Dequalinium Chloride | Dequalinium (chloride) | Potassium Channel Inhibitor

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地喹氯铵 /Dequalinium Chloride {[allProObj[0].p_purity_real_show]}

货号：A666741 同义名： Dequalinium (chloride);NSC 166454

Dequalinium Chloride is a PKC inhibitor with IC50 of 7-18 μM, and also a selective blocker of apamin-sensitive K+ channels with IC50 of 1.1 μM.

Dequalinium Chloride 化学结构
CAS号：522-51-0

Dequalinium Chloride 3D分子结构
CAS号：522-51-0

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Dequalinium Chloride 纯度/质量文件产品仅供科研

货号：A666741 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

转化生长因子-β 亚型比较
钾通道亚型比较
PKC 亚型比较

产品名称	ALK1 ↓ ↑	ALK2 ↓ ↑	ALK3 ↓ ↑	ALK4 ↓ ↑	ALK6 ↓ ↑	Smad3 ↓ ↑	TGF-β ↓ ↑	TGFβRI/ALK5 ↓ ↑	TGFβRII ↓ ↑	纯度
LDN193189	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%+
LDN-212854	++++ ALK1, IC50: 2.4 nM	++++ ALK2, IC50: 1.3 nM	+ ALK3, IC50: 85.8 nM	+ ALK4, IC50: 2133 nM				+ ALK5, IC50: 9276 nM		99%+
ML347	++ ALK1, IC50: 46 nM	++ ALK2, IC50: 32 nM								98%
K02288	++++ ALK1, IC50: 1.8 nM	++++ ALK2, IC50: 1.1 nM	++ ALK3, IC50: 34.4 nM		+++ ALK6, IC50: 6.4 nM					99%+
LDN-193189 dihydrochloride	++++ ALK1, IC50: 0.8 nM	++++ ALK2, IC50: 0.8 nM	+++ ALK3, IC50: 5.3 nM		+++ ALK6, IC50: 16.7 nM					99%
LDN-214117		++ ALK2, IC50: 24 nM								98%
DMH-1		+ ALK2, IC50: 107.9 nM								99%+
SB-505124				+ ALK4, IC50: 129 nM				++ ALK5, IC50: 47 nM		99%+
Vactosertib				+++ ALK4, IC50: 13 nM				+++ ALK5, IC50: 11 nM		99%+
Alantolactone						✔				98%
SIS3						✔				97%
Pirfenidone							✔			98%
Hesperetin							✔			97%
RepSox								++++ TGFβR1(ALK5), IC50: 4 nM		98%
GW788388								+++ ALK5, IC50: 18 nM		98%
LY364947								++ TGFβRI, IC50: 59 nM	+ TGFβRII, IC50: 0.4 μM	98%
SD-208								++ TGF-βRI (ALK5), IC50: 48 nM		98%
SB-525334								+++ TGFβR1(ALK5), IC50: 14.3 nM		99%+
LY2109761								++ TβRI, Ki: 38 nM	+ TβRII, Ki: 300 nM	99%+
Galunisertib								++ TβRI, IC50: 56 nM		98%
SB 431542								+ ALK5, IC50: 94 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	Potassium Channel ↓ ↑	纯度
Tolbutamide	✔	98%
Glimepiride	++++ SUR2B, IC50: 7.3 nM SUR1, IC50: 5.4 nM	97%
Dronedarone Hydrochloride	✔	95%
Gliquidone	++ Potassium channel, IC50: 27.2 nM	98%
TRAM-34	+++ IKCa1 (KCa3.1), Kd: 20 nM	98%
Glibenclamide	✔	98%
Amiodarone HCl	✔	97%
Gliclazide	++ Potassium channel, IC50: 184 nM	98%
Repaglinide	✔	98%
Dofetilide	✔	98%
Nateglinide	✔	99%
Quinine hydrochloride dihydrate	✔	98%
ML133 HCl	+ Kir2.1, IC50: 290 nM	97%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	PKC ↓ ↑	PKCα ↓ ↑	PKCβ ↓ ↑	PKCγ ↓ ↑	PKCδ ↓ ↑	PKCε ↓ ↑	PKCζ ↓ ↑	PKCη ↓ ↑	PKCθ ↓ ↑	其他靶点	纯度
Daphnetin	+ PKC, IC50: 25.01 μM									PKA,EGFR	95%
Dequalinium Chloride											99%+
Quercetin	✔									Src,Sirtuin	97%
Myricetrin		✔									96%
Go 6983		+++ PKCα, IC50: 7 nM	+++ PKCβ, IC50: 7 nM	+++ PKCγ, IC50: 6 nM	+++ PKCδ, IC50: 10 nM		++ PKCζ, IC50: 60 nM				99%+
Go6976	+++ PKC, IC50: 7.9 nM	++++ PKCα, IC50: 2.3 nM	+++ PKCβ1, IC50: 6.2 nM							FLT3	99%+
Bisindolylmaleimide I		+++ PKCα, IC50: 20 nM	+++ PKCβ1, IC50: 17 nM PKCβ2, IC50: 16 nM	+++ PKCγ, IC50: 20 nM							99%+
Lawsone methyl ether			✔								99%
Sotrastaurin		++++ PKCα, Ki: 0.95 nM	++++ PKCβ1, Ki: 0.64 nM		++++ PKCδ, Ki: 2.1 nM	++++ PKCε, Ki: 3.2 nM		++++ PKCη, Ki: 1.8 nM	++++ PKCθ, Ki: 0.22 nM		99%+
Enzastaurin		++ PKCα, IC50: 39 nM	+++ PKCβ, IC50: 6 nM	+ PKCγ, IC50: 83 nM		+ PKCε, IC50: 110 nM					98%
Midostaurin		++ PKCα, IC50: 22 nM	++ PKCβ1, IC50: 30 nM PKCβ2, IC50: 31 nM	++ PKCγ, IC50: 24 nM	+ PKCδ, IC50: 330 nM	+ PKCε, IC50: 1.25 μM		+ PKCη, IC50: 160 nM			99%
Ro 31-8220 mesylate		++++ PKCα, IC50: 5 nM	+++ PKCβ1, IC50: 24 nM PKCβ2, IC50: 14 nM	++ PKCγ, IC50: 27 nM		++ PKCε, IC50: 24 nM					99%+
Staurosporine		++++ PKCα, IC50: 2 nM		++++ PKCγ, IC50: 5 nM	+++ PKCδ, IC50: 20 nM	++ PKCε, IC50: 73 nM		++++ PKCη, IC50: 4 nM			99%+
Ruboxistaurin HCl		+ PKCα, IC50: 0.36 μM	++++ PKCβ1, IC50: 4.7 nM PKCβ2, IC50: 5.9 nM	+ PKCγ, IC50: 0.3 μM	+ PKCδ, IC50: 0.25 μM			++ PKCη, IC50: 0.052 μM			99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

