Diphenyleneiodonium chloride [4673-26-1]

Référence HY-100965-50mg

Conditionnement : 50mg

Marque : MedChemExpress


Description

Diphenyleneiodonium chloride is a NADPH oxidase (NOX) inhibitor and also functions as a TRPA1 activator with an EC50 of 1 to 3 μM. Diphenyleneiodonium chloride selectively inhibits intracellular reactive oxygen species.

IC50 & Target

NOX[1]
EC50: 1 to 3 μM (TRPA1)[1]

Cellular Effect
Cell Line Type Value Description References
Neutrophil IC50
1.8 μM
Compound: DPI
Inhibition of PMA-stimulated super oxide anion generation in Sprague-Dawley rat neutrophils
Inhibition of PMA-stimulated super oxide anion generation in Sprague-Dawley rat neutrophils
[PMID: 19278854]
Neutrophil IC50
2.7 μM
Compound: DPI
Inhibition of fMLP/cytochalasin B-stimulated super oxide anion generation in Sprague-Dawley rat neutrophils
Inhibition of fMLP/cytochalasin B-stimulated super oxide anion generation in Sprague-Dawley rat neutrophils
[PMID: 19278854]
Neutrophil IC50
3.3 μM
Compound: DPI
Inhibition of 3 nM PMA-stimulated superoxide anion generation in rat neutrophils
Inhibition of 3 nM PMA-stimulated superoxide anion generation in rat neutrophils
[PMID: 17320246]
Neutrophil IC50
4.3 μM
Compound: DPI
Inhibition of PMA-induced superoxide generation in Sprague-Dawley rat neutrophils
Inhibition of PMA-induced superoxide generation in Sprague-Dawley rat neutrophils
[PMID: 19699097]
Neutrophil IC50
5.2 μM
Compound: DPI
Inhibition of fMLP-induced superoxide generation in Sprague-Dawley rat neutrophils
Inhibition of fMLP-induced superoxide generation in Sprague-Dawley rat neutrophils
[PMID: 19699097]
Neutrophil IC50
5.8 μM
Compound: DPI
Inhibition of 0.3 uM fMLP-stimulated superoxide anion generation in rat neutrophils
Inhibition of 0.3 uM fMLP-stimulated superoxide anion generation in rat neutrophils
[PMID: 17320246]
In Vitro

Diphenyleneiodonium chloride is a NADPH oxidase (NOX) inhibitor and also functions as a TRPA1 activator with an EC50 of 1 to 3 μM. Application of Diphenyleneiodonium chloride to HEK-TRPA1 cells at a concentration ranges of 0.03 to 10 μM effectively induces a Ca2+ response. However, Diphenyleneiodonium chloride fails to evoke a Ca2+ response in control HEK cells, even at a relatively high dose of 10 μM[1]. When Diphenyleneiodonium chloride is included in the co-cultures, lipopolysaccharide (LPS)-induced preOL apoptosis is significantly inhibited. Treatment with Diphenyleneiodonium chloride is found to significantly attenuate the LPS-induced O2- production by 2.0-fold, reducing it to within 27% of the controls[2].

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

In Vivo

Intraplantar injection of 2 mM Diphenyleneiodonium chloride to the hindpaw causes licking or biting behavior[1]. Diphenyleneiodonium chloride treatment immediately or 24 h after lipopolysaccharide (LPS) injection significantly attenuates the LPS-induced loss of O4 positive cells. Treatment with Diphenyleneiodonium chloride either immediately or 24 h after LPS injection significantly ameliorates the LPS-induced disorganization of the white matter nerve fibers. However, treatment with DPI 48 h after LPS injection does not appear to correct the LPS-induced white matter damage. DPI treatment either immediately or 24 h after LPS injection significantly reduces the accumulation of both gp91phox and p67phox in the membrane fraction[2].

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

Masse moléculaire

314.55

Formule

C12H8ClI

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

C12=CC=CC=C1C3=CC=CC=C3[I+]2.[Cl-]

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

Solvant et solubilité
In Vitro: 

DMSO : 3.33 mg/mL (10.59 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : < 0.1 mg/mL (insoluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1791 mL 15.8957 mL 31.7915 mL
5 mM 0.6358 mL 3.1791 mL 6.3583 mL
View the Complete Stock Solution Preparation Table

* 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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

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

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: ≥ 0.33 mg/mL (1.05 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.33 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (3.3 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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 0.33 mg/mL (1.05 mM); Clear solution

    This protocol yields a clear solution of ≥ 0.33 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 (3.3 mg/mL) to 900 μL Corn oil, and mix evenly.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  50% PEG300    50% Saline

    Solubility: 10 mg/mL (31.79 mM); Suspended solution; Need ultrasonic

Pureté et documentation
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