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Zileuton/齐留通 {[allProObj[0].p_purity_real_show]}

货号：A202709 同义名： 齐留通(Zileuton) / A 64077; Abbott 64077

Zileuton是一种可逆的 5-脂氧合酶抑制剂，在大鼠嗜碱性白血病-1（RBL-1）细胞中的 IC50 值为 0.5 µM。它还具有显著的抑制白三烯 B4 产生的作用，IC50 值为 0.6 µM。

Zileuton/齐留通 化学结构 CAS号：111406-87-2
Zileuton/齐留通 化学结构
CAS号：111406-87-2
Zileuton/齐留通 3D分子结构
CAS号：111406-87-2
Zileuton/齐留通 化学结构 CAS号：111406-87-2
Zileuton/齐留通 3D分子结构 CAS号：111406-87-2
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Zileuton/齐留通 纯度/质量文件 产品仅供科研

货号：A202709 标准纯度： {[allProObj[0].p_purity_real_show]}
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产品名称 lipoxygenase ↓ 其他靶点 纯度
Zileuton ✔ 97%
Nordihydroguaiaretic acid ✔ 99%+
MK-886 ✔ 99%+
Esculetin ✔ 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Zileuton/齐留通 生物活性

靶点

  • lipoxygenase
描述 Leukotrienes (LT) are metabolites of arachidonic acid (AA) formed from the 5-lipoxygenase (5-LOX) pathway. They exhibit a number of biological effects such as contraction of smooth muscles, especially bronchoconstriction, increased vascular permeability, and migration of leukocytes to areas of inflammation. Zileuton is a potent and selective inhibitor of 5-lipoxygenase with antiasthmatic properties[3]. In macrophages, zileuton overinterfered with arachidonic acid (AA) release to inhibit PG biosynthesis. In activated mouse peritoneal macrophages and macrophage J774, zileuton significantly reduces PGE2 and 6-ketone prostaglandin F1α (PGF1α) levels[4]. In anti-CD3-treated cells, IL-2 decreased in zileuton-treated and untreated cells with increasing incubation time. Zileuton likely reduced IL-2 levels by inhibiting 5-lipoxygenase[3]. Zileuton treatement on rats with TNB colitis, however, showed a significant reduction in the macroscopic damage score after four weeks of treatment compared with 5-ASA and placebo groups. The intracolonic administration of 50 mg/kg of zileuton after colitis induction decreased the local peak release of LTB4 by 90%[5]. In zileuton (5 mg/kg, p.o.) treated ischemia/reperfusion (I/R) rat, the effect of zileuton to decrease NF-κB expression did not change significantly in the presence of COX inhibitors, and the group revealed significantly lower level of NF-κB staining. Zileuton (5 mg/kg, p.o.) treatment given to I/R rats decreased apoptotic index significantly. In 5-LOX gene knockout mice, administration of zileuton before I/R significantly reduced the degree of renal dysfunction (urea, creatinine) and injury (AST, histology). In addition, zileuton reduced the expression of ICAM-1 and the associated polymorphonuclear leukocyte infiltration caused by I/R of the mouse kidney[6]. Although zileuton inhibited LTB4 production in the peritonitis model more effectively than the LTA4H inhibitor, the influx of neutrophils into the peritoneum after 1 and 2h was significantly higher in zileuton- versus JNJ-26993135-treated animals[7].

