1. GPCR/G Protein Cytoskeleton Cell Cycle/DNA Damage
  2. LPL Receptor PAK
  3. Fingolimod hydrochloride

Fingolimod hydrochloride  (Synonyms: 盐酸芬戈莫德; FTY720)

目录号: HY-12005 纯度: 99.95%
COA 产品使用指南

Fingolimod hydrochloride (FTY720) 是鞘氨醇的类似物,是一种有效的 1-磷酸鞘氨醇 (S1P) 受体调节剂。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。Fingolimod hydrochloride 还是一种 pak1 激活剂。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

Fingolimod hydrochloride Chemical Structure

Fingolimod hydrochloride Chemical Structure

CAS No. : 162359-56-0

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥610
In-stock
100 mg ¥550
In-stock
200 mg ¥850
In-stock
500 mg ¥1500
In-stock
1 g ¥1900
In-stock
5 g ¥7500
In-stock
10 g   询价  
50 g   询价  

* Please select Quantity before adding items.

Customer Review

Other Forms of Fingolimod hydrochloride:

注册 MCE会员完成审核
即刻享有 积分商城 300 专属积分

Top Publications Citing Use of Products

    Fingolimod hydrochloride purchased from MCE. Usage Cited in: Cancer Lett. 2018 Aug 16;436:75-86.  [Abstract]

    Immunoblotsof sphingolipid metabolizing enzymes SPHK1, SPHK2, acid ceramidase (AC), and glucosylceramide synthase (GCS) in A2780. cp20, SKOV3. TR, HeyA8. MDR, COV362, and CAOV3 cell lines exposed to the indicated concentrations of FTY720 (FTY) or DMSO (VC) for 24 h.

    Fingolimod hydrochloride purchased from MCE. Usage Cited in: Cancer Lett. 2018 Aug 16;436:75-86.  [Abstract]

    FTY720+ICI 47699 and FTY720+NSC 241240 increase apoptosis marker, cleaved caspase 3 in a PDX model of EOC. IHC of tumor sections is used to detect the apoptosis marker cleaved caspase 3 and the cell cycle inhibitor p21.

    Fingolimod hydrochloride purchased from MCE. Usage Cited in: Breast Cancer Res. 2017 Aug 4;19(1):90.  [Abstract]

    The effect of ZD1839-FTY720 treatment on CD44 expression in TNBC cell lines. HCC1806, Hs578T, and MDA-MB-468 TNBC cell lines at ~40% confluence in 12-well plates are exposed for 24 h to ZD1839 (Gef: 0.1 to 10 μM), with or without the addition of 1.5 μM FTY720.

    查看 LPL Receptor 亚型特异性产品:

    查看 PAK 亚型特异性产品:

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Fingolimod hydrochloride (FTY720), an analog of sphingosine, is a potent sphingosine 1-phosphate (S1P) receptors modulator. Fingolimod hydrochloride is phosphorylated by sphingosine kinases, particularly by SK2, and then binds S1PR1, 3, 4, and 5. Fingolimod hydrochloride induces the internalization of S1P1, and consequently, inhibits S1P activity. Fingolimod hydrochloride also is a pak1 activator[1][4].

    IC50 & Target[1]

    S1P

    0.033 nM (IC50, in K562 and NK cells)

    PAK1

     

    体外研究
    (In Vitro)

    Fingolimod hydrochloride (FTY720) 是一种 S1P 拮抗剂,在 K562 和 NK 细胞中的 IC50 为 0.033 nM[1]
    单核细胞来源的未成熟树突状细胞 (iDC) 在与 NK 细胞孵育之前,先用不同浓度的 S1P 预处理不同的时间段。将自体或同种异体 iDC 与 0.2 -20 μM S1P 孵育 4 小时可显著保护这些细胞免受 NK 细胞裂解。S1P 的 IC50 值计算为自体 iDC 为 160 nM,同种异体 iDC 为 34 nM。接下来,S1P 的抑制作用被各种浓度的盐酸 Fingolimod hydrochloride (FTY720) 或 SEW2871 所证实,其 IC50 效应分别为 173 或 15 nM[1]。免疫调节剂 Fingolimod hydrochloride (FTY720) 是 S1P 的结构类似物,在其磷酸化亚型中作为 S1P1 和 S1P3-5 的非选择性激动剂和选择性功能拮抗剂起作用在 S1P1 上。
    FTY720 通过抑制 S1P 裂解酶活性提高血清 S1P 水平[2]
    统计同侧 CA3 区 Iba1+ 细胞数,对应图显示红藻氨酸 CA3 区 Iba1+ 细胞数显著减少 (KA) +FTY720 组优于 KA 组 CA3[3]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    给予免疫调节剂 Fingolimod hydrochloride (0.1 mg/kg iv) 可增加血清 S1P,改善受损的收缩收缩力并激活心脏中的 PI3K 通路。施用盐酸 Fingolimod hydrochloride (FTY720) 会导致假手术动物和接受 LPS/PepG 攻击的动物的血清 S1P 水平显著升高 (P<0.0001)[2]。FTY720 减弱小胶质细胞增生,通过减少 LPS 介导的 p38 MAPK 信号通路激活来调节小胶质细胞炎症表型。因此,FTY720 具有直接的神经保护和抗炎特性,可促进整体神经保护。特别是,FTY720 将小胶质细胞表型从有害表型转变为保护表型的潜力代表了一种减轻急性和慢性 CNS 损伤的处理机制[3]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    分子量

