Zileuton sodium

5-lipoxygenase and leukotrienes inhibitor CAS# 118569-21-4

Zileuton sodium

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Chemical structure

Zileuton sodium

3D structure

Chemical Properties of Zileuton sodium

Cas No. 118569-21-4 SDF Download SDF
PubChem ID 78357785 Appearance Powder
Formula C11H11N2NaO2S M.Wt 258.27
Type of Compound N/A Storage Desiccate at -20°C
Solubility Soluble in DMSO
Chemical Name sodium;1-[1-(1-benzothiophen-2-yl)ethyl]-1-oxidourea
SMILES CC(C1=CC2=CC=CC=C2S1)N(C(=O)N)[O-].[Na+]
Standard InChIKey USURPRPAYRQEOV-UHFFFAOYSA-N
Standard InChI InChI=1S/C11H11N2O2S.Na/c1-7(13(15)11(12)14)10-6-8-4-2-3-5-9(8)16-10;/h2-7H,1H3,(H2,12,14);/q-1;+1
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Zileuton sodium

DescriptionZileuton sodium is a potent and selective inhibitor of 5-lipoxygenase, exhibiting inflammatory activities.In Vitro:In anti-CD3-treated cells, IL-2 decreases in zileuton-treated and untreated cells with increasing incubation time. Zileuton likely reduces IL-2 levels by inhibiting 5-lipoxygenase, hence leukotriene B4 production, an IL-2 inducer[2].In Vivo:In zileuton (5 mg/kg, p.o.) treated I/R rat, the effect of zileuton to decrease NF-κB expression does not change significantly in the presence of COX inhibitors, and the group reveals significantly lower level of NF-κB staining. Zileuton (5 mg/kg, p.o.) treatment given to I/R rats decreases apoptotic index significantly. Zileuton has no significant effect on increased serum TNF-α levels in I/R group[1]. Zileuton (1200 mg/kg) inhibits the polyp formation in APCΔ468 colon and small intestine. Zileuton treatment inhibits the proliferation rates of non epithelial cells in polyps, and increases the apoptosis rates in polyps in rat. There is significant increase in the number of apoptotic cells in the Zileuton-treated cells both in small intestine and in the colon. The reduced proliferation rate may significantly contribute to the reduction of polyposis in both the small intestine and colon of Zileuton-fed APCΔ468 mice[3].

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.

Protocol

Animal Administration [1]
Rats: Rats are randomized into 6 groups (n=12 per group): sham I/R group, I/R group, zileuton+I/R group, zileuton+indomethacin+I/R group, zileuton+ketorolac+I/R group, and zileuton+nimesulide+I/R group. 5-LOX inhibitor zileuton (5 mg/kg, orally twice daily) is given alone or with non-selective COX inhibitor indomethacin (5 mg/kg, intraperitoneally), selective COX-1 inhibitor ketorolac (10 mg/kg, orally) or selective COX-2 inhibitor nimesulide (10 mg/kg, subcutaneously). COX inhibitors are given 15 minutes before zileuton administration. All drugs are given for 3 days prior to I/R or sham I/R procedure. Dose of zileuton (5 mg/kg, twice daily) is used in this study. Rats in sham I/R group receive the vehicle of zileuton orally. Zileuton is dissolved in dimethyl sulfoxide (DMSO) and further dilutions are made using saline to achieve a final DMSO concentration of 1%.

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.

Zileuton sodium Dilution Calculator

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Zileuton sodium Molarity Calculator

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Preparing Stock Solutions of Zileuton sodium

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 3.8719 mL 19.3596 mL 38.7192 mL 77.4383 mL 96.7979 mL
5 mM 0.7744 mL 3.8719 mL 7.7438 mL 15.4877 mL 19.3596 mL
10 mM 0.3872 mL 1.936 mL 3.8719 mL 7.7438 mL 9.6798 mL
50 mM 0.0774 mL 0.3872 mL 0.7744 mL 1.5488 mL 1.936 mL
100 mM 0.0387 mL 0.1936 mL 0.3872 mL 0.7744 mL 0.968 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Zileuton sodium

Zileuton sodium is an inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes(LTB4, LTC4, LTD4 and LTE4) formation with an IC50 value of 0.5μM [1].