Zileuton/齐留通 细胞实验

Cell Line
Concentration Treated Time Description References
HUVECs 1–50 µM 1 hour Zileuton significantly inhibited VEGF-induced proliferation of HUVECs, as confirmed by MTT assay and BrdU incorporation assay. Cells. 2019 Sep 30;8(10):1182.
Mouse peritoneal macrophages 1-100 µM 24 hours Zileuton significantly reduced PGE2 and 6-keto PGF1α levels, with an IC50 of 5.79 µM. Br J Pharmacol. 2010 Oct;161(3):555-70.
J774 macrophages 1-100 µM 24 hours Zileuton significantly inhibited PGE2 production, with an IC50 of 1.94 µM. Br J Pharmacol. 2010 Oct;161(3):555-70.
Human whole blood 1-100 µM 24 hours Zileuton significantly inhibited COX-2-dependent PGE2 production, with an IC50 of 12.9 µM. Br J Pharmacol. 2010 Oct;161(3):555-70.
BV-2 cells 5, 10, 15, 20 µM 24 hours To investigate the effect of Zileuton on BV-2 cell viability, results showed that Zileuton at high concentrations (20 µM) could inhibit the over-proliferation of BV-2 cells. Int J Mol Sci. 2022 Apr 28;23(9):4910.
Human dermal fibroblasts (HDFs) 0, 5, 10, 20 µM 24 hours Zileuton treatment significantly reduced 5-LO and SASP levels and inhibited the expression of senescence markers. Int J Mol Sci. 2022 Jul 29;23(15):8390.

Zileuton/齐留通 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Rats Carrageenan-induced pleurisy Intraperitoneal injection 10 mg/kg Single dose, lasting 4 hours Zileuton significantly reduced the levels of LTB4, PGE2, and 6-keto PGF1α in pleural exudates and attenuated the inflammatory response. Br J Pharmacol. 2010 Oct;161(3):555-70.
SKH-1 mice Radiation-induced cutaneous ulcer model Topical application 200 μM Daily until the day of euthanasia Zileuton treatment significantly inhibited 5-LO expression and inflammatory cell infiltration, promoting the healing of radiation ulcers. Int J Mol Sci. 2022 Jul 29;23(15):8390.
Sprague Dawley rats Asthma model Oral gavage 30 mg/kg Once daily for 15 days To evaluate gender differences in the pharmacokinetics of zileuton in a rat model. Results showed that female rats exhibited higher plasma concentrations of zileuton compared to male rats across all forms of zileuton (API, PM, and NfZ). Int J Pharm X. 2024 May 4;7:100254
Wistar albino rats PCOS model Oral 5 mg/kg Twice daily for 15 days Zileuton significantly alleviated inflammation, apoptosis, and ferroptosis in the PCOS rat model, and improved oxidative stress and hormonal levels Redox Rep. 2025 Dec;30(1):2445398
C57BL/6J mice Matrigel plug model Subcutaneous injection 50 µM Once daily for 7 days Zileuton significantly inhibited VEGF-induced angiogenesis in vivo, as confirmed by Matrigel plug assay and hemoglobin content measurement. Cells. 2019 Sep 30;8(10):1182.
CD1 mice Spinal cord injury model Oral 50 mg/kg 1 hour and 6 hours after injury, daily for 10 days To evaluate the effect of Zileuton on inflammation and tissue injury after spinal cord injury. Results showed that Zileuton significantly reduced spinal cord inflammation and tissue injury, and improved the recovery of motor function. Br J Pharmacol. 2008 Feb;153(3):568-82

Zileuton/齐留通 动物研究

Dose Mice: 10 mg/kg[3] (i.p.); 50 mg/kg[4] (p.o.) Rat: 1 mg/kg, 3 mg/kg[5] (i.v.)
Administration i.p., i.v., p.o.

Zileuton/齐留通 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00595114 - Completed - United States, Massachusetts ... 展开 >> Brigham and Women's Hospital Boston, Massachusetts, United States, 02115 收起 <<
NCT00595114 - Completed - -
NCT01125748 - Completed - -

Zileuton/齐留通 参考文献

[1]Rossi A, Pergola C, et al. The 5-lipoxygenase inhibitor, zileuton, suppresses prostaglandin biosynthesis by inhibition of arachidonic acid release in macrophages. Br J Pharmacol. 2010 Oct;161(3):555-70.