    343.93

    Formula

    C19H34ClNO2

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    盐酸芬戈莫德;芬戈莫德盐酸盐

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : ≥ 100 mg/mL (290.76 mM; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    Ethanol 中的溶解度 : 100 mg/mL (290.76 mM; 超声助溶)

    H2O 中的溶解度 : 50 mg/mL (145.38 mM; 超声助溶)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.9076 mL 14.5378 mL 29.0757 mL
    5 mM 0.5815 mL 2.9076 mL 5.8151 mL
    查看完整储备液配制表

    * 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
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    In Vivo:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (6.05 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (6.05 mM); 澄清溶液

      此方案可获得 ≥ 2.08 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      20% SBE-β-CD in Saline 的配制(4°C,储存一周):2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
    纯度 & 产品资料

    纯度: 99.95%

    参考文献
    Cell Assay
    [1]

    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 1 μg/mL FITC-conjugated mouse anti-human CD80, 1 μg/mL FITC-conjugated mouse anti-human CD83, 1 μg/mL FITC-conjugated mouse anti-human CD86, 1 μg/mL FITC-conjugated mouse anti-human HLA-class I, 1 μg/mL FITC-conjugated mouse anti-human HLA-DR, 1 μg/mL FITC-conjugated mouse anti-human HLA-E, or 1 μg/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[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2][3]

    Mice[2]
    This study is 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 receives i.p.-injections of LPS (9 mg/kg)/PepG (1 mg/kg) or its vehicle (0.9% saline). Sham mice are not subjected to LPS/PepG, but are otherwise treated in the same way. At 1 h after LPS/PepG challenge, mice are treated with Fingolimod hydrochloride (0.1 mg/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 (0.3 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).
    Rat[3]
    The Sprague-Dawley rats (200 to 250 g) are used. Fingolimod hydrochloride is applied icv (1 μg/2 μL), together with Kainic acid (KA), plus intraperitoneally (ip; 1 mg/kg) 24 h 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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    Fingolimod hydrochloride 相关分类

    完整储备液配制表

    * 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
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO / Ethanol 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
    15 mM 0.1938 mL 0.9692 mL 1.9384 mL 4.8459 mL
    20 mM 0.1454 mL 0.7269 mL 1.4538 mL 3.6345 mL
    25 mM 0.1163 mL 0.5815 mL 1.1630 mL 2.9076 mL
    30 mM 0.0969 mL 0.4846 mL 0.9692 mL 2.4230 mL
    40 mM 0.0727 mL 0.3634 mL 0.7269 mL 1.8172 mL
    50 mM 0.0582 mL 0.2908 mL 0.5815 mL 1.4538 mL
    60 mM 0.0485 mL 0.2423 mL 0.4846 mL 1.2115 mL
    80 mM 0.0363 mL 0.1817 mL 0.3634 mL 0.9086 mL
    100 mM 0.0291 mL 0.1454 mL 0.2908 mL 0.7269 mL

    * 备注:如您选择水作为储备液,请稀释至工作液后,再用 0.22 μm 的滤膜过滤除菌后使用。

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    您最近查看的产品:

    Your information is safe with us. * Required Fields.

       产品名称:

     

    * 需求量:

    * 客户姓名:

     

    * Email:

    * 电话:

     

    * 公司或机构名称:

       留言给我们:

    Bulk Inquiry

    Inquiry Information

    产品名称:
    Fingolimod hydrochloride
    目录号:
    HY-12005
    需求量: