Dequalinium Chloride 是 Apamin

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 可阻断豚鼠肝细胞中血管紧张素 II (100 nM) 诱发的 K⁺ 损失，IC₅₀ 为 1.5 μM^[5]。
Dequalinium (0-100 μg/mL, 72 h) chloride 抑制人 Pca 细胞系 (PC3、DU145、LNCaP、MDA-PCA-2B) 中的细胞生长，并诱导 PC3 细胞中的细胞凋亡 (0.9 μM, 4 h)^[7]。

Dequalinium chloride 在小鼠中的 LD₅₀ 为 18.3 mg/kg (腹腔注射，单次)^[2]。
Dequalinium chloride (2 mg/kg，腹膜内注射，每日一次，持续 10 天) 抑制小鼠膀胱癌 (MB49皮下瘤) 的肿瘤生长^[3] 。
Dequalinium chloride (2 mg/kg，皮下注射) 可减少二异丙基氟磷酸盐引起的小鼠震颤 (有机磷中毒)^[6]。

528.00

C₃₀H₄₀Cl₂N₄

522-51-0

固体

Off-white to light yellow

地喹氯铵；地喹氯胺；克菌定

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)

• [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]