Diazoxide

Catalog No.S4630 Batch:S463001

Technical Data

Formula	C₈H₇ClN₂O₂S
Molecular Weight	230.67	CAS No.	364-98-7
Solubility (25°C)*	In vitro	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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description

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.

Targets

KATP channels ^[2]

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].

Protocol (from reference)

Cell Assay:^{^[1]}	Cell lines Mouse microglial cell line BV-2 Concentrations 100 μM Incubation Time 30 min Method 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.
Animal Study:^{^[1]}	Animal Models Female C57BL/6J mice Dosages 0.8 mg/kg Administration oral administration

Cell Assay:^{^[1]}

Cell lines
Mouse microglial cell line BV-2
Concentrations
100 μM
Incubation Time
30 min
Method
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.

Animal Study:^{^[1]}

Animal Models
Female C57BL/6J mice
Dosages
0.8 mg/kg
Administration
oral administration

References

Selleck's Diazoxide has been cited by 3 publications

Propafenone facilitates mitochondrial-associated ferroptosis and synergizes with immunotherapy in melanoma [ J Immunother Cancer, 2024, 12(11)e009805]	PubMed: 39581704
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

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SHIPPING AND STORAGE
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