1. Immunology/Inflammation
  2. SPHK

Fingolimod hydrochloride (Synonyms: FTY720)

Cat. No.: HY-12005 Purity: 99.76%
Data Sheet SDS Handling Instructions

Fingolimod hydrochloride is a sphingosine 1-phosphate (S1P) antagonist with IC50 of 0.033 nM in K562 and NK cells.

For research use only. We do not sell to patients.
Fingolimod hydrochloride Chemical Structure

Fingolimod hydrochloride Chemical Structure

CAS No. : 162359-56-0

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Other Forms of Fingolimod hydrochloride:

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

    The effect of Gefitinib-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 Gefitinib (Gef: 0.1 to 10 μM), with or without the addition of 1.5 μM FTY720.

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    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Fingolimod hydrochloride is a sphingosine 1-phosphate (S1P) antagonist with IC50 of 0.033 nM in K562 and NK cells.

    IC50 & Target

    IC50: 0.033 nM (S1P, in K562 and NK cells)[1]

    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 hydrochloride (FTY720) or SEW2871, with an IC50 effect of 173 or 15 nM, respectively[1]. 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[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].

    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].

    Clinical Trial
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    References
    Preparing Stock Solutions
    Concentration Volume 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
    10 mM 0.2908 mL 1.4538 mL 2.9076 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [1]

    Fingolimod hydrochloride (FTY720) is dissolved in DMSO and stored, and then diluted with appropriate media before use[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]

    Fingolimod hydrochloride (FTY720) is dissolved in DMSO and diluted with saline (Mice)[2].
    Fingolimod hydrochloride (FTY720) is dissolved in DMSO and diluted in vehicle (saline solution) (Rat)[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
    Molecular Weight

    343.93

    Formula

    C₁₉H₃₄ClNO₂

    CAS No.

    162359-56-0

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    Purity: 99.76%

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    Inquiry Information

    Product Name:
    Fingolimod hydrochloride
    Cat. No.:
    HY-12005
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