| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| Targets |
Lisofylline targets lysophosphatidic acid acyltransferase (LPAAT) with an IC₅₀ of 0.6 µM. It inhibits the generation of phosphatidic acid (PA) and free fatty acids. The compound blocks the release of pro-inflammatory cytokines in oxidative tissue injury, in response to cancer chemotherapy, and in experimental sepsis. It inhibits IFN-γ production and IL-12-mediated STAT-4 activation.
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|---|---|
| ln Vitro |
In vitro, lisofylline inhibits the formation of oleate- and linoleate-containing phosphatidic acid in LPS-stimulated P388 monocytic leukemia cells. It does not inhibit the activation of phosphatidylinositol-specific phospholipase C. The compound enhances glucose-stimulated insulin secretion from β-cells and suppresses pro-inflammatory cytokine production.
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| ln Vivo |
In vivo, lisofylline protected BALB/c mice from LPS-induced lethality. In rats, it prevented oxidant-mediated capillary leak in isolated rat lungs previously treated with IL-8. The compound also protects intestinal barrier function after ischemic or hemorrhagic shock, possibly by preserving microvascular structure and perfusion. Lisofylline has been explored for therapeutic effects in sepsis, autoimmune diseases, and chronic inflammatory disorders.
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| Enzyme Assay |
LPAAT enzyme assays: Enzyme preparations are incubated with [¹⁴C]-oleoyl-CoA and lysophosphatidic acid substrate in the presence of lisofylline at various concentrations. Radioactive phosphatidic acid product is extracted and quantified by scintillation counting. IC₅₀ values are calculated from dose-response curves. For cytokine inhibition studies, immune cells are stimulated with LPS or cytokines and treated with lisofylline.
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| Cell Assay |
Immune cells (e.g., macrophages or monocytes) are cultured in appropriate media and stimulated with LPS or inflammatory cytokines (TNF-α, IL-1β) in the presence or absence of lisofylline at various concentrations (typically 1-100 µM). Cytokine levels (IFN-γ, IL-12, TNF-α) in supernatant are measured by ELISA. STAT-4 activation is assessed by Western blot for phosphorylated STAT-4.
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| Animal Protocol |
In animal studies, lisofylline is administered intraperitoneally or orally to mice or rats at doses typically ranging from 10-100 mg/kg. LPS-induced endotoxic shock models: animals are challenged with LPS and survival rates are monitored. Lung injury models: rats are treated with IL-8 and lisofylline, and capillary leak is assessed by measuring protein content in bronchoalveolar lavage fluid. Ischemia-reperfusion models are used to study intestinal barrier protection.
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| ADME/Pharmacokinetics |
Lisofylline (racemic) has molecular formula C₁₃H₂₀N₄O₃ and molecular weight 280.3. It is soluble in DMSO. The compound is a metabolite of pentoxifylline and is approximately 800-times more active as an inhibitor of phosphatidic acid formation. Purity is approximately 98% by TLC.
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| References | |
| Additional Infomation |
1-(5-hydroxyhexyl)-3,7-dimethyl-3,7-dihydro-1H-purine-2,6-dione is a dimethylxanthine formed by substituting 5-hydroxyhexyl, methyl, and methyl groups at the 1, 3, and 7 positions of 3,7-dihydro-1H-purine-2,6-dione, respectively. It is a secondary alcohol and a dimethylxanthine.
Lisofylline is a synthetic methylxanthine with potent anti-inflammatory activity. It selectively inhibits the formation of phosphatidic acid, a proinflammatory second messenger. The compound has been explored for therapeutic effects in sepsis, autoimmune diseases, and chronic inflammatory disorders. It also enhances glucose-stimulated insulin secretion, suggesting potential applications in diabetes research. |
| Molecular Formula |
C13H20N4O3
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|---|---|
| Molecular Weight |
280.32300
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| Exact Mass |
280.153
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| CAS # |
6493-06-7
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| Related CAS # |
(S)-Lisofylline;100324-80-9;(R)-Lisofylline;100324-81-0;(±)-Lisofylline-d6;1185995-26-9
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| PubChem CID |
57782
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
511.2±56.0 °C at 760 mmHg
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| Melting Point |
123-125ºC
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| Flash Point |
263.0±31.8 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.621
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| LogP |
0.34
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
20
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| Complexity |
390
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NSMXQKNUPPXBRG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C13H20N4O3/c1-9(18)6-4-5-7-17-12(19)10-11(14-8-15(10)2)16(3)13(17)20/h8-9,18H,4-7H2,1-3H3
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| Chemical Name |
1-(5-hydroxyhexyl)-3,7-dimethylpurine-2,6-dione
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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) |
DMSO : ~100 mg/mL (~356.74 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (7.13 mM) (saturation unknown) in 10% DMSO + 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 20.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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: ≥ 2 mg/mL (7.13 mM) (saturation unknown) in 10% DMSO + 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 20.0 mg/mL clear DMSO 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: ≥ 2 mg/mL (7.13 mM) (saturation unknown) in 10% DMSO + 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 | 3.5674 mL | 17.8368 mL | 35.6735 mL | |
| 5 mM | 0.7135 mL | 3.5674 mL | 7.1347 mL | |
| 10 mM | 0.3567 mL | 1.7837 mL | 3.5674 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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