[2]Bertran X, Mane J, et al. Intracolonic administration of zileuton, a selective 5-lipoxygenase inhibitor, accelerates healing in a rat model of chronic colitis. Gut. 1996 Jun;38(6):899-904.

[3]Abueid L, Uslu Ü, Cumbul A, Velioğlu Öğünç A, Ercan F, Alican İ. Inhibition of 5-lipoxygenase by zileuton in a rat model of myocardial infarction. Anatol J Cardiol. 2017 Apr;17(4):269-275. doi: 10.14744/AnatolJCardiol.2016.7248. Epub 2016 Nov 10. PMID: 27849187; PMCID: PMC5469106.

[4]Rossi A, Pergola C, Koeberle A, Hoffmann M, Dehm F, Bramanti P, Cuzzocrea S, Werz O, Sautebin L. The 5-lipoxygenase inhibitor, zileuton, suppresses prostaglandin biosynthesis by inhibition of arachidonic acid release in macrophages. Br J Pharmacol. 2010 Oct;161(3):555-70. doi: 10.1111/j.1476-5381.2010.00930.x. PMID: 20880396; PMCID: PMC2990155.

[5]Bertrán X, Mañé J, Fernández-Bañares F, Castellá E, Bartolí R, Ojanguren I, Esteve M, Gassull MA. Intracolonic administration of zileuton, a selective 5-lipoxygenase inhibitor, accelerates healing in a rat model of chronic colitis. Gut. 1996 Jun;38(6):899-904. doi: 10.1136/gut.38.6.899. PMID: 8984030; PMCID: PMC1383199.

[6]Patel NS, Cuzzocrea S, Chatterjee PK, Di Paola R, Sautebin L, Britti D, Thiemermann C. Reduction of renal ischemia-reperfusion injury in 5-lipoxygenase knockout mice and by the 5-lipoxygenase inhibitor zileuton. Mol Pharmacol. 2004 Aug;66(2):220-7. doi: 10.1124/mol.66.2.220. PMID: 15266012.

[7]Rao NL, Dunford PJ, Xue X, Jiang X, Lundeen KA, Coles F, Riley JP, Williams KN, Grice CA, Edwards JP, Karlsson L, Fourie AM. Anti-inflammatory activity of a potent, selective leukotriene A4 hydrolase inhibitor in comparison with the 5-lipoxygenase inhibitor zileuton. J Pharmacol Exp Ther. 2007 Jun;321(3):1154-60. doi: 10.1124/jpet.106.115436. Epub 2007 Mar 19. PMID: 17371808.

Zileuton/齐留通 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.23mL

0.85mL

0.42mL

21.16mL

4.23mL

2.12mL

42.32mL

8.46mL

4.23mL

Zileuton/齐留通 技术信息

CAS号111406-87-2
分子式C11H12N2O2S
分子量 236.29
SMILES Code CC(N(O)C(N)=O)C1=CC2=CC=CC=C2S1
MDL No. MFCD00866097
别名 齐留通(Zileuton) ;A 64077; Abbott 64077
运输蓝冰
InChI Key MWLSOWXNZPKENC-UHFFFAOYSA-N
Pubchem ID 60490
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place, sealed in dry, room temperature
溶解方案

DMSO: 105 mg/mL(444.37 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配，短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。
方案 一

Tags: Zileuton | 111406-87-2 | A 64077 | Abbott 64077 | A64077 | A-64077 | Abbott64077 | Abbott 64077 | Abbott-64077 | 5-Lipoxygenase Inhibitor | Metabolic Enzyme/Protease | Apoptosis | Lipoxygenase | Ferroptosis | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Zileuton/齐留通 纯度/质量文件 | Zileuton/齐留通 亚型比较 | Zileuton/齐留通 生物活性 | Zileuton/齐留通 动物研究 | Zileuton/齐留通 临床数据 | Zileuton/齐留通 参考文献 | Zileuton/齐留通 实验方案 | Zileuton/齐留通 技术信息

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