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Fingolimod (FTY-720)

Name: Fingolimod (FTY-720)
Brand: Selleck Chemicals
SKU: S5950
Rating: 5 (22 reviews)

Synonyms: FTY-720A

Catalog No.S5950 Purity: 99.97%

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

Fingolimod (FTY-720) Chemical Structure

CAS: 162359-55-9

Selleck's Fingolimod (FTY-720) has been cited by 22 publications

Purity & Quality Control

Batch: Purity: 99.97%

99.97

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Biological Activity

Description

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

Targets

S1P receptor ^[1]

In vitro
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].
Cell Research	Cell lines	NSCLC cells
	Concentrations	10 μM
	Incubation Time	72 h
	Method	Cells were treated with various concentrations of drug for 72 h.
Experimental Result Images	Methods	Biomarkers	Images	PMID
Experimental Result Images	Western blot	p-myosin IIA HC / p-histone H3 S10 / Histone H3 / Cleaved TRPM7 PTEN / p53 / p-AKT / p-GSK3β / p-ERK / ERK / p-STAT3 / STAT3 / Mcl-1 / Cyclin D1		29299124

In Vivo
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].
Animal Research	Animal Models	C57/B6 mice
	Dosages	1 mg/kg
	Administration	o.g.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05141669	Completed	Multiple Sclerosis	Novartis Pharmaceuticals\|Novartis	May 18 2020	--
NCT03345940	Terminated	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	Cognition\|Brain Volume Loss	Novartis Pharmaceuticals\|Novartis	February 16 2016	Phase 4

References

Chemical lnformation & Solubility

Molecular Weight	307.47	Formula	C₁₉H₃₃NO₂
CAS No.	162359-55-9	SDF	--
Smiles	CCCCCCCCC1=CC=C(C=C1)CCC(CO)(CO)N
Storage (From the date of receipt)	3 years -20°C powder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years -20°C powder		1 month-20°Cin solvent

In vitro
Batch:

DMSO : 13 mg/mL ( (42.28 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

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In vivo
Batch:

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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