Zileuton sodium has been reported to concentration-dependently inhibit the 5-lipoxygenase activity with an IC50 value of 0.5μM in RBL-1cell lysate. In addition, Zileuton sodium has been found to be a potent inhibitor of LTB formation with an IC50 value of 0.6μM. Furthermore, stimulated with A23187, Zileuton sodium has shown a dose-dependent reduction in LTB4 and 5-HETE generation in rat leukocyte with IC50 values of 0.38μM and 0.31μM, respectively. About 40-fold higher concentrations of Zileuton sodium also reduced the production of PGE2 with a IC50 of 16μM [1].

References:
[1] Carter GW1, Young PR, Albert DH, Bouska J, Dyer R, Bell RL, Summers JB, Brooks DW. 5-lipoxygenase inhibitory activity of zileuton. J Pharmacol Exp Ther. 1991 Mar; 256(3):929-37.

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References on Zileuton sodium

A randomized, comparative, multicentric clinical trial to assess the efficacy and safety of zileuton extended-release tablets with montelukast sodium tablets in patients suffering from chronic persistent asthma.[Pubmed:22926233]

Am J Ther. 2013 Mar-Apr;20(2):154-62.

Leukotriene (LT) modifiers are anti-inflammatory drugs that are useful as an add-on therapy with first-line asthma-controller medications. This group includes LT synthesis inhibitors (eg, Zileuton) and receptor antagonists (eg, Montelukast), whose direct comparative clinical data are not available. This study was conducted to assess the comparative efficacy and safety of orally administered Zileuton extended-release (ER) with Montelukast sodium in patients suffering from chronic persistent asthma. Patients of 18-65 years of age with mild to moderate chronic stable asthma were randomized to treatment with Zileuton ER 2400 mg/d or Montelukast 10 mg/d for 12 weeks. Peak expiratory flow rate (PEFR) and asthma symptoms (cough, wheeze, chest tightness, and shortness of breath each on a 4-point scale) were assessed on monthly scheduled out-patient visits. Safety assessments by clinical and laboratory parameters were carried out during the course of the study. Among 210 patients eligible for efficacy assessment, PEFR improved by 64.8 +/- 52.8 (95% confidence interval: 54.8-74.7) L/min with Zileuton ER (n = 109) and 40.6 +/- 47.5 (31.3-49.9) L/min with Montelukast (n = 101; P < 0.001), whereas percent improvements were 27.0% (22.6%-31.5%) versus 18.4% (14.1%-22.7%), respectively (P = 0.006). Zileuton ER lead to >/=12% PEFR improvements in 74 of 109 [67.9% (59.1%-76.7%)] patients, whereas the same was noted in 52 of 101 [51.5% (41.7%-61.2%)] patients receiving Montelukast (P = 0.015). The reduction in the mean overall symptom intensity score was also significantly better with Zileuton ER [-5.0 +/- 2.1 (4.6-5.4) versus -4.2 +/- 2.3 (3.8-4.7)] (P = 0.018); however, the same was not observed for the decline in the individual symptom scores. A lesser but not significantly different adverse event rate was reported in the Zileuton ER group than the Montelukast group with the commonest events being headache and gastrointestinal effects in both the groups. Thus, Zileuton ER seems to be more efficacious than Montelukast and well tolerated for the treatment of mild to moderate chronic persistent asthma in adult patient population. Further studies can elucidate the comparative treatment benefits of these LT modifiers in asthma management.

Description

Zileuton sodium (A 64077 sodium) is a potent and selective inhibitor of 5-lipoxygenase, exhibiting inflammatory activities.

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