Zileuton

Zileuton is an orally active inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes (LTB4, LTC4, LTD4, and LTE4) formation, used to decrease the symptoms of asthma. Zileuton induces apoptosis while inhibits ferroptosis.

CAS No. 111406-87-2

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
20mg	JPY 22000	国内在庫あり
1g	JPY 145500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

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Lipoxygenase阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
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
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生物活性

製品説明

Zileuton is an orally active inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes (LTB4, LTC4, LTD4, and LTE4) formation, used to decrease the symptoms of asthma. Zileuton induces apoptosis while inhibits ferroptosis.

Targets

Ferroptosis ^[6]

5-lipoxygenase ^[1]

In Vitro
In vitro	Zileuton suppresses PG biosynthesis by interference with arachidonic acid (AA) release in macrophages. Zileuton significantly reduces PGE2 and 6-keto prostaglandin F1α (PGF1α) levels in activated mouse peritoneal macrophages and in J774 macrophages. Zileuton inhibits PGE2 production in LPS-stimulated human whole blood and suppresses PGE2 and 6-keto PGF1α pleural levels in rat carrageenan-induced pleurisy. ^[1]

In Vivo
In Vivo	Zileuton significantly reduces macroscopic damage score after four weeks of treatment in rats. Zileuton administration significantly increases the intracolonic release of both thromboxane B2 at week 1 and prostaglandin E2 at weeks 2 and 4 in rats. ^[2] Zileuton reduces the spinal cord inflammation and tissue injury, neutrophil infiltration, TNF-alpha, COX-2 and pERK1/2 expression, PGE(2) and LTB(4) production, and apoptosis in mice. Zileuton significantly improves the recovery of limb function over 10 days in mice.^[3] Zileuton administrated before I/R significantly reduces the degree of renal dysfunction (urea, creatinine) and injury (AST, histology) in 5-lipoxygenase knockout mice. Zileuton reduces the expression of ICAM-1 and the associated PMN infiltration caused by I/R of the mouse kidney in 5-lipoxygenase knockout mice. ^[4] Zileuton inhibits LTB(4) production in the peritonitis model more effectively than the LTA(4)H inhibitor, but the influx of neutrophils into the peritoneum after 1 and 2 hours is significantly higher in Zileuton- versus JNJ-26993135-treated mice. ^[5]

In Vivo

Zileuton significantly reduces macroscopic damage score after four weeks of treatment in rats. Zileuton administration significantly increases the intracolonic release of both thromboxane B2 at week 1 and prostaglandin E2 at weeks 2 and 4 in rats. ^[2] Zileuton reduces the spinal cord inflammation and tissue injury, neutrophil infiltration, TNF-alpha, COX-2 and pERK1/2 expression, PGE(2) and LTB(4) production, and apoptosis in mice. Zileuton significantly improves the recovery of limb function over 10 days in mice.^[3]

Zileuton administrated before I/R significantly reduces the degree of renal dysfunction (urea, creatinine) and injury (AST, histology) in 5-lipoxygenase knockout mice. Zileuton reduces the expression of ICAM-1 and the associated PMN infiltration caused by I/R of the mouse kidney in 5-lipoxygenase knockout mice. ^[4]

Zileuton inhibits LTB(4) production in the peritonitis model more effectively than the LTA(4)H inhibitor, but the influx of neutrophils into the peritoneum after 1 and 2 hours is significantly higher in Zileuton- versus JNJ-26993135-treated mice. ^[5]

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-01-11)
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

参考
[1] Rossi A1, et al. Br J Pharmacol, 2010, 161(3), 555-570. [2] Bertr醤 X, et al. Gut, 1996, 38(6), 899-904. [3] Genovese T, et al. Br J Pharmacol, 2008, 153(3), 568-582. [4] Patel NS, et al. Mol Pharmacol, 2004, 66(2), 220-227. [5] Rao NL, et al. J Pharmacol Exp Ther, 2007, 321(3), 1154-1160. [6] Yang Liu, et al. Biol Pharm Bull . 2015;38(8):1234-9. + 展開

参考

+ 展開

化学情報

分子量	236.29	化学式	C₁₁H₁₂N₂O₂S
CAS No.	111406-87-2	SDF	Download Zileuton SDFをダウンロードする
Smiles	CC(C1=CC2=CC=CC=C2S1)N(C(=O)N)O
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 47 mg/mL ( (198.9 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 47 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):