Diazoxide

製品コードS4630 バッチS463002

印刷

化学情報

Chemical Structure Synonyms Sch-6783, SRG-95213 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C8H7ClN2O2S
分子量 230.67 CAS No. 364-98-7
Solubility (25°C)* 体外 DMSO 46 mg/mL (199.41 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.

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生物活性

製品説明 Diazoxide is a well-known small molecule that activates KATP channels in the smooth muscle of blood vessels and pancreatic beta-cells by increasing membrane permeability to potassium ions.
in vitro Diazoxide inhibits microglial inflammatory activity. Diazoxide treatment partially inhibits the inflammatory pattern induced by LPS/IFN-γ in microglial cells, inducing a decrease in NO production that could be because of the decreased expression of iNOS detected. Diazoxide has no effect on microglial phagocytosis[1].
in vivo Diazoxide is beneficial on the improvement in cognitive tasks, reduction of anxiety, decrease in the accumulation of amyloid-beta oligomers and hyperphosphorylation of tau proteins. Diazoxide may also exerts neuroprotective effects independently of K+ channel activation by decreasing neuronal excitability and activation of N-methyl-D-aspartate (NMDA) receptors or by increasing currents trough α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptors. Diazoxide-treated animals show a decrease in disease severity a few days after the first clinical signs are observed, corresponding to the acute inflammatory phase of the disease. Daily oral administration of diazoxide in EAE mice during the effector phase of the disease reduces the severity of the clinical signs without any apparent adverse effect. Diazoxide decreases demyelination and axonal loss, reduces tissue damage, inhibits microglial/macrophage and astrocytic activation and preserves neuron integrity. No effects are observed on the number of B and T lymphocytes infiltrating the spinal cord[1].

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Mouse microglial cell line BV-2
濃度 100 μM
反応時間 30 min
実験の流れ The phagocytic ability of microglia is determined by the uptake of 2-μm red fluorescent microspheres by BV-2 cells. Cells are treated with diazoxide 100 μM and activated with LPS/IFN-γ and then incubated with microspheres at a concentration of 0.01% for 30 min in the dark at 37°C and 5% CO2. Cells are rinsed twice in PBS solution, pelleted at 1,000 g for 5 min and resuspended in 300 μL PBS. Cells are kept on ice and analyzed by flow cytometry.
動物実験 動物モデル Female C57BL/6J mice
投薬量 0.8 mg/kg
投与方法 oral administration

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：

Novel luciferase-based glucagon-like peptide 1 reporter assay reveals naturally occurring secretagogues [ Br J Pharmacol, 2022, 10.1111/bph.15896] PubMed: 35736785
Melatonin-mediated upregulation of Sirt3 attenuates sodium fluoride-induced hepatotoxicity by activating the MT1-PI3K/AKT-PGC-1α signaling pathway [Song C, et al. Free Radic Biol Med, 2017, 112:616-630] PubMed: 28912098

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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