Diazoxide

For research use only.

Catalog No.S4630 Synonyms: Sch-6783, SRG-95213, Proglycem

1 publication

Diazoxide Chemical Structure

CAS No. 364-98-7

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.

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Selleck's Diazoxide has been cited by 1 publication

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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

Cell Research:[1]
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  • 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.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: Female C57BL/6J mice
  • Dosages: 0.8 mg/kg
  • Administration: oral administration
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 46 mg/mL (199.41 mM)
Water Insoluble
Ethanol 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.

Chemical Information

Molecular Weight 230.67
Formula

C8H7ClN2O2S

CAS No. 364-98-7
Storage powder
in solvent
Synonyms Sch-6783, SRG-95213, Proglycem
Smiles CC1=NS(=O)(=O)C2=C(N1)C=CC(=C2)Cl

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03941236 Enrolling by invitation Drug: dasiglucagon Congenital Hyperinsulinism Zealand Pharma May 1 2019 Phase 3
NCT00901823 Withdrawn Drug: Diazoxide choline|Drug: Diazoxide choline high dose Hypertriglyceridemia Essentialis Inc. March 2011 Phase 1
NCT00696475 Completed Drug: Diazoxide choline|Drug: Placebo Hypertriglyceridemia Essentialis Inc.|Medpace Inc. June 2008 Phase 2
NCT00688857 Completed Drug: Diazoxide choline Hypertriglyceridemia Essentialis Inc.|Cetero Research San Antonio May 2008 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID