Zileuton

카탈로그 번호S1443 배치:S144305

인쇄

기술 자료

화학식

C11H12N2O2S
분자량 236.29 CAS 번호 111406-87-2
용해도 (25°C)* 시험관 내(In vitro) DMSO 47 mg/mL (198.9 mM)
Ethanol 47 mg/mL (198.9 mM)
Water Insoluble
생체 내(In Vivo) (개별적으로 순서대로 용매를 제품에 첨가하십시오.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml은 약간 용해되거나 불용해됨을 의미합니다.
* Selleck은 모든 화합물의 용해도를 자체적으로 테스트하며, 실제 용해도는 게시된 값과 약간 다를 수 있습니다. 이는 정상적인 현상이며, 약간의 배치 간 변동으로 인해 발생합니다.
* 실온 배송 (안정성 테스트 결과 이 제품은 냉각 조치 없이 배송될 수 있음을 보여줍니다.)

원액 준비

생물학적 활성

설명 Zileuton은 경구 활성 5-Lipoxygenase 억제제로, 류코트리엔(LTB4, LTC4, LTD4 및 LTE4) 생성을 억제하여 천식 증상을 완화하는 데 사용됩니다. 이 화합물은 Apoptosis related 과정을 유도하는 동시에 Ferroptosis를 억제합니다.
표적
Ferroptosis 5-lipoxygenase
시험관 내(In vitro)

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

생체 내(In Vivo)

Zileuton significantly reduces macroscopic damage score after four weeks of treatment in rats. This compound administration significantly increases the intracolonic release of both thromboxane B2 at week 1 and prostaglandin E2 at weeks 2 and 4 in rats. It 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. This chemical significantly improves the recovery of limb function over 10 days in mice.

 

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

 

It 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 this compound- versus JNJ-26993135-treated mice.

프로토콜 (참조)

참조

  • https://pubmed.ncbi.nlm.nih.gov/20880396/
  • https://pubmed.ncbi.nlm.nih.gov/8984030/
  • https://pubmed.ncbi.nlm.nih.gov/18059327/
  • https://pubmed.ncbi.nlm.nih.gov/15266012/
  • https://pubmed.ncbi.nlm.nih.gov/17371808/
  • https://pubmed.ncbi.nlm.nih.gov/26235588/

고객 제품 검증

CD19+ B cells (A) or PBMCs (B) from a healthy donor were treated with zileuton (10 μM) prior to 17-HDHA or RvD1 treatment, followed by stimulation with the IgE-inducing cocktail. Cell culture supernatants were collected at day 7, and IgE levels were measured. The experiment was done in one representative donor (mean ± SEM). Data were analyzed by 1-way ANOVA with Tukey’s post test, **P ≤ 0.01, ***P ≤ 0.001. PBMC, peripheral blood mononuclear cell.

데이터 출처 [ , , JCI Insight, 2017, 2(3):e88588 ]

Selleck's Zileuton 인용됨 22 출판물

Synergistic Renoprotective Effect of Melatonin and Zileuton by Inhibition of Ferroptosis via the AKT/mTOR/NRF2 Signaling in Kidney Injury and Fibrosis [ Biomolecules & Therapeutics, May 15 2023, 599-610]
Identifying novel radioprotective drugs via salivary gland tissue chip screening [ bioRxiv, July 13 2023, nan] PubMed: 37503292
AGER-Mediated Lipid Peroxidation Drives Caspase-11 Inflammasome Activation in Sepsis [ Frontiers in Immunology, August 08 2019, 1904] PubMed: 31440260
Elucidating the role of S100A10 in CD8+ T cell exhaustion and HCC immune escape via the cPLA2 and 5-LOX axis [ Cell Death & Disease, August 01 2024, 558] PubMed: 39117605
Inhibiting Arachidonate-5-lipoxygenase expression ameliorates osteoarthritis progression by suppressing ferroptosis via the JAK2/STAT3 signaling pathway [ Free Radic Biol Med, 2026, 246:334-349] PubMed: 41581577
Inhibiting Arachidonate-5-lipoxygenase expression ameliorates osteoarthritis progression by suppressing ferroptosis via the JAK2/STAT3 signaling pathway [ Free Radical Biology and Medicine, 2026, 334-349] PubMed: 41581577
Elucidating the role of S100A10 in CD8+ T cell exhaustion and HCC immune escape via the cPLA2 and 5-LOX axis [ Cell Death & Disease, 2024 Aug 8, 573] PubMed: 39117605
Inhibition of neutrophil swarming by type I interferon promotes intracellular bacterial evasion [ Nat Commun, 2024, 15(1):8663] PubMed: 39375351
Cancer-educated neutrophils promote lung cancer progression via PARP-1-ALOX5-mediated MMP-9 expression [ Cancer Biology & Medicine, 2024, 175-192] PubMed: 38172525
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

반품 정책
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배송 및 보관
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