Art. -Nr.: HY-15381

Fingolimod phosphate

(Synonyms: FTY720 phosphate)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

Fingolimod phosphate (FTY720 phosphate) is an orally active sphingosine 1-phosphate (S1P) receptor agonist. Fingolimod phosphate can promote the neuroprotective effects of microglia. Fingolimod phosphate can be used for the research of multiple sclerosis and neurologic diseases.

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Reinheit: 99.18%
CAS. Nr.: 402615-91-2
Formel: C₁₉H₃₄NO₅P
Molecular Weight:387.45

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Fingolimod phosphate Chemical Structure

CAS. Nr.: 402615-91-2

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Alle LPL Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	0.28 nM Compound: 2	Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 1 expressed on CHO cell membranes Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 1 expressed on CHO cell membranes	[PMID: 15149705]
CHO	IC₅₀	0.77 nM Compound: 2	Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 5 expressed on CHO cell membranes	[PMID: 15149705]
CHO	IC₅₀	15 nM Compound: 2	Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 4 expressed on CHO cell membranes Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 4 expressed on CHO cell membranes	[PMID: 15149705]
CHO	IC₅₀	6.3 nM Compound: 2	Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 3 expressed on CHO cell membranes Inhibition of [33P]-S1P binding to human Sphingosine 1-phosphate receptor 3 expressed on CHO cell membranes	[PMID: 15149705]
CHO	EC₅₀	0.3 nM Compound: 2	Activity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay Activity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay	[PMID: 15615513]
CHO	IC₅₀	0.28 nM Compound: 2	Displacement of [33P]sphingosine 1 phosphate from human S1P1 receptor expressed in CHO cells Displacement of [33P]sphingosine 1 phosphate from human S1P1 receptor expressed in CHO cells	[PMID: 15615513]
CHO	IC₅₀	0.77 nM Compound: 2	Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells Displacement of [33P]sphingosine 1 phosphate from human S1P5 receptor expressed in CHO cells	[PMID: 15615513]
CHO	IC₅₀	1100 nM Compound: 2	Displacement of [33P]sphingosine 1 phosphate from human S1P2 receptor expressed in CHO cells Displacement of [33P]sphingosine 1 phosphate from human S1P2 receptor expressed in CHO cells	[PMID: 15615513]
CHO	IC₅₀	15 nM Compound: 2	Displacement of [33P]sphingosine 1 phosphate from human S1P4 receptor expressed in CHO cells Displacement of [33P]sphingosine 1 phosphate from human S1P4 receptor expressed in CHO cells	[PMID: 15615513]
CHO	IC₅₀	6.3 nM Compound: 2	Displacement of [33P]sphingosine 1 phosphate from human S1P3 receptor expressed in CHO cells Displacement of [33P]sphingosine 1 phosphate from human S1P3 receptor expressed in CHO cells	[PMID: 15615513]
CHO	EC₅₀	1.2 nM Compound: (rac)-5	Agonism of human S1P-1 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand Agonism of human S1P-1 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand	[PMID: 16078855]
CHO	EC₅₀	1.4 nM Compound: (rac)-5	Agonism of human S1P-3 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand Agonism of human S1P-3 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand	[PMID: 16078855]
CHO	EC₅₀	2.4 nM Compound: (rac)-5	Agonism of human S1P-4 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand Agonism of human S1P-4 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand	[PMID: 16078855]
CHO	EC₅₀	4.9 nM Compound: (rac)-5	Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand	[PMID: 16078855]
CHO	EC₅₀	>10000 nM Compound: (rac)-5	Agonism of human S1P-2 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand Agonism of human S1P-2 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand	[PMID: 16078855]
