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转化生长因子-β
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/ Dequalinium Chloride/地喹氯铵

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

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

Dequalinium Chloride是一种 PKC 抑制剂，IC50 值为 7-18 μM，同时也是一种选择性钾通道阻滞剂，能阻止 apamin 敏感的 K+ 通道，IC50 为 1.1 μM。

Dequalinium Chloride/地喹氯铵 化学结构 CAS号：522-51-0
Dequalinium Chloride/地喹氯铵 化学结构
CAS号：522-51-0
Dequalinium Chloride/地喹氯铵 3D分子结构
CAS号：522-51-0
Dequalinium Chloride/地喹氯铵 化学结构 CAS号：522-51-0
Dequalinium Chloride/地喹氯铵 3D分子结构 CAS号：522-51-0
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Dequalinium Chloride/地喹氯铵 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]}
批次查询： 批次纯度:

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更多 >
产品名称 ALK1 ↓ ALK2 ↓ ALK3 ↓ ALK4 ↓ ALK6 ↓ Smad3 ↓ TGF-β ↓ TGFβRI/ALK5 ↓ TGFβRII ↓ 其他靶点 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 2HCl ++++

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%
(E/Z)-SIS3 free base ✔ 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

 		99%
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 ↓ 其他靶点 纯度
Tolbutamide ✔ 98%
Glimepiride ++++

SUR1, IC50: 5.4 nM

SUR2B, IC50: 7.3 nM

 		97%
Dronedarone HCl ✔ 95%
Gliquidone ++

Potassium channel, IC50: 27.2 nM

 		99%
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 HCl dihydrate ✔ 98%
ML133 HCl +

Kir2.1, IC50: 290 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 PKC ↓ PKCα ↓ PKCβ ↓ PKCγ ↓ PKCδ ↓ PKCε ↓ PKCζ ↓ PKCη ↓ PKCθ ↓ 其他靶点 纯度
Daphnetin +

PKC, IC50: 25.01 μM

 		EGFR,PKA 95%
Dequalinium Chloride 99%+
Quercetin ✔ Sirtuin,Src 95%
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

 		+++

PKCβ2, IC50: 16 nM

PKCβ1, IC50: 17 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

 		++

PKCβ2, IC50: 31 nM

PKCβ1, IC50: 30 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

 		+++

PKCβ2, IC50: 14 nM

PKCβ1, IC50: 24 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

 		++++

PKCβ2, IC50: 5.9 nM

PKCβ1, IC50: 4.7 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/地喹氯铵 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/地喹氯铵 细胞实验

Cell Line
Concentration Treated Time Description References
HEK 293 cells 30 μM Inhibited TRPM7-mediated Ca2+ influx Br J Pharmacol. 2012 Jun;166(4):1357-76.
293T cells 10 μM 24 hours Screening FDA-approved drug library for compounds that interfere with Cdc7-Dbf4 interaction EBioMedicine. 2018 Oct;36:241-251.
African green monkey kidney epithelial cell line CV-1 250 μM 3 hours Evaluate the toxicity of Dequalinium to CV-1 cells, showing an IC50 of 250 μM Proc Natl Acad Sci U S A. 1987 Aug;84(15):5444-8.
Human breast carcinoma cell line MCF-7 2 μM 3 hours Evaluate the toxicity of Dequalinium to MCF-7 cells, showing an IC50 of 2 μM, 125-fold more toxic than CV-1 cells Proc Natl Acad Sci U S A. 1987 Aug;84(15):5444-8.
NB TICs (NB12, NB88R2, NB122R) 100 nM 72 hours Significantly reduced cell viability and induced apoptosis EMBO Mol Med. 2010 Sep;2(9):371-84.
NB TICs (NB12) 100 nM 24 hours Induced apoptosis, characterized by nuclear morphology changes and increased sub-2n DNA content EMBO Mol Med. 2010 Sep;2(9):371-84.
Yeast cells 0.7-4 μM 24 hours DECA inhibits Su9-Ura3 import into mitochondria Proc Natl Acad Sci U S A. 2014 Oct 7;111(40):14406-11.
CHO-K1 cells 2-10 μM 4 hours DECA inhibits mitochondrial protein translocation and restores AGTP11LG170R trafficking to peroxisomes Proc Natl Acad Sci U S A. 2014 Oct 7;111(40):14406-11.
Rat cultured sympathetic neurones 0.60 ± 0.05 μM 1-3 minutes To evaluate the inhibitory effect of Dequalinium on SKCa channels in sympathetic neurones, results showed that Dequalinium effectively inhibited the slow afterhyperpolarization (AHP). Br J Pharmacol. 1996 Jan;117(1):35-42.
HEK293 cells 0.4 μM Investigated the blocking effect of Dequalinium on hSK1 current, with an IC50 of 0.48 μM. Br J Pharmacol. 2000 Feb;129(4):627-30.
Rat superior cervical ganglion (SCG) neurones 0.62 μM Test the inhibitory effect of Dequalinium on SK Ca channels, results showed weak inhibition Br J Pharmacol. 2000 Apr;129(7):1431-8.
Rabbit blood cells 410 μM Test the inhibitory effect of Dequalinium on IK Ca channels, results showed weak inhibition Br J Pharmacol. 2000 Apr;129(7):1431-8.
OEC-M1 cells 2 μM 48 hours Evaluating the inhibitory effect of Dequalinium chloride on Cdc7-Dbf4 kinase activity EBioMedicine. 2018 Oct;36:241-251.
HEK 293 cells 444 nM To investigate the inhibitory effect of Dequalinium Chloride on hSK1 and rSK2 channels, showing IC50 values of 444 nM and 162 nM for hSK1 and rSK2, respectively. Br J Pharmacol. 2000 Mar;129(5):991-9.

