1. Immunology/Inflammation
  2. SPHK

Fingolimod hydrochloride (Synonyms: FTY720)

Cat. No.: HY-12005 Purity: 99.57%
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
    NCT Number Sponsor Condition Start Date Phase
    NCT01755871 Heinrich-Heine University, Duesseldorf|Novartis Pharmaceuticals Relapsing Remitting Multiple Sclerosis January 2013 Phase 4
    NCT02061137 University Hospital, Basel, Switzerland|Novartis Rett's Syndrome August 2013 Phase 1|Phase 2
    NCT02956200 Second Affiliated Hospital, School of Medicine, Zhejiang University Stroke|Inflammation November 2016 Phase 2
    NCT02490930 Sidney Kimmel Comprehensive Cancer Center Glioblastoma|Anaplastic Astrocytoma July 2015 Early Phase 1
    NCT01941004 Novartis Pharmaceuticals|Novartis Multiple Sclerosis (Relapsing Remitting) June 2014 Phase 3
    NCT01578330 Novartis Pharmaceuticals|Novartis Multiple Sclerosis|Relapsing-Remitting October 2012 Phase 4
    NCT00355134 Novartis Multiple Sclerosis June 2006 Phase 3
    NCT00662649 Novartis Multiple Sclerosis February 2008 Phase 3
    NCT00670449 Novartis|Mitsubishi Tanabe Pharma Corporation Multiple Sclerosis April 2008 Phase 2
    NCT01420055 Novartis Pharmaceuticals|Novartis Multiple Sclerosis, Relapsing-Remitting August 2011 Phase 4
    NCT02575365 Novartis Pharmaceuticals|Novartis Cognition|Brain Volume Loss February 2016 Phase 4
    NCT01757691 Novartis Pharmaceuticals|Novartis Acute Demylelinating Optic Neuritis August 2013 Phase 2
    NCT01499667 Novartis Pharmaceuticals|Novartis Relapsing Remitting Multiple Sclerosis (RRMS) September 2011 Phase 3
    NCT01498887 Novartis Pharmaceuticals|Novartis Relapsing Remitting Multiple Sclerosis December 21, 2011 Phase 4
    NCT01497262 Novartis Pharmaceuticals|Novartis Multiple Sclerosis February 2012 Phase 3
    NCT02002390 Tianjin Medical University General Hospital Stroke|Vascular Accident|Cerebral Stroke|Ischemic Cerebrovascular Accident|Stroke, Acute October 2012 Phase 2
    NCT01779700 Indiana University Schizophrenia January 2013 Phase 2
    NCT01281657 Novartis Multiple Sclerosis February 2011
    NCT01216072 Novartis Pharmaceuticals|Novartis Relapsing Forms of Multiple Sclerosis August 2010 Phase 4
    NCT01625182 Novartis Pharmaceuticals|Mitsubishi Tanabe Pharma Corporation|Novartis Chronic Inflammatory Demyelinating Polyradiculoneuropathy December 20, 2012 Phase 3
    NCT01633112 Novartis Pharmaceuticals|Novartis Relapsing-remitting Multiple Sclerosis (RRMS) August 9, 2012 Phase 4
    NCT02232061 Novartis Pharmaceuticals|Novartis Multiple Sclerosis September 29, 2014 Phase 4
    NCT02325440 University Hospital Muenster|Novartis Relapsing Remitting Multiple Sclerosis March 2014 Phase 4
    NCT02373098 Novartis Pharmaceuticals|Novartis Relapsing Remitting Multiple Sclerosis March 31, 2015 Phase 4
    NCT02342704 Biogen Relapsing-Remitting Multiple Sclerosis November 30, 2014 Phase 4
    NCT00340834 Novartis Multiple Sclerosis May 2006 Phase 3
    NCT02939079 Isfahan University of Medical Sciences|Shiraz University of Medical Sciences Multiple Sclerosis April 2015 Phase 2|Phase 3
    NCT00289978 Novartis Relapsing-remitting Multiple Sclerosis January 2006 Phase 3
