Setanaxib (GKT137831)

製品コードS7171 バッチS717102

化学情報

	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.

参考

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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
Inhibition of neutrophil swarming by type I interferon promotes intracellular bacterial evasion [ Nat Commun, 2024, 15(1):8663]	PubMed: 39375351
Autophagy-mediated activation of the AIM2 inflammasome enhances M1 polarization of microglia and exacerbates retinal neovascularization [ MedComm (2020), 2024, 5(8):e668]	PubMed: 39081514
Setanaxib mitigates oxidative damage following retinal ischemia-reperfusion via NOX1 and NOX4 inhibition in retinal ganglion cells [ Biomed Pharmacother, 2024, 170:116042]	PubMed: 38118351
Sevoflurane Exposure Induces Neuronal Cell Ferroptosis Initiated by Increase of Intracellular Hydrogen Peroxide in the Developing Brain via ER Stress ATF3 Activation [ Mol Neurobiol, 2024, 61(4):2313-2335]	PubMed: 37874483
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
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

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。

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