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
-
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
More
Biological Activity
|
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] |
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 No. 402615-91-2
-
Appearance Solid
-
Molecular Weight 387.45
-
Formula C19H34NO5P
-
Color White to off-white
-
SMILES
OCC(CCC1=CC=C(CCCCCCCC)C=C1)(N)COP(O)(O)=O
-
Synonyms
FTY720 phosphate
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (1)
-
Journal Impact Factor
-
Most Recent
Purity & Documentation
-
Data Sheet (267 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)
-
Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)