CHO	EC₅₀	12 nM Compound: 1-P, FTY20-P	Agonist activity at human S1P3 receptor expressed in CHO cells assessed as intracellular calcium mobilization Agonist activity at human S1P3 receptor expressed in CHO cells assessed as intracellular calcium mobilization	[PMID: 20337461]
CHO	EC₅₀	35.1 nM Compound: 3, FTY720-P	Agonist activity at human S1P3 receptor expressed in CHO cells preincubated for 2 hrs before IP1 addition by IP1-HTRF assay Agonist activity at human S1P3 receptor expressed in CHO cells preincubated for 2 hrs before IP1 addition by IP1-HTRF assay	[PMID: 25072873]
CHO	EC₅₀	9.1 nM Compound: 3, FTY720-P	Agonist activity at human S1P1 receptor expressed in CHO cells preincubated for 2 hrs before IP1 addition by IP1-HTRF assay Agonist activity at human S1P1 receptor expressed in CHO cells preincubated for 2 hrs before IP1 addition by IP1-HTRF assay	[PMID: 25072873]
CHO	EC₅₀	11 nM Compound: FTY720-phosphate	Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay	[PMID: 26509640]
CHO	EC₅₀	3.4 nM Compound: FTY720-phosphate	Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay	[PMID: 26509640]
CHO	EC₅₀	0.005 nM Compound: 1-P; FTY-P	Agonist activity at human S1P1 receptor expressed in CHO cells assessed as cAMP accumulation after 30 mins by HTRF analysis Agonist activity at human S1P1 receptor expressed in CHO cells assessed as cAMP accumulation after 30 mins by HTRF analysis	[PMID: 26985316]
CHO	EC₅₀	0.0056 nM Compound: 1-P; FTY-P	Agonist activity at human S1P1 receptor expressed in CHO cells assessed as ERK phosphorylation after 7 mins by alphaLISA Agonist activity at human S1P1 receptor expressed in CHO cells assessed as ERK phosphorylation after 7 mins by alphaLISA	[PMID: 26985316]
CHO	EC₅₀	0.07 nM Compound: 1-P; FTY-P	Agonist activity at human S1P1 receptor expressed in CHO cells co-expressing GFP assessed as cellular internalization after 45 mins by Hoechst assay Agonist activity at human S1P1 receptor expressed in CHO cells co-expressing GFP assessed as cellular internalization after 45 mins by Hoechst assay	[PMID: 26985316]
CHO	IC₅₀	0.014 nM Compound: 1-P; FTY-P	Displacement of 33-P-S1P from from human S1P receptor expressed in CHO cell membranes after 50 mins by scintillation counting Displacement of 33-P-S1P from from human S1P receptor expressed in CHO cell membranes after 50 mins by scintillation counting	[PMID: 26985316]
CHO	EC₅₀	14 nM Compound: 3, FTY-720P	Agonist activity at S1P1 receptor (unknown origin) expressed in CHO cells preincubated for 2 hrs followed by D2-labeled IP1 and Ab-Cryp addition measured after 1 hr by fluorescence assay Agonist activity at S1P1 receptor (unknown origin) expressed in CHO cells preincubated for 2 hrs followed by D2-labeled IP1 and Ab-Cryp addition measured after 1 hr by fluorescence assay	10.1039/C3MD00079F
CHO	EC₅₀	44 nM Compound: 3, FTY-720P	Agonist activity at S1P3 receptor (unknown origin) expressed in CHO cells preincubated for 2 hrs followed by D2-labeled IP1 and Ab-Cryp addition measured after 1 hr by fluorescence assay Agonist activity at S1P3 receptor (unknown origin) expressed in CHO cells preincubated for 2 hrs followed by D2-labeled IP1 and Ab-Cryp addition measured after 1 hr by fluorescence assay	10.1039/C3MD00079F
HEK-293T	EC₅₀	0.1 nM Compound: FTY720-P	Activity at human S1P3 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay Activity at human S1P3 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay	[PMID: 17113298]
HEK-293T	EC₅₀	1.3 nM Compound: FTY720-P	Activity at human S1P1 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay Activity at human S1P1 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay	[PMID: 17113298]
HEK-293T	EC₅₀	4 nM Compound: FTY720-P	Activity at human S1P4 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay Activity at human S1P4 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay	[PMID: 17113298]
HEK-293T	EC₅₀	4 nM Compound: FTY720-P	Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay	[PMID: 17113298]

