Cat. No.: HY-B1140

Diazoxide

(Synonyms: Sch-6783; SRG-95213)

8 Cited Publications

Customer Review

Based on 8 publication(s) in Google Scholar

Diazoxide (Sch-6783) is an ATP-sensitive potassium channel activator, has the potential for hyperinsulinism treatment.

For research use only. We do not sell to patients.

Purity: 99.99%
CAS No.: 364-98-7
Formula: C₈H₇ClN₂O₂S
Molecular Weight:230.67

Storage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Diazoxide Chemical Structure

CAS No.: 364-98-7

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Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (8)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

Diazoxide (Sch-6783) is an ATP-sensitive potassium channel activator, has the potential for hyperinsulinism treatment.

Cellular Effect

Cell Line	Type	Value	Description	References
Beta-TC3	EC₅₀	13.7 μM Compound: 3, diazoxide	Repolarization of tolbutamide-depolarized beta-TC3 cells Repolarization of tolbutamide-depolarized beta-TC3 cells	[PMID: 17425298]
Beta-TC3	EC₅₀	13.7 μM Compound: diazoxide	Repolarization of beta-TC3 cells Repolarization of beta-TC3 cells	[PMID: 16821773]
Beta-TC3	IC₅₀	13.7 μM Compound: Diazoxide	Ability to repolarize beta-TC3 cell membrane potential Ability to repolarize beta-TC3 cell membrane potential	[PMID: 15163199]
Beta-TC6	EC₅₀	22.98 μM Compound: diazoxide	Inhibition of glucose-stimulated insulin release in betaTC6 cells Inhibition of glucose-stimulated insulin release in betaTC6 cells	[PMID: 16821773]
Beta-TC6	IC₅₀	22.4 μM Compound: Diazoxide	In vitro inhibition of insulin release from murine beta-TC6 cells In vitro inhibition of insulin release from murine beta-TC6 cells	[PMID: 11425552]
Beta-TC6	IC₅₀	22.4 μM Compound: diazoxide	Ability to inhibit the release of insulin from the mouse beta-TC6 cell line Ability to inhibit the release of insulin from the mouse beta-TC6 cell line	[PMID: 12213059]
Beta-TC6	IC₅₀	22.4 μM Compound: Diazoxide	In vitro ability to inhibit glucose stimulated insulin release in beta-TC6 cells from rat islets In vitro ability to inhibit glucose stimulated insulin release in beta-TC6 cells from rat islets	[PMID: 15163199]
Beta-TC6	IC₅₀	22.98 μM Compound: Diazoxide	Concentration required for inhibition of glucose stimulated insulin release from beta TC6 cells Concentration required for inhibition of glucose stimulated insulin release from beta TC6 cells	[PMID: 15501029]
HEK293	EC₅₀	23.5 μM Compound: 3	Activation of human recombinant SUR1/Kir6.2 channel expressed in HEK293 cells assessed as increase in ionic current by whole cell patch clamp assay Activation of human recombinant SUR1/Kir6.2 channel expressed in HEK293 cells assessed as increase in ionic current by whole cell patch clamp assay	[PMID: 19919106]
HEK293	EC₅₀	31 μM Compound: 3, diazoxide	Activity at Kir6.2/SUR1 KATP channels expressed in HEK293 cells assessed as activation of K+ currents Activity at Kir6.2/SUR1 KATP channels expressed in HEK293 cells assessed as activation of K+ currents	[PMID: 17425298]
HEK293	EC₅₀	33 μM Compound: 3, diazoxide	Activity at Kir6.2/SUR1 KATP channels expressed in HEK293 cells assessed as repolarization of tolbutamide-induced membrane depolarization Activity at Kir6.2/SUR1 KATP channels expressed in HEK293 cells assessed as repolarization of tolbutamide-induced membrane depolarization	[PMID: 17425298]
HEK293	EC₅₀	33 μM Compound: diazoxide	Repolarization of HEK293 cells expressing Kir6.2/SUR1 KATP channels Repolarization of HEK293 cells expressing Kir6.2/SUR1 KATP channels	[PMID: 16821773]
HEK293	IC₅₀	194 μM Compound: diazoxide	Displacement of [3H]glibenclamide from human Kir6.2/SUR1 expressed in HEK293 cells in presence of 2 mM ATP Displacement of [3H]glibenclamide from human Kir6.2/SUR1 expressed in HEK293 cells in presence of 2 mM ATP	[PMID: 16821773]
HEK293	IC₅₀	198 μM Compound: diazoxide	Inhibition of [3H]glibenclamide binding to HEK293 cells co-expressing human Sulfonylurea receptor SUR1 and Inward rectifier K+ channel Kir6.2 at low affinity state with 2 mM MgATP Inhibition of [3H]glibenclamide binding to HEK293 cells co-expressing human Sulfonylurea receptor SUR1 and Inward rectifier K+ channel Kir6.2 at low affinity state with 2 mM MgATP	[PMID: 12213059]
HEK293	IC₅₀	33 μM Compound: Diazoxide	Potency by glucose stimulated insulin release from HEK 293 cells Potency by glucose stimulated insulin release from HEK 293 cells	[PMID: 15501029]
HEK293	IC₅₀	740 μM Compound: diazoxide	Displacement of [3H]glibenclamide from human Kir6.2/SUR1 expressed in HEK293 cells Displacement of [3H]glibenclamide from human Kir6.2/SUR1 expressed in HEK293 cells	[PMID: 16821773]
HEK293	IC₅₀	750 μM Compound: diazoxide	Inhibition of [3H]glibenclamide binding to HEK293 cells co-expressing human Sulfonylurea receptor SUR1 and Inward rectifier K+ channel Kir6.2 without ATP Inhibition of [3H]glibenclamide binding to HEK293 cells co-expressing human Sulfonylurea receptor SUR1 and Inward rectifier K+ channel Kir6.2 without ATP	[PMID: 12213059]
INS-1E	EC₅₀	20.28 μM Compound: 3, diazoxide	Inhibition of insulin release from rat INS-1E cells Inhibition of insulin release from rat INS-1E cells	[PMID: 17425298]
Murine cell line	EC₅₀	77.4 μM Compound: diazoxide	Changes in potassium fluxes assessed in the glucose responsive insulin-producing murine cell line beta-TC3 Changes in potassium fluxes assessed in the glucose responsive insulin-producing murine cell line beta-TC3	[PMID: 12213059]
Oocyte	EC₅₀	8.8 μM Compound: Diazoxide	Maximum activation of human KATP (SUR1/Kir6.2) channel expressed in Xenopus oocytes Maximum activation of human KATP (SUR1/Kir6.2) channel expressed in Xenopus oocytes	[PMID: 14741296]
VSMC	EC₅₀	22.4 μM Compound: 3	Myorelaxant effect in KCl-induced precontracted rat aorta ring VSMC Myorelaxant effect in KCl-induced precontracted rat aorta ring VSMC	[PMID: 21428460]

