Zileuton
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| カタログ番号GC16014 |
ジリュートンは、抗喘息特性を持つ 5-リポキシゲナーゼの強力かつ選択的な阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 111406-87-2
Sample solution is provided at 25 µL, 10mM.
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Zileuton, a benzothiophene N-hydroxyurea, is an oral inhibitor of 5-Lipoxygenase[1]. Zileuton blocks 5-lipoxygenase activity to regulate leukotriene formation and reduces bronchial smooth-muscle tone[2]. Zileuton is a weak inhibitor of human liver microsomal CYP3A4, CYP2C9, and CYP2D6 activity, with IC50 >100μM [3]. Zileuton has been widely used in animal models to suppress inflammation and improve airway function[4].
In vitro, Zileuton treatment at 0.05μM Zileuton for 14 days reduced the content of neutral lipids and the release of interleukin-6 in human SZ95 sebocytes[5]. Treatment with 100µM Zileuton for 24h inhibited the lipopolysaccharide (LPS)-triggered increase in PGE2 production in mouse J774 macrophages without affecting cell viability[6]. Treatment with 50µM Zileuton for 1 hour significantly inhibited the proliferation and migration of human umbilical vein endothelial cells (HUVEC) induced by vascular endothelial growth factor (VEGF)[7].
In vivo, Zileuton treatment (50mg/kg; twice daily; p.o.) for 7 days alleviated colonic injury and decreased colonic myeloperoxidase (MPO) activity in an experimental model of rat colitis[8]. Oral administration of drinking water containing Zileuton (200mg/L) daily for 3 months can restore the memory impairment in aged mice with Alzheimer's disease and reverse the amyloid protein and tau pathological changes[9]. A single oral dose of Zileuton at 50mg/kg for 72 hours can inhibit neuronal apoptosis in rats after focal cerebral ischemia and alleviate brain damage[10].
References:
[1] Berger W, De Chandt M T M, Cairns C B. Zileuton: clinical implications of 5‐Lipoxygenase inhibition in severe airway disease[J]. International journal of clinical practice, 2007, 61(4): 663-676.
[2] Bell R L, Young P R, Albert D, et al. The discovery and development of zileuton: an orally active 5-lipoxygenase inhibitor[J]. International journal of immunopharmacology, 1992, 14(3): 505-510.
[3] Lu P, Schrag M L, Slaughter D E, et al. Mechanism-based inhibition of human liver microsomal cytochrome P450 1A2 by zileuton, a 5-lipoxygenase inhibitor[J]. Drug Metabolism and Disposition, 2003, 31(11): 1352-1360.
[4] Muthukrishnan P T, Nouraie M, Parikh A, et al. Zileuton use and phenotypic features in asthma[J]. Pulmonary Pharmacology & Therapeutics, 2020, 60: 101872.
[5] Zouboulis C C. Zileuton, a new efficient and safe systemic anti-acne drug[J]. Dermato-endocrinology, 2009, 1(3): 188-192.
[6] Rossi A, Pergola C, Koeberle A, et al. The 5-lipoxygenase inhibitor, zileuton, suppresses prostaglandin biosynthesis by inhibition of arachidonic acid release in macrophages[J]. British journal of pharmacology, 2010, 161(3): 555-570.
[7] Lim H J, Park J, Um J Y, et al. Zileuton, a 5-lipoxygenase inhibitor, exerts anti-angiogenic effect by inducing apoptosis of HUVEC via BK channel activation[J]. Cells, 2019, 8(10): 1182.
[8] Zingarelli B, Squadrito F, Graziani P, et al. Effects of zileuton, a new 5-lipoxygenase inhibitor, in experimentally induced colitis in rats[J]. Agents and actions, 1993, 39(3): 150-156.
[9] Di Meco A, Lauretti E, Vagnozzi A N, et al. Zileuton restores memory impairments and reverses amyloid and tau pathology in aged Alzheimer's disease mice[J]. Neurobiology of aging, 2014, 35(11): 2458-2464.
[10] Shi S, Yang W, Tu X, et al. 5-Lipoxygenase inhibitor zileuton inhibits neuronal apoptosis following focal cerebral ischemia[J]. Inflammation, 2013, 36(6): 1209-1217.
| Cell experiment [1]: | |
Cell lines | Mouse J774 macrophages |
Preparation Method | Mouse J774 macrophages were cultured in DMEM medium supplemented with 2000µM glutamine, 25000µM HEPES, 100U/mL penicillin, 100µg/mL streptomycin, 10% FBS, and 1.2% sodium pyruvate. Cells were seeded in 24-well culture plates at a density of 2.5×105 cells/mL and incubated in a 5% CO2 incubator at 37°C for 2 hours in adherent culture. Cells were stimulated with LPS (10µg/mL) for 24h in the presence or absence of Zileuton (0, 1, 3.3, 10, 33, and 100µM), PGE2 levels were measured in cell supernatants. |
Reaction Conditions | 0, 1, 3.3, 10, 33, and 100µM; 24h |
Applications | Zileuton significantly inhibited the PGE2 generation induced by LPS within J774 macrophages in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | C57BL/B6 APCΔ468 mice |
Preparation Method | Four-week-old C57BL/B6 APCΔ468 mice were housed under standard conditions and fed AIN93G diet with or without 1200mg/kg daily Zileuton homogeneous particles (8 mice per group) for 3 months, and mice were sacrificed at 4 months of age and intestinal tissues were collected for analysis. |
Dosage form | 1200mg/kg/day for 3 months; p.o. |
Applications | Zileuton treatment significantly inhibited intestinal polyp development and inflammation in mice. |
References: | |
| Cas No. | 111406-87-2 | SDF | |
| 同義語 | A 64077 | ||
| Chemical Name | 1-[1-(1-benzothiophen-2-yl)ethyl]-1-hydroxyurea | ||
| Canonical SMILES | CC(C1=CC2=CC=CC=C2S1)N(C(=O)N)O | ||
| Formula | C11H12N2O2S | M.Wt | 236.29 |
| 溶解度 | ≥ 13.3mg/mL in DMSO, ≥ 12.73 mg/mL in EtOH | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 4.2321 mL | 21.1604 mL | 42.3209 mL |
| 5 mM | 846.4 μL | 4.2321 mL | 8.4642 mL |
| 10 mM | 423.2 μL | 2.116 mL | 4.2321 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 25 reference(s) in Google Scholar.)
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