Dequalinium Chloride
Based on 1 Customer Validation
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.
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- Pureza: 99.72%
- No. CAS: 522-51-0
- Fòrmula: C30H40Cl2N4
- Peso molecular:527.57
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Almacenamiento:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Astrocyte | EC50 |
1.418 μM
Compound: 29
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Antiproliferative activity against mouse astrocyte cells by MTT assay
Antiproliferative activity against mouse astrocyte cells by MTT assay
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[PMID: 17417631] |
| HEK293 | IC50 |
1.3 μM
Compound: 15
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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
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[PMID: 18774291] |
| HEK293 | IC50 |
2 μM
Compound: 15
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Inhibition of Kca2.3 channel expressed in HEK293 cells by electrophysiology assay
Inhibition of Kca2.3 channel expressed in HEK293 cells by electrophysiology assay
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[PMID: 18774291] |
| Hepatocyte | IC50 |
1.7 μM
Compound: 2
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Inhibition of apamin-sensitive SKCa channel of guinea-pig hepatocytes
Inhibition of apamin-sensitive SKCa channel of guinea-pig hepatocytes
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[PMID: 15225721] |
| HepG2 | IC50 |
>100 μM
Compound: 92125541
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HARVARD: Cytotoxicity in HepG2 cell line
HARVARD: Cytotoxicity in HepG2 cell line
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[PMID: 22586124] |
| HepG2 | IC50 |
1.71 μM
Compound: 92125541
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HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells
HARVARD: Inhibition of liver stage Plasmodium berghei infection in HepG2 cells
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[PMID: 22586124] |
| Huh-7 | CC50 |
30.99 μM
Compound: GNF-Pf-5483
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NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
NOVARTIS: Cytotoxicity against human hepatocellular carcinoma cell line (Huh7)
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[PMID: 18579783] |
| Sympathetic neuron | IC50 |
0.65 μM
Compound: Dequalinium
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Inhibition of after-hyperpolarization (AHP) in cultured rat sympathetic neurons
Inhibition of after-hyperpolarization (AHP) in cultured rat sympathetic neurons
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[PMID: 8863802] |
| Sympathetic neuron | IC50 |
0.74 μM
Compound: dequalinium (4)
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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
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[PMID: 7658440] |
| Sympathetic neuron | IC50 |
0.74 μM
Compound: 1
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Ability to inhibit the hyperpolarization (AHP) in cultured rat sympathetic neurons
Ability to inhibit the hyperpolarization (AHP) in cultured rat sympathetic neurons
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10.1016/0960-894X(95)00073-3 |
| Sympathetic neuron | IC50 |
0.74 μM
Compound: Dequalinium
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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).
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[PMID: 7861407] |
| Sympathetic neuron | IC50 |
0.9 μM
Compound: Dequalinium
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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.
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[PMID: 8784458] |
| Sympathetic neuron | IC50 |
1 μM
Compound: 22(dequalinium)
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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
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[PMID: 8558503] |
| Sympathetic neuron | IC50 |
490 nM
Compound: dequalinium
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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
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[PMID: 11000001] |
| Sympathetic neuron | IC50 |
570 nM
Compound: Deq
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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
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[PMID: 9438015] |
| Sympathetic neuron | IC50 |
900 nM
Compound: Dequalinium
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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
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[PMID: 15261276] |
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.
Dequalinium chloride (2 mg/kg, i.p., daily for 10 days) inhibits the tumor growth of mouse bladder carcinoma MB49[3].
Dequalinium chloride (2 mg/kg, s.c.) reduces Diisopropylfluorophosphate-induced tremors (organophosphate poisoning) in mice[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 522-51-0
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Appearance Solid
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Peso molecular 527.57
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Fòrmula C30H40Cl2N4
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Color Off-white to light yellow
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SMILES
CC1=[N+](C2=CC=CC=C2C(N)=C1)CCCCCCCCCC[N+](C3=CC=CC=C3C(N)=C4)=C4C.[Cl-].[Cl-]
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 50% PEG300 50% Saline
Solubility: 2 mg/mL (3.79 mM); Suspended solution; Need ultrasonic
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Kramer, W., [Treatment of tonsillitis with dequalinium chloride]. Fortschr Med, 1977. 95(16): p. 1108-10. [Content Brief]
[2]. Gamboa-Vujicic, G., et al., Toxicity of the mitochondrial poison dequalinium chloride in a murine model system. J Pharm Sci, 1993. 82(3): p. 231-5. [Content Brief]
[3]. Belanger-Coast MG, et al. Dequalinium chloride is an antagonists of α7 nicotinic acetylcholine receptors. Eur J Pharmacol. 2022 Jun 15;925:175000. [Content Brief]
[4]. Mendling W, et al. Use of locally delivered dequalinium chloride in the treatment of vaginal infections: a review. Arch Gynecol Obstet. 2016 Mar;293(3):469-84. [Content Brief]
[5]. Castle NA, et al. Dequalinium: a potent inhibitor of apamin-sensitive K+ channels in hepatocytes and of nicotinic responses in skeletal muscle. Eur J Pharmacol. 1993 May 19;236(2):201-7. [Content Brief]
[6]. Bugay V, et al. Effects of Sublethal Organophosphate Toxicity and Anti-cholinergics on Electroencephalogram and Respiratory Mechanics in Mice. Front Neurosci. 2022 May 2;16:866899. [Content Brief]
[7]. Abdul M, et al. Expression and activity of potassium ion channels in human prostate cancer. Cancer Lett. 2002 Dec 1;186(1):99-105. [Content Brief]
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O | 1 mM | 1.8955 mL | 9.4774 mL | 18.9548 mL | 47.3871 mL |
* 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.
Dequalinium Chloride Related Classifications
HY-B0567 Related Classifications
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