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

Fingolimod hydrochloride  (Synonyms: FTY720)

Cat. No.: HY-12005 Purity: 99.95%
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Fingolimod (FTY720) hydrochloride is a sphingosine 1-phosphate (S1P) antagonist with IC50 of 0.033 nM in K562 and NK cells. Fingolimod hydrochloride is also a pak1 activator and immunosuppressant.

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

Fingolimod hydrochloride Chemical Structure

Fingolimod hydrochloride Chemical Structure

CAS No. : 162359-56-0

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 67 In-stock
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10 mM * 1 mL in DMSO USD 67 In-stock
Solid
100 mg USD 61 In-stock
200 mg USD 94 In-stock
500 mg USD 165 In-stock
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Based on 43 publication(s) in Google Scholar

Other Forms of Fingolimod hydrochloride:

Fingolimod hydrochloride Related Antibodies

Top Publications Citing Use of Products

40 Publications Citing Use of MCE Fingolimod hydrochloride

WB
IHC

    Fingolimod hydrochloride 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 hydrochloride 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 hydrochloride 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.

    View All LPL Receptor Isoform Specific Products:

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    LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

    View All PAK Isoform Specific Products:

    View All Isoforms
    PAK1 PAK2 PAK3 PAK4 PAK5 PAK6

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Fingolimod (FTY720) hydrochloride is a sphingosine 1-phosphate (S1P) antagonist with IC50 of 0.033 nM in K562 and NK cells. Fingolimod hydrochloride is also a pak1 activator and immunosuppressant[1][2][3][4].

    IC50 & Target[1]

    S1P

    0.033 nM (IC50, in K562 and NK cells)

    PAK1

     

    In Vitro

    Fingolimod hydrochloride (FTY720) is a S1P antagonist with an IC50 of 0.033 nM in K562 and NK cells[1].
    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 hydrochloride (FTY720) or SEW2871, with an IC50 effect of 173 or 15 nM, respectively[1].
    FTY720 enhances serum S1P levels by inhibiting S1P lyase activity[2].
    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[3].

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

    Fingolimod hydrochloride Related Antibodies
    In Vivo

    Administration of the immunomodulator Fingolimod hydrochloride (0.1 mg/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)[2].
    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[3].

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

    343.93

    Formula

    C19H34ClNO2
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    OCC(N)(CO)CCC1=CC=C(C=C1)CCCCCCCC.[H]Cl
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

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

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (290.76 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Ethanol : 100 mg/mL (290.76 mM; Need ultrasonic)

    H2O : 50 mg/mL (145.38 mM; Need ultrasonic)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
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    Concentration
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    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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    Volume (final)

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    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% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.08 mg/mL (6.05 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.08 mg/mL (6.05 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    Purity & Documentation

    Purity: 99.95%

    SDS (393 KB)

    COA (241 KB) LCMS (262 KB)

    Handling Instructions (2659 KB)
    References
    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.
    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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 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

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Fingolimod hydrochloride Related Classifications

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    • 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.

    Keywords:

    Fingolimod162359-56-0FTY720FTY 720FTY-720LPL ReceptorPAKLysophospholipid Receptorp21 activated kinasesInhibitorinhibitorinhibit

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