CAS:111406-87-2
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:HPLC≥98%
Appearance:White to off-white Solid
Zileuton是一类选择性的5-脂氧合酶抑制剂。
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ZileutonCAS:111406-87-2
Storage:Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year
Purity:HPLC≥98%
Appearance:White to off-white Solid
CAS | 111406-87-2 |
Chinese Name | 齐留通 |
English Name | Zileuton |
Synonyms | 齐留通;N-羟基-N-(1-苯并噻吩-2-基-乙基)脲;Thifluzamide(Bsi,Iso,Ansi);ThifluzamideStandard;2,6-Diobromo-2-Methyl-4 |
Molecular Formula | C11H12N2O2S |
Molecular Weight | 236.29 |
Solubility | Soluble in DMSO |
Purity | HPLC≥98% |
Appearance | White to off-white Solid |
Storage | Powder:2-8℃,2 years;Insolvent(Mother Liquid):-20℃,6 months;-80℃,1 year |
EC | EINECS 601-087-3 |
MDL | MFCD00866097 |
SMILES | CC(N(O)C(N)=O)C1=CC2=CC=CC=C2S1 |
InChIKey | MWLSOWXNZPKENC-UHFFFAOYSA-N |
InChI | InChI=1S/C11H12N2O2S/c1-7(13(15)11(12)14)10-6-8-4-2-3-5-9(8)16-10/h2-7,15H,1H3,(H2,12,14) |
PubChem CID | 60490 |
Target Point | 5-Lipoxygenase |
Passage | Metabolic Enzyme&Protease |
Background | Zileuton is a class of selective 5-lipoxygenase inhibitors. |
Biological Activity | Zileuton是有效,选择性的5-脂氧合酶抑制剂,具有抗哮喘活性。[1-3] |
In Vitro | 在抗CD3处理的细胞中,随着孵育时间的增加,在齐留通处理和未处理的细胞中IL-2减少。 Zileuton可能通过抑制5-脂氧合酶来降低IL-2水平,因此白三烯B4的产生是一种IL-2诱导剂[2]。 |
In Vivo | 在齐留通(5mg / kg,口服)处理的I / R大鼠中,在COX抑制剂存在下,齐留通降低NF-κB表达的作用没有显着变化,并且该组显示出显着较低水平的NF-κB染色。给予I / R大鼠的齐留通(5mg / kg,口服)治疗显着降低细胞凋亡指数。 Zileuton对I / R组血清TNF-α水平升高没有显着影响[1]。 Zileuton(1,200 mg / kg)抑制APCΔ468结肠和小肠中的息肉形成。 Zileuton治疗抑制息肉中非上皮细胞的增殖,增加大鼠息肉的凋亡率。在小肠和结肠中,Zileuton处理的细胞中凋亡细胞的数量显着增加。降低的增殖率可能显着有助于减少Zileuton喂养的APCΔ468小鼠的小肠和结肠中的息肉[3]。 |
Animal Experiment | 大鼠:将大鼠随机分为6组(每组n = 12):假I / R组,I / R组,齐留通+ I / R组,齐留通+吲哚美辛+ I / R组,齐留通+酮咯酸+ I / R组和齐留通+尼美舒利+ I / R组。 5-LOX抑制剂齐留通(5 mg / kg,每日口服两次)单独给予或与非选择性COX抑制剂吲哚美辛(5 mg / kg,腹腔注射),选择性COX-1抑制剂酮咯酸(10 mg / kg,口服)或选择性COX-2抑制剂尼美舒利(10mg / kg,皮下注射)。在齐留通给药前15分钟给予COX抑制剂。在I / R或假I / R程序之前给予所有药物3天。在该研究中使用齐留通剂量(5mg / kg,每天两次)。假I / R组的大鼠口服接受齐留通的载体。将Zileuton溶解在二甲基亚砜(DMSO)中,并使用盐水进一步稀释以达到最终DMSO浓度为1%。 |
Data Literature Source | [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 |
Unit | Bottle |
Specification | 10mg 10mM*1mL in DMSO 50mg |
Zileuton是一类选择性的5-脂氧合酶抑制剂。