated for neurological score,neuronal loss in CA3 hippocampal region and activation of microglia at the lesion site. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液,使用的计算公式为:
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为:C1V1 = C2V2 ( 输入 输出 )