Size | Price | Stock | Qty |
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10mg |
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50mg |
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100mg |
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Zileuton sodium (also known as A-64077 sodium; Abbott-64077; ZYFLO; ZYFLO CR) is a novel, potent and orally bioactive inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes (LTB4, LTC4, LTD4, and LTE4) formation, it was introduced in 1996 to decrease the symptoms of asthma. Zileuton suppresses PG biosynthesis by interference with arachidonic acid (AA) release in macrophages. Zileuton significantly reduces PGE2 and 6-keto prostaglandin F1α (PGF1α) levels in activated mouse peritoneal macrophages and in J774 macrophages. Zileuton inhibits PGE2 production in LPS-stimulated human whole blood and suppresses PGE2 and 6-keto PGF1α pleural levels in rat carrageenan-induced pleurisy.
ln Vitro |
When zileuton sodium (A 64077 sodium) was added to anti-CD3-treated cells, IL-2 levels in both treated and untreated cells declined with longer incubation times. By blocking 5-lipoxygenase, zileutonodium (sodium A 64077) may lower IL-2 levels by preventing the synthesis of leukotriene B4, which is an IL-2 inducer [2].
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ln Vivo |
The effect of zileuton sodium (sodium A 64077) (5 mg/kg, p.o.) on lowering NF-κB expression was not significantly affected by COX inhibitors in rats with I/R. Additionally, this group's NF-κB staining levels were noticeably lower. The apoptotic index of I/R rats treated with zileuton (5 mg/kg, orally) can be dramatically decreased. Regarding the rise in serum TNF-α levels in the I/R group, zileuton showed no discernible impact [1]. In the colon and small intestine of APCΔ468, zileutonodium (A 64077 sodium) (1200 mg/kg) suppresses the formation of polyps. In rat polyps, zileuton therapy increases the rate of apoptosis and decreases the rate of proliferation of non-epithelial cells. The small intestine and colon treated with zileuton showed a considerable increase in the amount of apoptotic cells. In zileuton-fed APCΔ468 mice, a decreased proliferation rate may play a major role in the reduction of small intestine and colon polyposis [3].
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References |
[1]. Abueid L, et al. Inhibition of 5-lipoxygenase by zileuton in a rat model of myocardial infarction. Anatol J Cardiol. 2016 Nov 10
[2]. Kuvibidila S, et al. Hydroxyurea and Zileuton Differentially Modulate Cell Proliferation and Interleukin-2 Secretion by Murine Spleen Cells: Possible Implication on the Immune Function and Risk of Pain Crisis in Patients with Sickle Cell Disease. Ochsner [3]. Gounaris E, et al. Zileuton, 5-lipoxygenase inhibitor, acts as a chemopreventive agent in intestinal polyposis, by modulating polyp and systemic inflammation. PLoS One. 2015 Mar 6;10(3):e0121402 |
Molecular Formula |
C11H11N2O2S-.NA+
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Molecular Weight |
258.272
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CAS # |
118569-21-4
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Related CAS # |
Zileuton;111406-87-2;Zileuton-d4;1189878-76-9
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
CC(N([O-])C(N)=O)C1=CC2=CC=CC=C2S1.[Na+]
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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 Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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 | 3.8719 mL | 19.3596 mL | 38.7192 mL | |
5 mM | 0.7744 mL | 3.8719 mL | 7.7438 mL | |
10 mM | 0.3872 mL | 1.9360 mL | 3.8719 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.