In Vitro

Fingolimod phosphate prevents lymphocytes from moving out of the lymphoid organs and inhibits autoreactive lymphocytes from infiltrating the central nervous system^[1].
Fingolimod phosphate (0, 1, 10, 100 nM) binds S1P1 receptors to downregulate activated microglial production of such pro-inflammatory cytokines as tumor necrosis factor-a, interleukin-1β, and interleukin-6^[1].
Fingolimod phosphate (0, 1, 10, 100 nM) also upregulates microglial production of brain-derived neurotrophic factor and glial cell-derived neurotrophic factor^[1].

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

Chemical Information

CAS. Nr. 402615-91-2
Appearance Solid
Molecular Weight 387.45
Formel C₁₉H₃₄NO₅P
Color White to off-white
SMILES

OCC(CCC1=CC=C(CCCCCCCC)C=C1)(N)COP(O)(O)=O
Synonyms

FTY720 phosphate
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (1)

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Biomed Chromatogr

Liquid chromatography-tandem mass spectrometry for determination of fingolimod and its active metabolite fingolimod phosphate in whole blood of patients with multiple sclerosis. [Abstract]

2024 Jun 26:e5947. PMID: 38932506

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 22.22 mg/mL (57.35 mM; ultrasonic and adjust pH to 2 with 1 M HCL; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.5810 mL

12.9049 mL

25.8098 mL

5 mM

0.5162 mL

2.5810 mL

5.1620 mL

10 mM

0.2581 mL

1.2905 mL

2.5810 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.45 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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Animal Weight (Per Animal) Animal Weight (Per Animal)
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Dosing Volume (Per Animal) Dosing Volume (Per Animal)
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
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Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (268 KB)
SDS (421 KB)
- English - EN (421 KB)
- Français - FR (421 KB)
- Deutsch - DE (421 KB)
- Norwegian - NO (421 KB)
- Español - ES (421 KB)
- Swedish - SV (421 KB)
- Italian - IT (421 KB)
- Korean - KR (421 KB)
- Portuguese - PT (421 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Hiromi Noda, et al. Fingolimod phosphate promotes the neuroprotective effects of microglia. J Neuroimmunol. 2013 Mar 15;256(1-2):13-8. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5810 mL	12.9049 mL	25.8098 mL	64.5245 mL
	5 mM	0.5162 mL	2.5810 mL	5.1620 mL	12.9049 mL
	10 mM	0.2581 mL	1.2905 mL	2.5810 mL	6.4524 mL
	15 mM	0.1721 mL	0.8603 mL	1.7207 mL	4.3016 mL
	20 mM	0.1290 mL	0.6452 mL	1.2905 mL	3.2262 mL
	25 mM	0.1032 mL	0.5162 mL	1.0324 mL	2.5810 mL
	30 mM	0.0860 mL	0.4302 mL	0.8603 mL	2.1508 mL
	40 mM	0.0645 mL	0.3226 mL	0.6452 mL	1.6131 mL
	50 mM	0.0516 mL	0.2581 mL	0.5162 mL	1.2905 mL

Keywords

Fingolimod phosphate

1 Cited Publications

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Fingolimod phosphate

Anti-Infection Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Neuroprotective Compound Library

Human Metabolite Library

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Membrane Receptor-targeted Compound Library

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MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Fingolimod phosphate

Alle LPL Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Fingolimod phosphate

Anti-Infection Compound Library

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Neuroprotective Compound Library

Human Metabolite Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Fingolimod phosphate

Alle LPL Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Fingolimod phosphate Related Classifications

HY-15381 Related Classifications