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Chemical Structure| 364-98-7 Chemical Structure| 364-98-7

Structure of Diazoxide
CAS No.: 364-98-7

Chemical Structure| 364-98-7

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Diazoxide is an ATP-sensitive potassium channel activator which causes local relaxation in smooth muscle by increasing membrane permeability to potassium ions. and can be used to treat hyperinsulinism.

Synonyms: Sch-6783; SRG-95213; NSC 76130

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Product Citations

Product Citations

Fofie, Christian Kuete ; Granja-Vazquez, Rafael ; Truong, Vincent ; Walsh, Patrick ; Price, Theodore ; Biswas, Swati , et al.

Abstract: Chronic pain is a global health issue, yet effective treatments remain limited due to poor preclinical-to-human translation. To address this, we developed a high-content screening (HCS) platform using hiPSC-derived nociceptors to identify analgesics targeting the peripheral nervous system. These cells, cultured on multi-well microelectrode arrays, achieved nearly 100% active electrodes by week 2, maintaining stable activity for at least 2 weeks. After 28 days, we assessed drug effects on neuronal activity, achieving strong assay performance (robust Z′ > 0.5). Pharmacological tests confirmed responses to key analgesic targets, including ion channels (Nav, Cav, Kv, and TRPV1), neurotransmitter receptors (AMPAR and GABA-R), and kinase inhibitors (tyrosine and JAK1/2). Transcriptomic analysis validated target expression, though levels differed from primary human DRG cells. The platform was used to screen over 700 natural compounds, demonstrating its potential for analgesic discovery. This HCS platform facilitates the rapid discovery of uncharacterized analgesics, reducing preclinical-to-human translation failure.

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Product Details of Diazoxide

CAS No. :364-98-7
Formula : C8H7ClN2O2S
M.W : 230.67
SMILES Code : CC(NC1=CC=C(Cl)C=C12)=NS2(=O)=O
Synonyms :
Sch-6783; SRG-95213; NSC 76130
MDL No. :MFCD00078578
InChI Key :GDLBFKVLRPITMI-UHFFFAOYSA-N
Pubchem ID :3019

Safety of Diazoxide

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335-H351-H361
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
CD34+ cells 10 μM Diazoxide induced NO generation, which was blocked by L-NAME. PMC6887676
CD34+ cells 10 μM 10 min Diazoxide increased mitochondrial ROS generation, which was reversed by mitoTEMPO. PMC6887676
CD34+ cells 10 μM 30 min Diazoxide induced mitochondrial depolarization, which was blocked by 5-HD. PMC6887676
CD34+ cells 10 μM 48 h Diazoxide enhanced proliferation in CD34+ cells, comparable to SDF or VEGF. This effect was blocked by L-NAME or 5-HD. PMC6887676
CD34+ cells 10 μM 5 h Diazoxide stimulated migration in CD34+ cells, comparable to SDF or VEGF. This effect was blocked by L-NAME or 5-HD. PMC6887676
CRI-G1 insulin-secreting cell line 200 μM To investigate the effects of diazoxide on membrane potential and KATP channel currents in CRI-G1 cells. Results showed that diazoxide hyperpolarized the cells by activating KATP channels, with membrane potential decreasing from -38 mV to -76 mV and slope conductance increasing from 0.58 nS to 10.5 nS. PMC1565548
Mouse dorsal root ganglion (DRG) neurons 100 μM 24 h To evaluate the effect of Diazoxide on neurite outgrowth of DRG neurons, results showed that Diazoxide significantly elongated neurite lengths. PMC8719014
HK-2 cells 100uM 24 h To evaluate the effect of Diazoxide on sulfonylurea-induced apoptosis of PTECs, results showed that Diazoxide significantly alleviated glibenclamide-induced apoptosis and attenuated the protective effect of gliclazide PMC6122448
T1R3-GFP taste cells 40 μM Diazoxide mimicked the sweet-suppressing effect of leptin by activating KATP channels PMC4876703
GLUTag cells 100 µM 15 min To investigate the effect of Diazoxide on L-valine-induced intracellular calcium mobilization. Results showed that preincubation with diazoxide reduced the effect of 10 mM L-valine on intracellular calcium, making it no longer statistically significant. PMC11166632

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Wistar rats Obesity model Intraperitoneal injection 35 mg/kg 14 days Diazoxide and exercise improve muscle contraction during obesity by decreasing ROS levels and lipid peroxidation, and improving glutathione redox status. PMC7762033
Sprague-Dawley rats Normal Sprague-Dawley rats Intracerebroventricular (ICV) administration 9.69 mg/mL 0.006 mL/min for 240 minutes To investigate the contribution of central KATP channels to glucose effectiveness. Results showed that ICV administration of diazoxide restored glucose effectiveness, confirming that it is, at least in part, centrally mediated. PMC7243288
Wistar rats Isolated perfused rat small intestine model Intra-vascular perfusion 250 µM Continuous perfusion from minute 36 to 60 To investigate the effect of Diazoxide on L-valine-induced GLP-1 secretion. Results showed that diazoxide significantly inhibited the L-valine-induced GLP-1 response (P < 0.01), suggesting that L-valine-induced depolarization arises from intracellular metabolism and closure of KATP channels. PMC11166632

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00151684 Obesity|Hyperinsulinism PHASE2 COMPLETED - Rijnstate Hospital, Arnhem, Ne... More >>therlands Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

4.34mL

0.87mL

0.43mL

21.68mL

4.34mL

2.17mL

43.35mL

8.67mL

4.34mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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