Dequalinium (Chloride) [522-51-0]

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Référence HY-B0567-10mg

Conditionnement : 10mg

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Description

Dequalinium chloride is an Apamin (HY-P0256)-sensitive potassium channel selective blocker. Dequalinium chloride is a cationic, lipophilic mitochondrial poison. Dequalinium chloride is also an antagonist pf α7 nAChR, and an anti-microbial antiseptic agent with a broad bactericidal and fungicidal activity[1][2][3][4].

Cellular Effect
Cell Line Type Value Description References
Astrocyte EC50
1.418 μM
Compound: 29
Antiproliferative activity against mouse astrocyte cells by MTT assay
Antiproliferative activity against mouse astrocyte cells by MTT assay
[PMID: 17417631]
HEK293 IC50
1.3 μM
Compound: 15
Inhibition of Kca2.3 channel expressed in HEK293 cells by thallium flux assay
Inhibition of Kca2.3 channel expressed in HEK293 cells by thallium flux assay
[PMID: 18774291]
HEK293 IC50
2 μM
Compound: 15
Inhibition of Kca2.3 channel expressed in HEK293 cells by electrophysiology assay
Inhibition of Kca2.3 channel expressed in HEK293 cells by electrophysiology assay
[PMID: 18774291]
Hepatocyte IC50
1.7 μM
Compound: 2
Inhibition of apamin-sensitive SKCa channel of guinea-pig hepatocytes
Inhibition of apamin-sensitive SKCa channel of guinea-pig hepatocytes
[PMID: 15225721]
HepG2 IC50
>100 μM
Compound: 92125541
HARVARD: Cytotoxicity in HepG2 cell line
HARVARD: Cytotoxicity in HepG2 cell line
[PMID: 22586124]
HepG2 IC50
1.71 μM
Compound: 92125541
HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells
HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells
[PMID: 22586124]
Huh-7 CC50
30.99 μM
Compound: GNF-Pf-5483
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
[PMID: 18579783]
Sympathetic neuron IC50
0.65 μM
Compound: Dequalinium
Inhibition of after-hyperpolarization (AHP) in cultured rat sympathetic neurons
Inhibition of after-hyperpolarization (AHP) in cultured rat sympathetic neurons
[PMID: 8863802]
Sympathetic neuron IC50
0.74 μM
Compound: dequalinium (4)
The SKCa-blocking action was assessed by its ability to inhibit the after hyperpolarization (AHP) in cultured rat sympathetic neurones
The SKCa-blocking action was assessed by its ability to inhibit the after hyperpolarization (AHP) in cultured rat sympathetic neurones
[PMID: 7658440]
Sympathetic neuron IC50
0.74 μM
Compound: 1
Ability to inhibit the hyperpolarization (AHP) in cultured rat sympathetic neurons
Ability to inhibit the hyperpolarization (AHP) in cultured rat sympathetic neurons
10.1016/0960-894X(95)00073-3
Sympathetic neuron IC50
0.74 μM
Compound: Dequalinium
Ability to inhibit after-hyperpolarization (AHP) in cultured rat sympathetic neurons. (number of neurons tested, n=18).
Ability to inhibit after-hyperpolarization (AHP) in cultured rat sympathetic neurons. (number of neurons tested, n=18).
[PMID: 7861407]
Sympathetic neuron IC50
0.9 μM
Compound: Dequalinium
Compound was tested for its ability to inhibit the after hyperpolarization which follows the action potential in rat sympathetic neurons.
Compound was tested for its ability to inhibit the after hyperpolarization which follows the action potential in rat sympathetic neurons.
[PMID: 8784458]
Sympathetic neuron IC50
1 μM
Compound: 22(dequalinium)
SKCa-blocking activity by its ability to inhibit after hyperpolarization (AHP) in cultured rat sympathetic neurons
SKCa-blocking activity by its ability to inhibit after hyperpolarization (AHP) in cultured rat sympathetic neurons
[PMID: 8558503]
Sympathetic neuron IC50
490 nM
Compound: dequalinium
tested for their ability to inhibit the after- hyperpolarization (AHP) in cultured rat sympathetic neurons
tested for their ability to inhibit the after- hyperpolarization (AHP) in cultured rat sympathetic neurons
[PMID: 11000001]
Sympathetic neuron IC50
570 nM
Compound: Deq
Compound was tested for SKCa blocking action by measuring its ability to inhibit after hyperpolarization (AHP) in cultured rat sympathetic neurones
Compound was tested for SKCa blocking action by measuring its ability to inhibit after hyperpolarization (AHP) in cultured rat sympathetic neurones
[PMID: 9438015]
Sympathetic neuron IC50
900 nM
Compound: Dequalinium
Inhibition of after hyperpolarization (AHP) of cultured rat sympathetic neurons as SKCa channel blocking activity
Inhibition of after hyperpolarization (AHP) of cultured rat sympathetic neurons as SKCa channel blocking activity
[PMID: 15261276]
In Vitro

Dequalinium chloride blocks angiotensin II (100 nM)-evoked K+ loss in guinea-pig hepatocytes, with an IC50 of 1.5 μM[5].
Dequalinium (0-100 μg/mL, 72 h) chloride inhibits cell growth in human Pca cell lines (PC3, DU145, LNCaP, MDA-PCA-2B), and induces cell apoptosis in PC3 cells (0.9 μM, 4 h)[7].

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

Solvant et solubilité
In Vitro: 

H2O : 0.99 mg/mL (1.88 mM; ultrasonic and warming and adjust pH to 3 with 1 M HCl and heat to 60°C)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8955 mL 9.4774 mL 18.9548 mL
5 mM --- --- ---
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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: 2 mg/mL (3.79 mM); Suspended solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Pureté et documentation
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