For research use only.

Catalog No.S5950 Synonyms: FTY-720A, FTY-720

15 publications

Fingolimod Chemical Structure

CAS No. 162359-55-9

Fingolimod (FTY-720A, FTY-720) is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis.

Selleck's Fingolimod has been cited by 15 publications

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Biological Activity

Description Fingolimod (FTY-720A, FTY-720) is a sphingosine 1-phosphate receptor modulator used for the treatment of relapsing-remitting multiple sclerosis.
S1P receptor [1]
In vitro

The main immunomodulatory mechanism of action of fingolimod is based on its effect on lymphocyte homing. It reversibly redistributes T and B cells from the circulation to secondary lymphoid organs like peripheral and mesenteric lymph nodes and Peyer's patches, thereby causing a state of peripheral lymphopenia[1].

Methods Test Index PMID
Western blot
p-myosin IIA HC / p-histone H3 S10 / Histone H3 / Cleaved TRPM7 ; 

PubMed: 29299124     

Western blot analysis of whole cell lysates prepared from neuroblastoma cells treated with 3 μM or 10 μM FTY-720.

PTEN / p53 / p-AKT / p-GSK3β / p-ERK / ERK / p-STAT3 / STAT3 / Mcl-1 / Cyclin D1 ; 

PubMed: 21391227     

Western blot analysis of the dose-dependent effects of OSU-2S and FTY720 on the phosphorylation/expression levels of PTEN, p53, Akt, GSK3β, ERK, Stat3, Mcl-1, and cyclin D1 in Huh7 cells after 24 h of treatment.

29299124 21391227
In vivo

SphK2 is the only enzyme which activates fingolimod in vivo,since only Sphk2 knockout mice are resistant to fingolimod-induced lymphopenia. A major advantage of fingolimod as a therapeutic agent is the possibility of its oral application. Absorption is food-independent and slow (maximal plasma concentration after 12-16 h), but extensive, and its bioavailability is high (93%). It reaches steady state concentrations after 1-2 months during daily intake. Fingolimod shows high plasma protein binding (>99.7%), mainly to albumin, and in contrast to S1P, there is no evidence for fingolimod binding to ApoM/HDL. It has a large volume of distribution of approx. 20L/kg and shows slow blood clearance (6.3±2.3 L/h), resulting in a half-life of 6-9 days[1]. Fingolimod alleviates disease burden in immune-mediated animal models of multiple sclerosis[2].


Solubility (25°C)

In vitro DMSO 13 mg/mL (42.28 mM)
Ethanol 5 mg/mL (16.26 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 307.47


CAS No. 162359-55-9
Storage powder
in solvent
Synonyms FTY-720A, FTY-720

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03345940 Terminated Drug: Fingolimod|Drug: Dimethyl Fumarate Relapsing Remitting Multiple Sclerosis Fondazione I.R.C.C.S. Istituto Neurologico Carlo Besta|Patient-Centered Outcomes Research Institute|Universita degli Studi di Genova April 30 2017 Phase 4
NCT02575365 Terminated Drug: 05 mg Fingolimod Cognition|Brain Volume Loss Novartis Pharmaceuticals|Novartis February 16 2016 Phase 4
NCT02490930 Completed Drug: Fingolimod Glioblastoma|Anaplastic Astrocytoma Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins July 2015 Early Phase 1

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S1P Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID