Fingolimod phosphate
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.
For research use only. We do not sell to patients.
- Purity: 99.18%
- CAS No.: 402615-91-2
- Formula: C19H34NO5P
- Molecular Weight:387.45
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications Citing Use of MedChemExpress (MCE) Fingolimod phosphate
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Biological Activity
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Cell Line
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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] |
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
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CAS No. 402615-91-2
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Appearance Solid
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Molecular Weight 387.45
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Formula C19H34NO5P
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Color White to off-white
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SMILES
OCC(CCC1=CC=C(CCCCCCCC)C=C1)(N)COP(O)(O)=O
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Synonyms
FTY720 phosphate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
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Journal Impact Factor
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Most Recent
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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-
-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (268 KB)
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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)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
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.
| 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 |