Dequalinium Chloride 生物活性

靶点

PKC

PKC, IC50:7 μM-18 μM

描述

Dequalinium chloride (DECA), a cationic, lipophilic mitochondrial poison, selectively targets the mitochondrial membrane of certain epithelial carcinoma cells, in which it inhibits cellular energy production. After a single ip administration, we found a maximum tolerated dose of 15 mg/kg and a lethal dose (LD50) of 18.3 mg/kg. Single ip doses of 20 and 25 mg/kg produced > 50% mortality^[3]. The compound antagonized M3 mACHRs (M3 muscarinic receptor) with an IC50 of 0.27 μM for dequalinium chloride^[4]. Dequalinium chloride (DQC) is an anti-microbial antiseptic agent with a broad bactericidal and fungicidal activity. Vaginal DQC (Fluomizin vaginal tablets) has been shown to have equal clinical efficacy as clindamycin in the treatment of BV(bacterial vaginosis)^[5]. Dequalinium chloride inhibits and kills clinical isolates of A. vaginae at concentrations similar to those of clindamycin and lower than those of metronidazole^[6].

Dequalinium Chloride 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02242695	Vulvovaginal Candidiasis	Phase 4	Completed	-	Thailand ... 展开 >> Siriraj Gynaecologic ID and Female STD Unit, Department of Obstetrics & Gynaecology, Faculty of Medicine Siriraj Hospital, Mahidol University Bangkok, Bangkok Noi district, Thailand, 10700 收起 <<
NCT01125410	Bacterial Vaginosis	Phase 3	Completed	-	Belgium ... 展开 >> AZ Imelda Ziekenhuis Bonheiden, Belgium AZ St. Dimpna Geel, Belgium AZ Ziekenhuis Oost-Limburg Genk, Belgium AZ Heilig Hart Tienen, Belgium Czech Republic Centrum Ambulantni gynekologie a prodnictvi Brno, Czech Republic Faculty Hospital Brno Brno, Czech Republic University Hospital Hradec Kralove Hradec Kralove, Czech Republic Charles University Prague, Czech Republic Fakultni nemocnice Na Bulovce Prague, Czech Republic Ambulance pro gynekologie a prodnictvi Telc, Czech Republic Germany LMU Munich Munich, Germany Slovakia JLF UK a MFN Martin, Slovakia Switzerland University Hospital of Geneva and Faculty of Medicine Geneva, Switzerland CHUV Lausanne, Switzerland 收起 <<

Dequalinium Chloride 参考文献

[1]Dunn PM. Dequalinium, a selective blocker of the slow afterhyperpolarization in rat sympathetic neurones in culture. Eur J Pharmacol. 1994 Feb 3;252(2):189-94.

[2]Manetta A, Emma D, et al. Failure to enhance the in vivo killing of human ovarian carcinoma by sequential treatment with dequalinium chloride and tumor necrosis factor. Gynecol Oncol. 1993 Jul;50(1):38-44.

[3]Gamboa-Vujicic G, Emma DA, Liao SY, Fuchtner C, Manetta A. Toxicity of the mitochondrial poison dequalinium chloride in a murine model system. J Pharm Sci. 1993 Mar;82(3):231-5

[4]Bugay V, Wallace DJ, Wang B, Salinas I, Chapparo AP, Smith HR, Dube PH, Brooks EG, Berg KA, Brenner R. Bis-Quinolinium Cyclophane Blockers of SK Potassium Channels Are Antagonists of M3 Muscarinic Acetylcholine Receptors. Front Pharmacol. 2020 Sep 16;11:552211

[5]Mendling W, Weissenbacher ER, Gerber S, Prasauskas V, Grob P. Use of locally delivered dequalinium chloride in the treatment of vaginal infections: a review. Arch Gynecol Obstet. 2016 Mar;293(3):469-84

[6]Lopes dos Santos Santiago G, Grob P, Verstraelen H, Waser F, Vaneechoutte M. Susceptibility testing of Atopobium vaginae for dequalinium chloride. BMC Res Notes. 2012 Mar 19;5:151

Dequalinium Chloride 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.90mL

0.38mL

0.19mL

9.48mL

1.90mL

0.95mL

18.95mL

3.79mL

1.90mL

Dequalinium Chloride 技术信息

CAS号	522-51-0
分子式	C₃₀H₄₀Cl₂N₄
分子量	527.571

别名	Dequalinium (chloride);NSC 166454;Dequavagyn
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

溶解度

动物实验配方

地喹氯铵 /Dequalinium Chloride {[allProObj[0].p_purity_real_show]}

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