Dequalinium Chloride/地喹氯铵 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
BALB/c nude mice Subcutaneous OEC-M1 oral carcinoma xenograft model Oral administration 15 mg/kg Twice a week for six consecutive weeks Evaluating the antitumor activity of Dequalinium chloride in vivo EBioMedicine. 2018 Oct;36:241-251.
BDF1 mice I.p. implanted mouse bladder carcinoma MB49 Intraperitoneal injection 2 mg/kg or 4 mg/kg Daily or every other day for 25 days Evaluate the survival prolongation effect of Dequalinium on MB49 tumors, showing a T/C (treated/control ratio) of 190%, more effective than seven anticancer drugs Proc Natl Acad Sci U S A. 1987 Aug;84(15):5444-8.
Zebrafish Embryonic development model Solution treatment 20 μM 3 days DECA does not affect zebrafish embryonic development at low concentrations Proc Natl Acad Sci U S A. 2014 Oct 7;111(40):14406-11.
Rats PGE2-induced hyperalgesia model Subcutaneous injection 50 mg/paw Single administration, measured after 30 minutes To evaluate the effect of Dequalinium on baclofen-induced peripheral antinociception, results showed no significant effect Br J Pharmacol. 2006 Nov;149(6):733-9

Dequalinium Chloride/地喹氯铵 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/地喹氯铵 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/地喹氯铵 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/地喹氯铵 技术信息

CAS号522-51-0
分子式C30H40Cl2N4
分子量 527.57
SMILES Code CC1=[N+](C2=CC=CC=C2C(N)=C1)CCCCCCCCCC[N+](C3=CC=CC=C3C(N)=C4)=C4C.[Cl-].[Cl-]
MDL No. MFCD00063502
别名 Dequalinium (chloride); NSC 166454; Dequavagyn
运输蓝冰
InChI Key LTNZEXKYNRNOGT-UHFFFAOYSA-N
Pubchem ID 10649
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Inert atmosphere, 2-8°C
溶解方案 请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议现用现配，当天使用； 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶
方案 一

Tags: Dequalinium | 522-51-0 | Potassium Channel Inhibitor | Membrane Transporter/Ion Channel | Neuronal Signaling | Apoptosis | Anti-infection | Potassium Channel | nAChR | Apoptosis | Bacterial | Parasite | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Dequalinium Chloride/地喹氯铵 纯度/质量文件 | Dequalinium Chloride/地喹氯铵 亚型比较 | Dequalinium Chloride/地喹氯铵 生物活性 | Dequalinium Chloride/地喹氯铵 临床数据 | Dequalinium Chloride/地喹氯铵 参考文献 | Dequalinium Chloride/地喹氯铵 实验方案 | Dequalinium Chloride/地喹氯铵 技术信息

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