塩化デカリニウム  (Synonyms: Dequalinium (Chloride))

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].

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 shows a LD₅₀ of 18.3 mg/kg in mice (i.p., a single time)^[2].
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.

527.57

C₃₀H₄₀Cl₂N₄

522-51-0

Solid

Off-white to light yellow

CC1=[N+](C2=CC=CC=C2C(N)=C1)CCCCCCCCCC[N+](C3=CC=CC=C3C(N)=C4)=C4C.[Cl-].[Cl-]

Room temperature in continental US; may vary elsewhere.

4°C, sealed storage, away from moisture

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

* 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.

• [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]