Zileuton

製品コードS1443 バッチS144304

印刷

化学情報

Synonyms

A-64077

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₁₁H₁₂N₂O₂S

分子量

236.29

CAS No.

111406-87-2

Solubility (25°C)*

体外

DMSO

47 mg/mL (198.9 mM)

Ethanol

30 mg/mL (126.96 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Clear solution

5%DMSO 1 Corn oil

1.0mg/ml

Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

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.
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	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]

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.

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

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]

プロトコル(参考用のみ)

参考

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カスタマーフィードバック

: Data from [Data independently produced by , , JCI Insight, 2017, 2(3):e88588]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

ALOX5 acts as a key role in regulating the immune microenvironment in intrahepatic cholangiocarcinoma, recruiting tumor-associated macrophages through PI3K pathway [ J Transl Med, 2023, 21(1):923]	PubMed: 38124204
Phospholipid metabolic adaptation promotes survival of IDH2 mutant acute myeloid leukemia cells [ Cancer Sci, 2023, 10.1111/cas.15994]	PubMed: 37882467
Synergistic Renoprotective Effect of Melatonin and Zileuton by Inhibition of Ferroptosis via the AKT/mTOR/NRF2 Signaling in Kidney Injury and Fibrosis [ Biomol Ther (Seoul), 2023, 10.4062/biomolther.2023.062]	PubMed: 37183002
Phospholipid peroxidation inhibits autophagy via stimulating the delipidation of oxidized LC3-PE [ Redox Biol, 2022, 55:102421]	PubMed: 35964342
Inhibiting 5-lipoxygenase prevents skeletal muscle atrophy by targeting organogenesis signalling and insulin-like growth factor-1 [ J Cachexia Sarcopenia Muscle, 2022, 13(6):3062-3077]	PubMed: 36221153
Inhibiting 5-lipoxygenase prevents skeletal muscle atrophy by targeting organogenesis signalling and insulin-like growth factor-1 [ J Cachexia Sarcopenia Muscle, 2022, 13(6):3062-3077]	PubMed: 36221153
Arachidonic acid drives adaptive responses to chemotherapy-induced stress in malignant mesothelioma [ J Exp Clin Cancer Res, 2021, 40(1):344]	PubMed: 34727953
PE_PGRS31-S100A9 Interaction Promotes Mycobacterial Survival in Macrophages Through the Regulation of NF-κB-TNF-α Signaling and Arachidonic Acid Metabolism [ Front Microbiol, 2020, 11:845]	PubMed: 32457723
AGER-Mediated Lipid Peroxidation Drives Caspase-11 Inflammasome Activation in Sepsis. [ Front Immunol, 2019, 10:1904]	PubMed: 31440260
Corticosteroids inhibit anti-IgE activities of specialized proresolving mediators on B cells from asthma patients. [Kim N, et al. JCI Insight, 2017, 2(3):e88588]	PubMed: 28194434

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。