Setanaxib (GKT137831)

製品コードS7171 バッチS717106

印刷

化学情報

Chemical Structure Synonyms GKT831 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21H19ClN4O2
分子量 394.85 CAS No. 1218942-37-0
Solubility (25°C)* 体外 DMSO 78 mg/mL warmed with 50ºC water bath (197.54 mM)
Water Insoluble
Ethanol Insoluble
* <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 Setanaxib (GKT137831, GKT831) is a potent, dual NADPH oxidase NOX1/NOX4 inhibitor with Ki of 110 nM and 140 nM, respectively. Treatment with GKT137831 suppresses reactive oxygen species (ROS) production. GKT137831 partly inhibits ferroptosis.
in vitro

GKT137831 attenuates hypoxia-induced H(2)O(2) release, cell proliferation, and TGF-β1 expression and blunted reductions in PPARγ in HPAECs and HPASMCs. [2] GKT137831 also prevents oxidative stress in response to hyperglycemia in human aortic endothelial cells. [3]
in vivo

In WT and SOD1mut mice, GKT137831 (60 mg/kg i.g.) blocks liver fibrosis and downregulates markers of oxidative stress, inflammation, and fibrosis. [1] GKT137831 (60 mg/kg/d p.o.) also attenuates chronic hypoxia–induced right ventricular hypertrophy, vascular remodeling, lung cell proliferation, and hypoxic alterations in lung PPARγ and TGF-β1 expression in mouse model of chronic hypoxia exposure. [2] In diabetic apolipoprotein E-deficient mice, GKT137831 (60 mg/kg/d p.o.) attenuates diabetes mellitus-accelerated atherosclerosis. [3] Moreover, in angII-infused c-hNox4Tg mice, GKT137831 abolishes the increase in oxidative stress, suppresses Akt-mTOR and NF-κB signaling pathway and attenuates cardiac remodeling. [4]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Hypoxic HPASMC and HPAECs
濃度 20 μM
反応時間 72 hours
実験の流れ

Hypoxic HPASMC and HPAEC proliferation is determined using MTT assay, by Western blotting to detect proliferating cell nuclear antigen (PCNA) expression, or by manual cell counting after Trypan blue staining. Amplex Red Hydrogen Peroxide/Peroxidase Assay Kit is used to measure H2O2 released into the culture media from HPAECs or HPASMCs. After exposure to control or hypoxic environments for 72 hours, Amplex Red reagent is added, and the cells are returned to control or hypoxic environments for an additional hour before fluorescence measurements.
動物実験 動物モデル Mouse models of liver fibrosis
投薬量 60 mg/kg daily
投与方法 i.g.

カスタマーフィードバック

, , Mol Med, 2016, doi: 10.2119/molmed.2015.00250

Data from [Data independently produced by , , Biochim Biophys Acta, 2016, 1861(1 Pt A):2912-2921. ]

Data from [Data independently produced by , , Exp Cell Res, 2017, 352(2):245-254]

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：

trans-Endothelial neutrophil migration activates bactericidal function via Piezo1 mechanosensing [ Immunity, 2024, 57(1):52-67.e10] PubMed: 38091995
Setanaxib mitigates oxidative damage following retinal ischemia-reperfusion via NOX1 and NOX4 inhibition in retinal ganglion cells [ Biomed Pharmacother, 2024, 170:116042] PubMed: 38118351
Fibroblast growth factor 18 alleviates stress-induced pathological cardiac hypertrophy in male mice [ Nat Commun, 2023, 14(1):1235] PubMed: 36871047
NOX4 is a potential therapeutic target in septic acute kidney injury by inhibiting mitochondrial dysfunction and inflammation [ Theranostics, 2023, 13(9):2863-2878] PubMed: 37284448
The TRIM21-FOXD1-BCL-2 axis underlies hyperglycaemic cell death and diabetic tissue damage [ Cell Death Dis, 2023, 14(12):825] PubMed: 38092733
Adipocyte-Derived Exosomal NOX4-Mediated Oxidative Damage Induces Premature Placental Senescence in Obese Pregnancy [ Int J Nanomedicine, 2023, 18:4705-4726] PubMed: 37608820
Adipocyte-Derived Exosomal NOX4-Mediated Oxidative Damage Induces Premature Placental Senescence in Obese Pregnancy [ Int J Nanomedicine, 2023, 18:4705-4726] PubMed: 37608820
COL4A3 Mutation Induced Podocyte Apoptosis by Dysregulation of NADPH Oxidase 4 and MMP-2 [ Kidney Int Rep, 2023, 8(9):1864-1874] PubMed: 37705901
Reduction of NADPH oxidase 4 in adipocytes contributes to the anti-obesity effect of dihydroartemisinin [ Heliyon, 2023, 9(3):e14028] PubMed: 36915539
NOX4-derived ROS Regulates Aerobic Glycolysis of Breast Cancer through YAP Pathway [ J Cancer, 2023, 14(13):2562-2573] PubMed: 37670970

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。