[CAS NO. 162359-55-9] Fingolimod

Name: Fingolimod
Brand: Arctom Scientific
SKU: AS572969

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PRODUCTS SPECIFICATIONS [162359-55-9]

Distributor

Catalog

AS572969

Brand

Arctom Scientific

CAS

162359-55-9

DESCRIPTION [162359-55-9]

Overview

MDL	MFCD14705150
Molecular Weight	307.47
Molecular Formula	C19H33NO2
SMILES	OCC(CCC1=CC=C(CCCCCCCC)C=C1)(N)CO

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

20 Publications Citing Use of MCE

Summary

Fingolimod (FTY720 free base) is a sphingosine 1-phosphate ( S1P ) antagonist with an IC ₅₀ of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant ^[1] .

IC50 & Target

S1P

0.033 nM (IC ₅₀ , in K562 and NK cells)

PAK1

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 IC ₅₀ 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 or SEW2871, with an IC ₅₀ effect of 173 or 15 nM, respectively ^[1] . Fingolimod has been reported to reduce LPA synthesis via inhibition of the lysophospholipase autotaxin. Fingolimod treatment correlates with a significant elevation of axonal cAMP, a crucial factor for axonal outgrowth. Additionally, Fingolimod significantly reduces LPA levels in the injured nerve. PF-8380 treatment correlates with improved myelin thickness ^[2] .

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

In Vivo

Fingolimod treatment results in significantly increased nerve conduction at 14 days post-crush in wildtype C57BL/6 mice. However, Foxn1 ^-/- mice, which are devoid of T- but not B-lymphocytes, show an improvement of nerve regeneration under fingolimod treatment. Although the mean increase in nerve conduction velocity in both fingolimod-treated and control Foxn1 ^-/- mice implies a potentially positive role of T-lymphocyte deficiency on nerve regeneration, only fingolimod-treated Foxn1 ^-/- mice show a significant improvement compared to C57BL/6 controls and performed better in the functional analysis ^[2] . Treatment of the animals with Fingolimod for 28 d results in a clear reduction in the binding of ¹⁸ F-GE180 when compare with vehicle-treated animals and evaluated by ex vivo autoradiography. Quantification of the binding of the radiotracer revealed a significant reduction in the binding potential of ¹⁸ F-GE180 (P<0.0001) after treatment with Fingolimod ^[3] .