In Vitro

Diazoxide (Sch-6783) has a number of physiological effects, including lowering the blood pressure and rectifying hypoglycemia. Diazoxide has powerful protective properties against cardiac ischemia^[1].
? Diazoxide (Sch-6783) could protect NSC-34 neurons against the main sources of neurodegenerative damage. Diazoxide increases Nrf2 nuclear translocation in NSC-34 motoneurons and prevents endogenous oxidative damage^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Diazoxide (Sch-6783) attenuates postresuscitation brain injury, protects mitochondrial function, inhibits brain cell apoptosis, and activates the PKC pathway by opening mitoKATP channels^[3].
Treatment with Diazoxide (Sch-6783) in wild-type mice decreases intraocular pressure (IOP) by 21.5±3.2% with an absolute IOP reduction of 3.9 ± 0.6 mm Hg^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 364-98-7
Appearance Solid
Molecular Weight 230.67
Formula C₈H₇ClN₂O₂S
Color Off-white to gray
SMILES

CC(NC1=CC=C(Cl)C=C12)=NS2(=O)=O
Synonyms

Sch-6783; SRG-95213
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (8)

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Cell Stem Cell

Enhanced viability and functional maturity of iPSC-derived islet organoids by collagen-VI-enriched ECM scaffolds. [Abstract]

