Zileuton
别名: A-64077 中文名称：齐留通
Zileuton是一种口服有效的5-脂氧合酶5-lipoxygenase抑制剂，从而抑制白三烯（LTB 4，LTC 4，LTD 4和LTE 4）的形成，用来缓解哮喘的症状。Zileuton 可诱导凋亡而抑制铁死亡。
Zileuton Chemical Structure
CAS: 111406-87-2
产品质控
批次：
纯度：
99.98%
99.98
Zileuton相关产品
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细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| RAW264.7 | Function assay | 5 uM | 24 hrs | Inhibition of LPS/IFNgamma-stimulated lipid peroxidation in mouse RAW264.7 cells at 5 uM after 24 hrs by BODIPY 581/591 C11-staining based FACS assay | 30964295 |
| RAW264.7 | Function assay | 5 uM | 48 hrs | Protection against LPS-induced cell death in mouse RAW264.7 cells assessed as increase in cell viability at 5 uM measured after 48 hrs by MTS assay relative to control | 30964295 |
| HEK293 | Function assay | 1 uM | 5 mins | Inhibition of human 5-LO transfected in HEK293 cells coexpressing FLAP assessed as reduction in leukotriene formation at 1 uM using arachidonic acid as substrate preincubated for 5 mins followed by calcium ionophore A23187/arachidonic acid addition and me | 31260889 |
| PMNL | Function assay | 1 uM | 5 mins | Inhibition of 5-LO in human PMNL cells assessed as reduction in leukotriene formation at 1 uM preincubated for 5 mins followed by thapsigargin stimulation measured after 15 mins by RP-HPLC analysis relative to control | 31260889 |
| PMNL | Function assay | 15 mins | Inhibition of 5-lipoxygenase in cell free S100 freshly isolated human PMNL cells assessed as inhibition of A23187-stimulated 5-LO product formation preincubated for 15 mins measured after 10 mins by HPLC analysis, IC50=0.5μM | 22551629 | |
| BMM | Function assay | 30 mins | Inhibition of 5-LO in mouse BMM cells assessed as formation of LTC4 after 30 mins by enzyme immunoassay, IC50=0.19μM | 26432605 | |
| A549 | Function assay | 15 mins | Inhibition of mPGES-1 isolated from microsomes of interleukin-1 beta-stimulated human A549 cells using PGH2 as substrate preincubated for 15 mins followed by substrate addition measured after 1 min by RP-HPLC analysis, IC50=0.6μM | 30053720 | |
| PMNL | Function assay | 5 mins | Inhibition of 5-LO in human PMNL cells assessed as reduction in leukotriene formation preincubated for 5 mins followed by thapsigargin stimulation measured after 15 mins by RP-HPLC analysis, IC50=2.31μM | 31260889 | |
| BL21 (DE3) | Function assay | 10 mins | Inhibition of recombinant human 5-lipoxygenase expressed in Escherichia coli BL21 (DE3) cells using arachidonic acid as substrate preincubated for 10 mins followed by susbtrate addition and measured after 10 mins by reverse phase HPLC method, IC50=0.5μM | 31465225 | |
| insect cells | Function assay | 5 mins | Inhibition of human recombinant 5-LOX expressed in insect cells assessed as decrease in production of 5-HPETE and 5-HETE using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 20 mins in dark by ferric io, IC50=23.9μM | 31774676 | |
| Sf21 | Function assay | 4 mins | Inhibition of rat 5-LOX expressed in Sf21 insect cells preincubated for 4 mins followed by AA substrate addition and measured after 4 mins by FOX assay, IC50=0.18μM | ChEMBL | |
| RBI-1 | Function assay | In vitro inhibition of 5-lipoxygenase (5-lo) from the 20000 g supernatant of RBI-1 cells, IC50=0.6μM | 2066989 | ||
| RBL-1 | Function assay | Inhibitory concentration against 5-lipoxygenase in rat RBL-1 cells, IC50=3.2μM | 8831759 | ||
| basophilic leukemia cells | Function assay | Inhibitory activity against 5-lipoxygenase obtained from rat basophilic leukemia cells, IC50=0.5μM | 9484493 | ||
| RBL-2H3 | Function assay | Inhibition of 5-lipoxygenase mediated conversion of [14C]arachidonic acid to leukotrienes in RBL-2H3 cells, IC50=0.804μM | 9599246 | ||
| granulocytes-type cells | Function assay | The compound was evaluated for its inhibitory activity against 5-lipoxygenase using granulocytes-type cells, IC50=2.9μM | 11859001 | ||
| polymorphonuclear cells | Antileukotrienic assay | Antileukotrienic activity in rat polymorphonuclear cells assessed as inhibition of LTB4 biosynthesis, IC50=0.01μM | 17448575 | ||
| MC9 | Function assay | Inhibition of LTB4 production in mouse MC9 cells, IC50=0.55μM | 18498150 | ||
| MC9 | Function assay | Inhibition of leukotrienes production in mouse MC9 cells | 18498150 | ||
| RBL-2H3 | Function assay | Inhibition of 5-Lipoxygenase of rat basophilic leukemia cells, IC50=0.14μM | ChEMBL | ||
| RBL-2H3 | Function assay | In vitro inhibition of 5-lipoxygenase in RBL-2H3 (Rat basophilic leukemia) cells, IC50=1.25μM | ChEMBL | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Zileuton是一种口服有效的5-脂氧合酶5-lipoxygenase抑制剂，从而抑制白三烯（LTB 4，LTC 4，LTD 4和LTE 4）的形成，用来缓解哮喘的症状。Zileuton 可诱导凋亡而抑制铁死亡。 | ||
|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 在巨噬细胞中，Zileuton过干扰花生四烯酸（AA）的释放来抑制PG生物合成。在活化的小鼠腹腔巨噬细胞和巨噬细胞J774中，Zileuton显著降低PGE2和6酮前列腺素F1α（PGF1α）水平。在LPS刺激的人全血中，Zileuton抑制PGE2产生与抑制PGE2。在大鼠角叉菜胶诱导的胸膜炎中，Zileuton抑制PGE2和6-酮前列腺素F1α胸膜水平。[1] |
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|---|---|---|---|---|
| 体内研究(In Vivo) | ||
| 体内研究活性 | 在大鼠中，Zileuton治疗4周后显著降低宏观损伤评分。在大鼠结肠内，Zileuton显著增加血栓素B2在1周的释放和前列腺素E2在周2和4的释放。[2] 在小鼠中，Zileuton减小脊髓炎症和组织损伤，中性粒细胞浸润，肿瘤坏死因子-α，COX-2和磷酸化ERK1/2的表达，前列腺素E（2）和LTB（4）的生产。在小鼠中，Zileuton显著改善肢体功能的恢复10天。[3] 在5脂氧合酶基因敲除小鼠中，Zileuton在I/R之前给药显著降低肾功能不全（尿素，肌酐）和损伤（AST，组织学）的程度。在5脂氧合酶基因敲除小鼠的肾中，Zileuton降低ICAM-1的表达和I/R的相关联的中性粒细胞浸润。[4] 在Zileuton和JNJ-26993135处理的小鼠中，Zileuton更有效地抑制白三烯B（4）的产生，和嗜中性粒细胞的流入。[5] |
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|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT01136941 | Completed | Sickle Cell Disease |
Children''s Hospital Medical Center Cincinnati |
September 2010 | Phase 1 |
| NCT01130688 | Terminated | Chronic Myelogenous Leukemia |
University of Massachusetts Worcester |
January 2010 | Phase 1 |
化学信息&溶解度
| 分子量 | 236.29 | 分子式 | C11H12N2O2S |
| CAS号 | 111406-87-2 | SDF | Download Zileuton SDF |
| Smiles | CC(C1=CC2=CC=CC=C2S1)N(C(=O)N)O | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 47 mg/mL ( (198.9 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Ethanol : 47 mg/mL (198.9 mM) Water : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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