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00099749	Novartis Pharmaceuticals\|Novartis	Kidney Transplantation	November 2003	Phase 2\|Phase 3
NCT01625182	Novartis Pharmaceuticals\|Mitsubishi Tanabe Pharma Corporation\|Novartis	Chronic Inflammatory Demyelinating Polyradiculoneuropathy	December 22, 2012	Phase 3
NCT01534182	Novartis Pharmaceuticals\|Novartis	Relapsing Remitting Multiple Sclerosis	January 2012	Phase 4
NCT02193217	Mitsubishi Tanabe Pharma Corporation	Relapsing-remitting Multiple Sclerosis		Phase 1
NCT01755871	Heinrich-Heine University, Duesseldorf\|Novartis Pharmaceuticals	Relapsing Remitting Multiple Sclerosis	January 2013	Phase 4
NCT04675762	Second Affiliated Hospital, School of Medicine, Zhejiang University\|Shaoxing People´s Hospital\|Jiaxing People´s Hospital\|Huzhou Center Hospital\|The Second Affiliated Hospital of Jiaxing University\|Jinhua Center Hospital\|Taizhou Hospital	Stroke\|Inflammation	January 15, 2021	Phase 2
NCT00239902	Novartis Pharmaceuticals\|Novartis	Renal Transplantation	May 2002	Phase 2
NCT01621269	Novartis Pharmaceuticals\|Novartis	Multiple Sclerosis	June 2013	Phase 4
NCT01791192	Novartis Pharmaceuticals\|Novartis	Acute Noninfectious Posterior, Intermediate, or Pan Uveitis	November 2013	Phase 2
NCT00239811	Novartis Pharmaceuticals\|Novartis	Renal Transplantation	April 2004	Phase 3
NCT01281657	Novartis	Multiple Sclerosis	February 2011
NCT00355134	Novartis	Multiple Sclerosis	June 2006	Phase 3
NCT01442194	Novartis Pharmaceuticals\|Novartis	Multiple Sclerosis	August 1, 2011
NCT01779700	Indiana University	Schizophrenia	January 2013	Phase 2
NCT00239785	Novartis Pharmaceuticals\|Novartis	Renal Transplantation	April 2003	Phase 3
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
NCT00099736	Novartis Pharmaceuticals\|Novartis	Kidney Transplantation	May 7, 2003	Phase 3
NCT04926818	Novartis Pharmaceuticals\|Novartis	Multiple Sclerosis (MS)	October 5, 2021	Phase 3
NCT00416845	Novartis	Healthy	October 2006	Phase 1
NCT02232061	Novartis Pharmaceuticals\|Novartis	Multiple Sclerosis	September 29, 2014	Phase 4
NCT04629872	Ning Wang, MD., PhD.\|First Affiliated Hospital of Fujian Medical University	Stroke Inflammation	November 12, 2020	Phase 2
NCT00670449	Novartis\|Mitsubishi Tanabe Pharma Corporation	Multiple Sclerosis	April 2008	Phase 2
NCT02061137	University Hospital, Basel, Switzerland\|Novartis	Rett´s Syndrome	August 2013	Phase 1\|Phase 2
NCT01436643	Novartis Pharmaceuticals\|Novartis	Depression\|Relapsing-remitting Multiple Sclerosis	November 2011	Phase 4
NCT01892722	Novartis Pharmaceuticals\|Novartis	Multiple Sclerosis	July 26, 2013	Phase 3
NCT02342704	Biogen	Relapsing-Remitting Multiple Sclerosis	November 30, 2014	Phase 4
NCT00099801	Novartis Pharmaceuticals\|Novartis	Kidney Transplantation	January 2005	Phase 3
NCT05145621	Alembic Pharmaceuticals Ltd.	Bioequivalence\|Safety	October 29, 2015	Phase 1
NCT03757338	Asofarma S.A.I. y C.\|Zenith Technology Corporation Limited	Healthy Volunteers	October 23, 2015	Phase 1
NCT00333138	Novartis	Multiple Sclerosis	May 2003	Phase 2
NCT00731523	Novartis	Renal Insufficiency	July 2008	Phase 1
NCT02002390	Tianjin Medical University General Hospital	Stroke\|Vascular Accident\|Cerebral Stroke\|Ischemic Cerebrovascular Accident\|Stroke, Acute	October 2012	Phase 2
NCT01623596	Novartis Pharmaceuticals\|Novartis	Relapsing Remitting Multiple Sclerosis	June 8, 2012	Phase 4
NCT01420055	Novartis Pharmaceuticals\|Novartis	Multiple Sclerosis, Relapsing-Remitting	August 2011	Phase 4
NCT04676204	Monash University	Multiple Sclerosis\|Adherence, Medication	September 25, 2020
NCT02575365	Novartis Pharmaceuticals\|Novartis	Cognition\|Brain Volume Loss	February 16, 2016	Phase 4
NCT02325440	University Hospital Muenster\|Novartis	Relapsing Remitting Multiple Sclerosis	March 2014	Phase 4
NCT00289978	Novartis	Relapsing-remitting Multiple Sclerosis	January 2006	Phase 3
NCT03257358	Novartis Pharmaceuticals\|Novartis	Relapsing Multiple Sclerosis	September 19, 2017	Phase 4
NCT01497262	Novartis Pharmaceuticals\|Novartis	Multiple Sclerosis	February 2012	Phase 3
NCT00239798	Novartis Pharmaceuticals\|Mitsubishi Tanabe Pharma Corporation\|Novartis	Renal Transplantation	November 2004	Phase 2
NCT04667949	Novartis Pharmaceuticals\|Novartis	Relapsing Multiple Sclerosis (RMS)	February 20, 2021	Phase 4
NCT01633112	Novartis Pharmaceuticals\|Novartis	Relapsing-remitting Multiple Sclerosis (RRMS)	August 9, 2012	Phase 3
NCT01199861	Novartis	Relapsing Multiple Sclerosis	August 2010	Phase 3
NCT05423769	Hikma Pharmaceuticals LLC	Relapsing-Remitting Multiple Sclerosis	January 19, 2022
NCT04088630	Wake Forest University Health Sciences	Intracerebral Hemorrhage\|Cerebral Edema\|Stroke Hemorrhagic\|Intracerebral Hemorrhage, Hypertensive\|Intracerebral Hemorrhage Intraparenchymal	August 7, 2020	Early Phase 1
NCT02490930	Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins	Glioblastoma\|Anaplastic Astrocytoma	July 2015	Early Phase 1