2025 Apr 3;32(4):547-563.e7. PMID: 39999846
Redox Biol

Kir6.2 is essential to maintain neurite features by modulating PM20D1-reduced mitochondrial ATP generation. [Abstract]

2021 Nov:47:102168. PMID: 34673451

Diazoxide purchased from MedChemExpress. Usage Cited in: Redox Biol. 2021 Nov:47:102168. [Abstract]

Diazoxide (oral administration, 10 mg/kg bodyweight, every day for two weeks). Immunoblotting analysis of neurite related markers including PSD95, SYP, MAP2, and Tau were detected in midbrain samples from diazoxide-treated and untreated mice.

Diazoxide purchased from MedChemExpress. Usage Cited in: Redox Biol. 2021 Nov:47:102168. [Abstract]

Diazoxide (oral administration, 10 mg/kg bodyweight, every day for two weeks). Neuronal morphology in Golgi staining was reflected in a two-dimensional map generated by the Image J software (up). Scale bar is 200 μm. Dendritic spines photographed by oil microscope under 100x magnification (down).

Diazoxide purchased from MedChemExpress. Usage Cited in: Redox Biol. 2021 Nov:47:102168. [Abstract]

Diazoxide (oral administration, 10 mg/kg bodyweight, every day for two weeks). Movement trace diagrams (red curve) of untreated and diazoxide-treated mice in the OFT. Statistical charts of movement distance and moved speed in the OFT.

Diazoxide purchased from MedChemExpress. Usage Cited in: Redox Biol. 2021 Nov:47:102168. [Abstract]

Diazoxide (oral administration, 10 mg/kg bodyweight, every day for two weeks). Analysis of the time consumed in pole test and the latency time in the rotarod test.

Diazoxide purchased from MedChemExpress. Usage Cited in: Redox Biol. 2021 Nov:47:102168. [Abstract]

Diazoxide (oral administration, 10 mg/kg bodyweight, every day for two weeks). Pm20d1 mRNA in the midbrain of untreated and diazoxide-treated mice detected by RT-PCR.

Diazoxide purchased from MedChemExpress. Usage Cited in: Redox Biol. 2021 Nov:47:102168. [Abstract]

Diazoxide (oral administration, 10 mg/kg bodyweight, every day for two weeks). Levels of PM20D1 in the midbrain of untreated and diazoxide-treated mice were determined by ELISA kit.

Diazoxide purchased from MedChemExpress. Usage Cited in: Redox Biol. 2021 Nov:47:102168. [Abstract]

Diazoxide (oral administration, 10 mg/kg bodyweight, every day for two weeks). Immunoblotting analysis of PM20D1 in midbrain samples from diazoxide-treated and untreated mice.

Diazoxide purchased from MedChemExpress. Usage Cited in: Redox Biol. 2021 Nov:47:102168. [Abstract]

Diazoxide (oral administration, 10 mg/kg bodyweight, every day for two weeks). ATP contents in the midbrain of untreated and diazoxide-treated mice.
Sci China Life Sci

Osmosensor TMEM63B facilitates insulin secretion in pancreatic β-cells. [Abstract]

2025 Feb 20. PMID: 39985646
ACS Environ Au

Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]

2025 Aug 5;5(6):573-582. PMID: 41277996
Pharmaceuticals (Basel)

An Alternative Mechanism of Glutamate Dehydrogenase Inhibition by EGCG: Promotion of Protein Degradation. [Abstract]

2025 Jun 12;18(6):877. PMID: 40573270
Cell Biol Int

Penehyclidine hydrochloride protects against anoxia/reoxygenation injury in cardiomyocytes through ATP-sensitive potassium channels, and the Akt/GSK-3β and Akt/mTOR signaling pathways. [Abstract]

2020 Jun;44(6):1353-1362. PMID: 32125033
Patent

US20240299405A1.
Biological Sciences

2020 Sep.

Solvent & Solubility

In Vitro:

DMSO : ≥ 35 mg/mL (151.73 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

4.3352 mL

21.6760 mL

43.3520 mL

5 mM

0.8670 mL

4.3352 mL

8.6704 mL

10 mM

0.4335 mL

2.1676 mL

4.3352 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (9.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (9.02 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocol

