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  3. Fingolimod

Fingolimod  (Synonyms: FTY720 free base)

Cat. No.: HY-11063 Purity: 99.54%
COA Handling Instructions

Fingolimod (FTY720 free base) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant.

For research use only. We do not sell to patients.

Fingolimod Chemical Structure

Fingolimod Chemical Structure

CAS No. : 162359-55-9

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Customer Review

Based on 30 publication(s) in Google Scholar

Other Forms of Fingolimod:

Top Publications Citing Use of Products

    Fingolimod purchased from MedChemExpress. 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 purchased from MedChemExpress. 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 purchased from MedChemExpress. 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.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Fingolimod (FTY720 free base) is a sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant[1].

    IC50 & Target[1]

    S1P

    0.033 nM (IC50, in K562 and NK cells)

    PAK1

     

    In Vitro

    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 0.2-20 μM of S1P significantly protectes these cells from NK cell lysis. The IC50 values of S1P are calculated at 160 nM for autologous iDCs, and 34 nM for allogeneic iDCs. Next, the inhibitory effect of S1P is revered by various concentrations of Fingolimod or SEW2871, with an IC50 effect of 173 or 15 nM, respectively[1]. Fingolimod has been reported to reduce LPA synthesis via inhibition of the lysophospholipase autotaxin. Fingolimod treatment correlates with a significant elevation of axonal cAMP, a crucial factor for axonal outgrowth. Additionally, Fingolimod significantly reduces LPA levels in the injured nerve. PF-8380 treatment correlates with improved myelin thickness[2].

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

    In Vivo

    Fingolimod treatment results in significantly increased nerve conduction at 14 days post-crush in wildtype C57BL/6 mice. However, Foxn1-/- mice, which are devoid of T- but not B-lymphocytes, show an improvement of nerve regeneration under fingolimod treatment. Although the mean increase in nerve conduction velocity in both fingolimod-treated and controlFoxn1-/- mice implies a potentially positive role of T-lymphocyte deficiency on nerve regeneration, only fingolimod-treated Foxn1-/- mice show a significant improvement compared to C57BL/6 controls and performed better in the functional analysis[2]. Treatment of the animals with Fingolimod for 28 d results in a clear reduction in the binding of 18F-GE180 when compare with vehicle-treated animals and evaluated by ex vivo autoradiography. Quantification of the binding of the radiotracer revealed a significant reduction in the binding potential of 18F-GE180 (P<0.0001) after treatment with Fingolimod[3].

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

    Clinical Trial
    Molecular Weight

    307.47

    Formula

    C19H33NO2

    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    OCC(CCC1=CC=C(CCCCCCCC)C=C1)(N)CO

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    Ethanol : 7.69 mg/mL (25.01 mM; Need ultrasonic)

    DMSO : 2 mg/mL (6.50 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.2523 mL 16.2617 mL 32.5235 mL
    5 mM 0.6505 mL 3.2523 mL 6.5047 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

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    Concentration (final)

    C2

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    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% EtOH    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1 mg/mL (3.25 mM); Clear solution

      This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (10.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% EtOH    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 1 mg/mL (3.25 mM); Clear solution

      This protocol yields a clear solution of ≥ 1 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (10.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 99.56%

    References
    Cell Assay
    [1]

    Immature dendritic cells (DCs) are left intact or are incubated with 2 μM S1P, 10 nM Fingolimod, 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]
    Rag1-/- mice(B6.129S7-Rag1tm1Mom/J), Foxn1-/- mice (B6.Cg/NTac-Foxn1nu) mice, and control C57BL/6 mice are used. Mice receive non-phosphorylated Fingolimod via intraperitoneal injection at a concentration of 1 mg/kg once daily over the course of 16 days, starting 2 days before crush until 14 days post-crush. PF-8380 is dissolved in DMSO and administered at a concentration of 10 mg/kg via intraperitoneal injection once daily, as well starting 2 days before until 14 days post-crush. Controls receive an equal volume of solvent.
    Rats[3]
    Male Lewis rats (50-100 g, n=18) are used. After the peripheral activation of the lesion, the DTH EAE lesions are allowed to develop until day 127 to generate large chronic lesions and the animals are then treated for 28 d with either Fingolimod (n=7) or vehicle (n=7). The Fingolimod treatment is given daily (0.3 mg/kg in 0.5 mL of water). The control group is given water (0.5 mL) as a vehicle control. The animals are dosed via oral gavage to ensure accurate dosing. In this model, the acute inflammation subsides after day 20 of activation of the lesion, and the BBB damage subsides. Thus, at day 127 the lesion clearly represents a well-developed chronic MS lesion. PET imaging is performed immediately before initiation of treatment and at the end of the treatment period.

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

    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO / Ethanol 1 mM 3.2523 mL 16.2617 mL 32.5235 mL 81.3087 mL
    5 mM 0.6505 mL 3.2523 mL 6.5047 mL 16.2617 mL
    Ethanol 10 mM 0.3252 mL 1.6262 mL 3.2523 mL 8.1309 mL
    15 mM 0.2168 mL 1.0841 mL 2.1682 mL 5.4206 mL
    20 mM 0.1626 mL 0.8131 mL 1.6262 mL 4.0654 mL
    25 mM 0.1301 mL 0.6505 mL 1.3009 mL 3.2523 mL
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    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.

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    Product Name:
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