    NCT01310166 Novartis Pharmaceuticals|Novartis Relapsing-remitting Multiple Sclerosis February 2011 Phase 4
    NCT01442194 Novartis Pharmaceuticals|Novartis Multiple Sclerosis August 1, 2011
    NCT01199861 Novartis Relapsing Multiple Sclerosis August 2010 Phase 3
    NCT01892722 Novartis Pharmaceuticals|Novartis Multiple Sclerosis July 2013 Phase 3
    NCT01534182 Novartis Pharmaceuticals|Novartis Relapsing Remitting Multiple Sclerosis January 2012 Phase 4
    NCT01621269 Novartis Pharmaceuticals|Novartis Multiple Sclerosis June 2013 Phase 4
    NCT01333501 Novartis Pharmaceuticals|Novartis Multiple Sclerosis May 2011 Phase 4
    NCT01436643 Novartis Pharmaceuticals|Novartis Depression|Relapsing-remitting Multiple Sclerosis November 2011 Phase 4
    NCT01623596 Novartis Pharmaceuticals|Novartis Relapsing Remitting Multiple Sclerosis June 2012 Phase 4
    NCT01317004 Novartis Pharmaceuticals|Novartis Relapsing Remitting Multiple Sclerosis May 2011 Phase 4
    NCT00731523 Novartis Renal Insufficiency July 2008 Phase 1
    NCT01285479 Novartis Pharmaceuticals|Novartis Multiple Sclerosis October 2011
    NCT02193217 Mitsubishi Tanabe Pharma Corporation Relapsing-remitting Multiple Sclerosis Phase 1
    NCT00099749 Novartis Pharmaceuticals|Novartis Kidney Transplantation November 2003 Phase 2|Phase 3
    NCT01791192 Novartis Pharmaceuticals|Novartis Acute Noninfectious Posterior, Intermediate, or Pan Uveitis November 2013 Phase 2
    NCT00537082 Novartis|Mitsubishi Tanabe Pharma Corporation Multiple Sclerosis September 2007 Phase 2
    NCT00333138 Novartis Multiple Sclerosis May 2003 Phase 2
    NCT00416845 Novartis Healthy October 2006 Phase 1
    NCT00785083 Novartis Asthma September 2008 Phase 2
    NCT01201356 Novartis Pharmaceuticals|Novartis Relapsing Forms of Multiple Sclerosis September 2010 Phase 3
    NCT01127750 Novartis Relapsing Multiple Sclerosis May 2010 Phase 3
    NCT00099736 Novartis Pharmaceuticals|Novartis Kidney Transplantation May 2003 Phase 3
    NCT00099801 Novartis Pharmaceuticals|Novartis Kidney Transplantation January 2005 Phase 3
    NCT00239876 Novartis Pharmaceuticals|Novartis Renal Transplantation May 2005 Phase 3
    NCT00239811 Novartis Pharmaceuticals|Novartis Renal Transplantation April 2004 Phase 3
    NCT00239902 Novartis Pharmaceuticals|Novartis Renal Transplantation May 2002 Phase 2
    NCT00239798 Novartis Pharmaceuticals|Mitsubishi Tanabe Pharma Corporation|Novartis Renal Transplantation November 2004 Phase 2
    NCT00239785 Novartis Pharmaceuticals|Novartis Renal Transplantation April 2003 Phase 3
    NCT00098735 Novartis Pharmaceuticals|Novartis Kidney Transplantation April 2004 Phase 3
    NCT00239863 Novartis Pharmaceuticals|Novartis Renal Transplantation May 2004 Phase 3
    NCT00731692 Novartis Pharmaceuticals|Novartis Primary Progressive Multiple Sclerosis July 28, 2008 Phase 3
    NCT01585298 Novartis Pharmaceuticals|Novartis Multiple Sclerosis June 29, 2012 Phase 4
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    References
    Preparing Stock Solutions
    Concentration Volume (DMSO) 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
    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: 99.57%

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