Cell Assay^[2]

Diazoxide is dissolved in DMSO to prepare 50 mM stock solution. NSC-34 cells are allowed to differentiate for 8 weeks under reduced serum conditions and then seeded in 24-well plates. Glutamate is dissolved in culture medium and added to cultures at concentration of 10 μM for 24 h. Cell treatment with 100 µM diazoxide starts 2 h before glutamate exposure. Cell viability is measured by the MTT assay^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[3]^[4]

Rats: Adult male Sprague-Dawley rats with induced cerebral ischemia (n=10 per group) receive an intraperitoneal injection of 0.1% DMSO (1 mL; vehicle group), diazoxide (10 mg/kg; DZ group), or diazoxide (10 mg/kg) plus 5-hydroxydecanoate (5 mg/kg; DZ + 5-HD group) 30 min after CPR. The control group (sham group, n=5) undergoes sham operation, without cardiac arrest. Mitochondrial respiratory control rate (RCR) is determined. Brain cell apoptosis is assessed using TUNEL staining. Expression of Bcl-2, Bax, and protein kinase C epsilon (PKCε) in the cerebral cortex is determined by Western blotting and immunohistochemistry^[3].

Mouse: Diazoxide is prepared by diluting a 100 mM stock solution in 10% polyethoxylated castor oil in PBS. In C57BL/6 wild-type and Kir6.2^(−/−) mice, a 5 μL drop of 5 mM diazoxide is topically administered to one eye of each mouse while the fellow control eye received vehicle (DMSO and 10% polyethoxylated castor oil in the same proportion as the treated eye). IOP is measured daily at 1 hour, 4 hours, and 23 hours following treatment. Treatment with diazoxide and vehicle is continued daily for 14 consecutive days^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Portuguese - PT (419 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Coetzee WA, et al. Multiplicity of effectors of the cardioprotective agent, diazoxide. Pharmacol Ther. 2013 Nov;140(2):167-75. [Content Brief]

[2]. Virgili N, et al. K(ATP) channel opener diazoxide prevents neurodegeneration: a new mechanism of action viaantioxidative pathway activation. PLoS One. 2013 Sep 11;8(9):e75189. [Content Brief]

[3]. Wu H, et al. Diazoxide Attenuates Postresuscitation Brain Injury in a Rat Model of Asphyxial Cardiac Arrest by Opening Mitochondrial ATP-Sensitive Potassium Channels. Biomed Res Int. 2016;2016:1253842. [Content Brief]

[4]. Chowdhury UR, et al. ATP-sensitive potassium (K(ATP)) channel openers diazoxide and nicorandil lower intraocular pressure in vivo. Invest Ophthalmol Vis Sci. 2013 Jul 22;54(7):4892-9. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	4.3352 mL	21.6760 mL	43.3520 mL	108.3799 mL
	5 mM	0.8670 mL	4.3352 mL	8.6704 mL	21.6760 mL
	10 mM	0.4335 mL	2.1676 mL	4.3352 mL	10.8380 mL
	15 mM	0.2890 mL	1.4451 mL	2.8901 mL	7.2253 mL
	20 mM	0.2168 mL	1.0838 mL	2.1676 mL	5.4190 mL
	25 mM	0.1734 mL	0.8670 mL	1.7341 mL	4.3352 mL
	30 mM	0.1445 mL	0.7225 mL	1.4451 mL	3.6127 mL
	40 mM	0.1084 mL	0.5419 mL	1.0838 mL	2.7095 mL
	50 mM	0.0867 mL	0.4335 mL	0.8670 mL	2.1676 mL
	60 mM	0.0723 mL	0.3613 mL	0.7225 mL	1.8063 mL
	80 mM	0.0542 mL	0.2709 mL	0.5419 mL	1.3547 mL
	100 mM	0.0434 mL	0.2168 mL	0.4335 mL	1.0838 mL

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Publications Citing Use of MedChemExpress (MCE) Diazoxide

Biological Activity

Chemical Information

Publications (8)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Diazoxide Related Classifications

Cat. No.: HY-B1140