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5mg |
Fingolimod phosphate (FTY-720-P) is the phosphate salt of Fingolimod (FTY-720; FTY 720; Gilenia and Gilenya) with improved water solubility. Fingolimod is an FDA approved drug for the treatment of Multiple sclerosis, acting as a S1P (sphingosine 1-phosphate) antagonist with potential antineoplastic activity. It inhibits S1P with an IC50 of 0.033 nM in K562 and NK cells. It is a folk medicine emerged from Fungi. Fingolimod was firstly found to be a therapeutic agent in organ transplantation. It plays the role in MS treatment through receptor-mediated actions both on the immune system and in the CNS. Fingolimod is used to treat multiple sclerosis, and has antineoplastic activity.
Targets |
sphingosine 1-phosphate (S1P)(IC50 = 0.033 nM, in K562 and NK cells); PAK1
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ln Vitro |
Fingolimod phosphate stops autoreactive lymphocytes from entering the central nervous system and stops lymphocytes from leaving lymphoid organs [1]. Fingolimod phosphate (0, 1, 10, 100 nM) binds to the S1P1 receptor and inhibits activated microglia's production of pro-inflammatory cytokines, including interleukin-1β, interleukin-6, and tumor necrosis factor-a[1]. Additionally, microglia produce more brain-derived neurotrophic factor and glial cell-derived neurotrophic factor when exposed to (0, 1, 10, 100 nM) [1].
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ln Vivo |
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Animal Protocol |
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References | |||
Additional Infomation |
Fingolimod phosphate is a primary amino compound that is fingolimod in which one on the hydroxy groups has been converted into its dihydrogen phosphate derivative. It is the active metabolite of fingolimod. It has a role as an antineoplastic agent, an immunosuppressive agent and a sphingosine-1-phosphate receptor agonist. It is a monoalkyl phosphate, a primary amino compound and a primary alcohol. It is functionally related to a fingolimod.
Fingolimod phosphate (FTY720) is a sphingosine 1-phosphate (S1P) receptor agonist that is being used as a new oral drug for multiple sclerosis. FTY720 prevents lymphocytes from moving out of the lymphoid organs and inhibits autoreactive lymphocytes from infiltrating the central nervous system. Whether FTY720 directly affects microglia-the innate immune cells of the central nervous system-is unclear. Here we show that FTY720 binds S1P1 receptors to downregulate activated microglial production of such pro-inflammatory cytokines as tumor necrosis factor-α, interleukin-1β, and interleukin-6. FTY720 also upregulates microglial production of brain-derived neurotrophic factor and glial cell-derived neurotrophic factor. These results suggested that FTY720 directly promotes the neuroprotective effects of microglia. Therefore, FTY720 may be a potent therapeutic agent for not only multiple sclerosis but also other neurologic diseases associated with microglial activation.[1] |
Molecular Formula |
C19H34NO5P
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Molecular Weight |
387.45100
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Exact Mass |
387.217
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CAS # |
402615-91-2
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Related CAS # |
FTY720 (S)-Phosphate;402616-26-6;Fingolimod phosphate-d4;1794828-93-5
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PubChem CID |
9908268
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Appearance |
White to off-white solid powder
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Density |
1.2±0.1 g/cm3
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Boiling Point |
584.2±60.0 °C at 760 mmHg
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Melting Point |
122-124ºC
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Flash Point |
307.1±32.9 °C
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Vapour Pressure |
0.0±1.7 mmHg at 25°C
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Index of Refraction |
1.541
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LogP |
4.27
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Hydrogen Bond Donor Count |
4
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Hydrogen Bond Acceptor Count |
6
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Rotatable Bond Count |
14
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Heavy Atom Count |
26
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Complexity |
409
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Defined Atom Stereocenter Count |
0
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InChi Key |
LRFKWQGGENFBFO-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C19H34NO5P/c1-2-3-4-5-6-7-8-17-9-11-18(12-10-17)13-14-19(20,15-21)16-25-26(22,23)24/h9-12,21H,2-8,13-16,20H2,1H3,(H2,22,23,24)
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Chemical Name |
[2-amino-2-(hydroxymethyl)-4-(4-octylphenyl)butyl] dihydrogen phosphate
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Synonyms |
Fingolimod phosphate; FTY720 phosphate; 402615-91-2; FTY720 (R)-Phosphate; rac FTY720 Phosphate; 402616-23-3; FTY720-phosphate; fingolimod-P;
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.