NCT00662649	Novartis	Multiple Sclerosis	February 2008	Phase 3
NCT00340834	Novartis	Multiple Sclerosis	May 2006	Phase 3
NCT04718064	The Affiliated Hospital of Xuzhou Medical University	Stroke	February 1, 2021	Not Applicable
NCT03345940	Fondazione I.R.C.C.S. Istituto Neurologico Carlo Besta\|Patient-Centered Outcomes Research Institute\|Universita degli Studi di Genova	Relapsing Remitting Multiple Sclerosis	April 30, 2017	Phase 4
NCT05307731	General Hospital of Shenyang Military Region	Diabetes Mellitus, Type 2	March 15, 2022	Phase 4
NCT05516303	University Hospital, Caen	Multiple Sclerosis	June 7, 2022
NCT02939079	Isfahan University of Medical Sciences\|Shiraz University of Medical Sciences	Multiple Sclerosis	April 2015	Phase 2\|Phase 3
NCT03941743	Mayo Clinic\|National Cancer Institute (NCI)	Breast Carcinoma	May 24, 2019	Phase 1
NCT02956200	Second Affiliated Hospital, School of Medicine, Zhejiang University\|Shaoxing People´s Hospital\|Jiaxing People´s Hospital\|Huzhou Center Hospital\|The Second Affiliated Hospital of Jiaxing University\|Jinhua Center Hospital\|Taizhou Hospital	Stroke\|Inflammation	November 2016	Phase 2
NCT01705236	Novartis Pharmaceuticals\|Novartis	Relapsing Remitting Multiple Sclerosis RRMS	August 20, 2012	Phase 4
NCT02373098	Novartis Pharmaceuticals\|Novartis	Relapsing Remitting Multiple Sclerosis	March 31, 2015	Phase 4
NCT01317004	Novartis Pharmaceuticals\|Novartis	Relapsing Remitting Multiple Sclerosis	May 2011	Phase 4
NCT01127750	Novartis	Relapsing Multiple Sclerosis	May 2010	Phase 3
NCT01498887	Novartis Pharmaceuticals\|Novartis	Relapsing Remitting Multiple Sclerosis	December 24, 2011	Phase 4
NCT03943498	Mayo Clinic\|National Cancer Institute (NCI)	Chemotherapy-Induced Peripheral Neuropathy\|Numbness\|Pain\|Tingling	May 24, 2019	Early Phase 1
NCT01310166	Novartis Pharmaceuticals\|Novartis	Relapsing-remitting Multiple Sclerosis	February 2011	Phase 4
NCT01333501	Novartis Pharmaceuticals\|Novartis	Multiple Sclerosis	May 2011	Phase 4
NCT05123703	Hoffmann-La Roche\|PPD	Relapsing-Remitting Multiple Sclerosis	February 4, 2022	Phase 3
NCT00239876	Novartis Pharmaceuticals\|Novartis	Renal Transplantation	May 2005	Phase 3
NCT04480853	Novartis Pharmaceuticals\|Novartis	Multiple Sclerosis	October 12, 2020	Phase 4
NCT01585298	Novartis Pharmaceuticals\|Novartis	Multiple Sclerosis	April 29, 2012	Phase 4
NCT00239863	Novartis Pharmaceuticals\|Novartis	Renal Transplantation	May 2004	Phase 3
NCT05285878	The Methodist Hospital Research Institute	Interstitial Fibrosis\|Kidney Transplant; Complications\|Kidney Transplant Rejection\|Kidney Transplant Failure and Rejection\|Kidney Transplant Failure\|Kidney Failure, Chronic\|Graft Rejection	April 15, 2022	Phase 2
NCT00537082	Novartis\|Mitsubishi Tanabe Pharma Corporation	Multiple Sclerosis	September 2007	Phase 2
NCT05141669	Novartis Pharmaceuticals\|Novartis	Multiple Sclerosis	May 18, 2020
NCT04280588	First Affiliated Hospital of Fujian Medical University	Coronavirus Disease (COVID-19)	February 22, 2020	Phase 2
NCT00731692	Novartis Pharmaceuticals\|Novartis	Primary Progressive Multiple Sclerosis	July 28, 2008	Phase 3
NCT01941004	Novartis Pharmaceuticals\|Novartis	Multiple Sclerosis (Relapsing Remitting)	June 2014	Phase 3
NCT00098735	Novartis Pharmaceuticals\|Novartis	Kidney Transplantation	April 2004	Phase 3
NCT02720107	Novartis Pharmaceuticals\|Novartis	Relapsing-remitting Multiple Sclerosis	May 12, 2016	Phase 4
NCT00785083	Novartis	Asthma	September 2008	Phase 2
NCT01216072	Novartis Pharmaceuticals\|Novartis	Relapsing Forms of Multiple Sclerosis	August 2010	Phase 4
NCT01285479	Novartis Pharmaceuticals\|Novartis	Multiple Sclerosis	October 15, 2011
NCT01201356	Novartis Pharmaceuticals\|Novartis	Relapsing Forms of Multiple Sclerosis	September 13, 2010	Phase 3
NCT01578330	Novartis Pharmaceuticals\|Novartis	Multiple Sclerosis\|Relapsing-Remitting	October 2012	Phase 4

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

Ethanol : 7.69 mg/mL ( 25.01 mM ; Need ultrasonic)

DMSO : 2 mg/mL ( 6.50 mM ; ultrasonic and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.2523 mL	16.2617 mL	32.5235 mL
5 mM	0.6505 mL	3.2523 mL	6.5047 mL
10 mM	0.3252 mL	1.6262 mL	3.2523 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% EtOH >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 1 mg/mL (3.25 mM); Clear solution
2.

Add each solvent one by one: 10% EtOH >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 1 mg/mL (3.25 mM); Clear solution
3.

Add each solvent one by one: 10% EtOH >> 90% corn oil

Solubility: ≥ 1 mg/mL (3.25 mM); Clear solution

* All of the co-solvents are available by MCE.

References

Synonyms

1,3-Propanediol, 2-amino-2-[2-(4-octylphenyl)ethyl]-

2-Amino-2-[2-(4-octylphenyl)ethyl]-1,3-propanediol

Fingolimod

2-Amino-2-[2-(4-octylphenyl)ethyl]-1,3-propandiol

2-Amino-2-[2-(4-octylphenyl)ethyl]propane-1,3-diol