| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
(R)-FTY 720P targets the sphingosine-1-phosphate (S1P) receptors, specifically S1P1, S1P3, S1P4, and S1P5. The (R)-isomer has a weaker binding affinity to these receptors compared to its (S)-isomer counterpart. The (S)-FTY 720P is a potent agonist of S1P receptors and induces receptor internalization, which is the basis for the immunomodulatory effects of fingolimod.
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| ln Vitro |
(R)-FTY 720P has less potent binding affinities to S1P1, S1P3, S1P4, and S1P5 than the (S)-isomer . This stereoselectivity makes it a valuable control to study the specific activity of the (S)-enantiomer. The EC50 for (S)-FTY 720P to activate the S1P1 receptor is 0.14 nM in a [3⁵S]GTPgammaS binding assay, but the EC50 for the (R)-isomer is not reported. The (S)-isomer is the active form that induces receptor internalization.
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| ln Vivo |
(R)-FTY 720P (administered by intravenous bolus) had no significant effect on the heart rate of anesthetized rats at doses up to 0.3 mg/kg [1].
No specific in vivo data was found for (R)-FTY 720P. As a less potent isomer, it is not the primary active moiety of fingolimod. The (S)-isomer is the active principle that causes lymphocyte sequestration in lymph nodes, leading to a reduced number of circulating lymphocytes. It is also known that FTY720P can cause bradycardia by activating S1P1 receptors on atrial myocytes. |
| Enzyme Assay |
Standard S1P receptor radioligand binding assay: Cell membrane homogenates expressing the human S1P1 receptor (e.g., from CHO cells) are incubated with a radiolabeled ligand, such as [33P]S1P or [3H]FTY720P, in a binding buffer. The test compound, (R)-FTY 720P, is added at varying concentrations to compete for binding. After incubation and separation of bound from free radioactivity via filtration, the scintillation count is measured, and the Ki or IC50 for the test compound is calculated. This data is then compared to the (S)-isomer.
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| Cell Assay |
Standard S1P1 receptor functional assay (e.g., [35S]GTPgammaS binding): Membranes from CHO cells expressing the human S1P1 receptor are incubated with varying concentrations of (R)-FTY 720P, along with [35S]GTPgammaS and GDP. The amount of [35S]GTPgammaS bound to the membrane, which is proportional to the receptor's G-protein activation, is quantified. This allows the determination of the compound's agonism (EC50) and efficacy (Emax). (R)-FTY 720P is expected to have a higher EC50 and lower Emax compared to the (S)-isomer.
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| Animal Protocol |
No specific animal protocol was found. In a standard model, (R)-FTY 720P could be administered to C57BL/6 mice via oral gavage or IP injection to assess its effect on peripheral lymphocyte counts. Blood samples would be collected at various time points (e.g., 4, 8, 24 hours) post-dosing, and a complete blood count (CBC) would be performed to measure the absolute number of lymphocytes. This effect would then be compared to that of the active (S)-isomer.
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| ADME/Pharmacokinetics |
No specific PK data was found. As the chiral isomer of FTY720P, (R)-FTY 720P would have a very similar PK profile to its (S)-counterpart. After administration, it would be highly protein-bound and distribute extensively into tissues. The PK parameters (half-life, clearance, volume of distribution) would be determined by standard LC-MS/MS methods.
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| Toxicity/Toxicokinetics |
No specific toxicity data was found. (R)-FTY 720P is not a clinical drug, but its parent compound, fingolimod, has several known side effects, the most notable being bradycardia (slowing of the heart rate) due to S1P1 activation on atrial myocytes, and macular edema. The (R)-isomer, being less potent, would likely have a lower risk of such on-target toxicities.
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| References | |
| Additional Infomation |
(R)-FTY 720P (CAS: 402616-23-3) has a molecular formula of C19H34NO5P and a molecular weight of 387.45. It is the R-isomer of FTY 720P, with less potent binding affinities to S1P1, S1P3, S1P4, and S1P5 than the (S)-isomer. This product is a controlled substance and is for research use only.
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| Molecular Formula |
C19H34NO5P
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|---|---|
| Molecular Weight |
387.45
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| Exact Mass |
387.217
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| CAS # |
402616-23-3
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| PubChem CID |
9908268
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| Appearance |
Typically exists as solids at room temperature
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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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| 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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| 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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| SMILES |
CCCCCCCCC1=CC=C(C=C1)CC[C@@](CO)(COP(=O)(O)O)N
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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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| 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.
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