| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
|
||
| 250mg |
|
||
| 500mg |
|
||
| 1g |
|
||
| 5g |
|
Purity: ≥98%
Fingolimod (formerly FTY720; FTY-720; FTY 720; trade names Gilenia and Gilenya), an approved medication for treating Multiple sclerosis, is a potent S1P
(sphingosine 1-phosphate) antagonist with anticancer 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.
| ln Vitro |
Before surviving with NK cells, monocyte-derived immature dendritic cells (iDCs) were exposed to various doses of S1P for variable amounts of time. In these dishes, autologous or allogeneic iDCs that were exposed to 0.2–20 μM S1P for four hours considerably shielded the NK cells. For autologous iDCs and allogeneic iDCs, the IC50 values for S1P were determined to be 160 nM and 34 nM, respectively. Subsequently, fingolimod or SEW2871 at varying doses were able to counteract the inhibitory effect of S1P, with IC50 values of 173 or 15 nM, respectively [1]. It has been observed that fungiolimod causes LPA to be synthesized by preventing lysophospholipase automobility in cells. An important component of axonal development, axonal cAMP concentration, showed a strong correlation with fingolim therapy. Furthermore, fingolimod dramatically lowered the nerve center's LPA levels. Myelin thickness improvements are linked to PF-8380 therapy [2].
|
|---|---|
| ln Vivo |
Fourteen days after extrusion, fingolimod therapy led to a notable increase in nerves in wild-type C57BL/6 nozzles. On the other hand, T-deficient B-deleted Foxn1-/-nozzles treated with fingolimod demonstrated enhanced nerve regeneration. Though the average rate of nerve growth in Foxn1-/- nozzles treated with Fingolimod and control Foxn1-/- nozzles suggested that T deficit affects nerve regeneration. Possibility of a role, although only Foxn1-/-treated mice significantly outperformed C57BL/6 and fared better in functional examination [2]. Ex vivo radioactive autobinding was used to quantify the amount of 18F-GE180 tracer binding that occurred after animals treated with fingolimod for 28 days. The results showed that the binding potential of 18F-GE180 was significantly reduced (P<0.0001) after treatment with fingolimod.
|
| References |
[1]. Rolin J, et al. FTY720 and SEW2871 reverse the inhibitory effect of S1P on natural killer cell mediated lysis of K562 tumor cells and dendritic cells but not on cytokine release. Cancer Immunol Immunother. 2010, 59(4), 575-586.
[2]. Szepanowski F, et al. Fingolimod promotes peripheral nerve regeneration via modulation of lysophospholipid signaling. J Neuroinflammation. 2016 Jun 10;13(1):143. [3]. Airas L, et al. In vivo PET imaging demonstrates diminished microglial activation after fingolimod treatment in an animal model of multiple sclerosis. J Nucl Med. 2015 Feb;56(2):305-10. [4]. Shirakabe K, et al. Modification of lymphocyte migration to Peyer's patches by inhibition of sphingosine-1-phosphate lyase ameliorates murine colitis. J Gastroenterol Hepatol. 2018 Jan 15 |
| Molecular Formula |
C19H33NO2
|
|---|---|
| Molecular Weight |
307.478
|
| Exact Mass |
307.2511
|
| CAS # |
162359-55-9
|
| Related CAS # |
Fingolimod-d4;1346747-38-3;Fingolimod-d4 hydrochloride;1346604-90-7;Fingolimod hydrochloride;162359-56-0
|
| SMILES |
O([H])C([H])([H])C(C([H])([H])O[H])(C([H])([H])C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H])N([H])[H]
|
| Chemical Name |
2-Amino-2-[2-(4-octylphenyl)ethyl]-1,3-propandiol
|
| Synonyms |
FTY720 (free base); FTY720; Fingolimod HCl; FTY-720; FTY 720; Trade name: Gilenia and Gilenya.
|
| 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)
|
| Solubility (In Vitro) |
Ethanol : ~7.69 mg/mL (~25.01 mM)
DMSO : ~2 mg/mL (~6.50 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (3.25 mM) (saturation unknown) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear EtOH stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1 mg/mL (3.25 mM) (saturation unknown) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear EtOH stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1 mg/mL (3.25 mM) (saturation unknown) in 10% EtOH + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2522 mL | 16.2612 mL | 32.5224 mL | |
| 5 mM | 0.6504 mL | 3.2522 mL | 6.5045 mL | |
| 10 mM | 0.3252 mL | 1.6261 mL | 3.2522 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA