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Metabolism
Lipoxygenase inhibitor
-
Apoptosis related activator
-
Ferroptosis inhibitor
Zileuton
僅限科研使用
Zileuton
別名: A-64077 中文名稱：齊留通
Zileuton是一種口服有效的5-脂氧合酶5-lipoxygenase抑制劑，從而抑制白三烯（LTB 4，LTC 4，LTD 4和LTE 4）的形成，用來緩解哮喘的癥狀。Zileuton 可誘導凋亡而抑制鐵死亡。
Zileuton Chemical Structure
CAS: 111406-87-2
產(chǎn)品質(zhì)控
批次：
純度：
99.98%
99.98
Zileuton相關產(chǎn)品
| 相關產(chǎn)品 | ML355 PD146176 Malotilate AKBA (3-O-Acetyl-11-keto-β-boswellic acid) Demethylnobiletin Esculetin | 點擊展開 |
|---|---|---|
| 相關化合物庫 | 代謝化合物庫 抗癌代謝化合物庫 谷氨酰胺代謝化合物庫 糖代謝化合物庫 脂代謝化合物庫 | 點擊展開 |
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
生物活性
| 產(chǎn)品描述 | Zileuton是一種口服有效的5-脂氧合酶5-lipoxygenase抑制劑，從而抑制白三烯（LTB 4，LTC 4，LTD 4和LTE 4）的形成，用來緩解哮喘的癥狀。Zileuton 可誘導凋亡而抑制鐵死亡。 | ||
|---|---|---|---|
| 靶點 |
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| 體外研究(In Vitro) | ||||
| 體外研究活性 | 在巨噬細胞中，Zileuton過干擾花生四烯酸（AA）的釋放來抑制PG生物合成。在活化的小鼠腹腔巨噬細胞和巨噬細胞J774中，Zileuton顯著降低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產(chǎn)生與抑制PGE2。在大鼠角叉菜膠誘導的胸膜炎中，Zileuton抑制PGE2和6-酮前列腺素F1α胸膜水平。[1] |
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|---|---|---|---|---|
| 體內(nèi)研究(In Vivo) | ||
| 體內(nèi)研究活性 | 在大鼠中，Zileuton治療4周后顯著降低宏觀損傷評分。在大鼠結(jié)腸內(nèi)，Zileuton顯著增加血栓素B2在1周的釋放和前列腺素E2在周2和4的釋放。[2] 在小鼠中，Zileuton減小脊髓炎癥和組織損傷，中性粒細胞浸潤，腫瘤壞死因子-α，COX-2和磷酸化ERK1/2的表達，前列腺素E（2）和LTB（4）的生產(chǎn)。在小鼠中，Zileuton顯著改善肢體功能的恢復10天。[3] 在5脂氧合酶基因敲除小鼠中，Zileuton在I/R之前給藥顯著降低腎功能不全（尿素，肌酐）和損傷（AST，組織學）的程度。在5脂氧合酶基因敲除小鼠的腎中，Zileuton降低ICAM-1的表達和I/R的相關聯(lián)的中性粒細胞浸潤。[4] 在Zileuton和JNJ-26993135處理的小鼠中，Zileuton更有效地抑制白三烯B（4）的產(chǎn)生，和嗜中性粒細胞的流入。[5] |
|
|---|---|---|
| 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 |
化學信息&溶解度
| 分子量 | 236.29 | 分子式 | C11H12N2O2S |
| CAS號 | 111406-87-2 | SDF | Download Zileuton SDF |
| Smiles | CC(C1=CC2=CC=CC=C2S1)N(C(=O)N)O | ||
| 儲存條件(自收到貨起) | |||
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體外溶解度 |
DMSO : 47 mg/mL ( (198.9 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Ethanol : 47 mg/mL (198.9 mM) Water : Insoluble |
摩爾濃度計算器 |
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體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(jié)果：
工作液濃度： mg/ml；
DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；
體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。
體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。
注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。
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