Zileuton sodium5-lipoxygenase and leukotrienes inhibitor CAS# 118569-21-4 |
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Quality Control & MSDS
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| 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. |
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| 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. |
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| 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. | ||
| Description | Zileuton 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: | |||||
Zileuton sodium Dilution Calculator
Zileuton sodium Molarity Calculator
| 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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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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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.
