Diazoxide

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

For research use only.

Diazoxide (Sch-6783, SRG-95213, Proglycem) 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.

Diazoxide Chemical Structure

CAS No. 364-98-7

Selleck's Diazoxide has been cited by 1 Publication

Purity & Quality Control

Choose Selective ADC Cytotoxin Inhibitors

Biological Activity

Description Diazoxide (Sch-6783, SRG-95213, Proglycem) 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 Research:[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.
  • (Only for Reference)
Animal Research:[1]
  • 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 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=NS(=O)(=O)C2=C(N1)C=CC(=C2)Cl

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

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

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3
If you have any other enquiries, please leave a message.

* Indicates a Required Field

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.
Tags: buy Diazoxide | Diazoxide ic50 | Diazoxide price | Diazoxide cost | Diazoxide solubility dmso | Diazoxide purchase | Diazoxide manufacturer | Diazoxide research buy | Diazoxide order | Diazoxide mouse | Diazoxide chemical structure | Diazoxide mw | Diazoxide molecular weight | Diazoxide datasheet | Diazoxide supplier | Diazoxide in vitro | Diazoxide cell line | Diazoxide concentration | Diazoxide nmr