产品介绍 |
Hexachlorophene (Hexachlorofen) 是一种有效的抗菌 (antibacterial) 剂, 抗真菌 (antifungal) 剂。Hexachlorophene可导致原生质体的裂解和细菌内容物的渗漏。Hexachlorophene 是 SARS-CoV 3CL 蛋白酶抑制剂,其 IC50 值为 5 μM。Hexachlorophene 也是一种有效的 KCNQ1/KCNE1 钾通道激活剂,其 EC50 值为 4.61 μM。Hexachlorophene 还可抑制 Wnt/β-catenin 信号通路,可用于心律失常,细菌,癌症等方面的研究。
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生物活性 |
Hexachlorophene (Hexachlorofen) is an effective anti-bacterial and antifungal agent. Hexachlorophene can cause lysis of protoplasts and leakage of intracellular contents in bacterial. Hexachlorophene is an inhibitor of SARS-CoV 3CL protease with an IC50 value of 5 μM. Hexachlorophene is also a potent KCNQ1/KCNE1 potassium channel activator with an EC50 value of 4.61 μM. Hexachlorophene inhibits Wnt/β-catenin signaling as well, and can be used in the research of arrhythmia, bacterial, cancers[4].
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体外研究 |
Hexachlorophene (0.1-10 μM approximately) increases the current amplitude of KCNQ1/KCNE1 with an EC50 value of 4.61 μM, and shortens the action potential.
Hexachlorophene (10 μM) rescues the loss of function of the LQTs mutants caused by either impaired activation gating or PIP2 binding affinity in CHO cells.
Hexachlorophene (0-50 μg/mL approximately, 30 min) has antibacterial activities against micrococcus sp., staphylococcus, staphylococcus epidermidis and streptococcus with IC50 values of 0.83 μg/mL, 1.5 μg/mL, 1.75 μg/mL, 1.3 μg/mL, respectively.
Hexachlorophene (20 μM, 15 h) inhibits Wnt/β-catenin signaling through the Siah-1-mediated β-catenin degradation in HEK293 and HCT116 cells.
Hexachlorophene (0-10 μM, 48 h) inhibits the growth of HCT116 cells.
Hexachlorophene is a competitive inhibitor of SARS-CoV 3CL with an IC50 value of 5 μM, and can form hydrogen bonds with SARS-CoV 3CL with Ki value estimated to be 4 μM[4].
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
Western Blot Analysis
Cell Line: |
HEK293 cells |
Concentration: |
0-40 μM |
Incubation Time: |
15 h |
Result: |
Degraded β-catenin response transcription (CRT) induced by Wnt3a CM by promoting the degradation of β-catenin, with an IC50 value of 7.03 μM. |
Cell Proliferation Assay
Cell Line: |
HCT116 colon cancer cells |
Concentration: |
0, 1.25, 2.5, 5, 10 μM. |
Incubation Time: |
48 h |
Result: |
Inhibited the growth of HCT116 cells in a concentration-dependent manner. |
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体内研究 (In Vivo) |
Hexachlorophene (tail immersion for 5 minutes, 1.25% w/v, one day prior to cercarial exposure) has inhibitory activity against Schistosoma mansoni infections in mice (exposed to WRAIR,Puerto Rican strain)[6].
Hexachlorophene has acute and subacute toxic effects with i.p. LD50 ranged between 21.8 mg/kg-40.0 mg/kg, and the oral LD50 varied from 57.6 to 87.0 mg/kg, respectively[5].
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: |
Wistar rats (acute and subacute assays)[5] |
Dosage: |
0-100 mg/kg approximately |
Administration: |
Intraperitoneal injection or oral administration |
Result: |
Displayed acute and subacute toxic effects with i.p. LD50 ranged between 21.8 mg/kg-40.0 mg/kg, and the oral LD50 varied from 57.6 to 87.0 mg/kg, respectively. |
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体内研究 |
Hexachlorophene (tail immersion for 5 minutes, 1.25% w/v, one day prior to cercarial exposure) has inhibitory activity against Schistosoma mansoni infections in mice (exposed to WRAIR,Puerto Rican strain)[6].
Hexachlorophene has acute and subacute toxic effects with i.p. LD50 ranged between 21.8 mg/kg-40.0 mg/kg, and the oral LD50 varied from 57.6 to 87.0 mg/kg, respectively[5].
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: |
Wistar rats (acute and subacute assays)[5] |
Dosage: |
0-100 mg/kg approximately |
Administration: |
Intraperitoneal injection or oral administration |
Result: |
Displayed acute and subacute toxic effects with i.p. LD50 ranged between 21.8 mg/kg-40.0 mg/kg, and the oral LD50 varied from 57.6 to 87.0 mg/kg, respectively. |
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体内研究 |
Hexachlorophene (tail immersion for 5 minutes, 1.25% w/v, one day prior to cercarial exposure) has inhibitory activity against Schistosoma mansoni infections in mice (exposed to WRAIR,Puerto Rican strain)[6].
Hexachlorophene has acute and subacute toxic effects with i.p. LD50 ranged between 21.8 mg/kg-40.0 mg/kg, and the oral LD50 varied from 57.6 to 87.0 mg/kg, respectively[5].
西域 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: |
Wistar rats (acute and subacute assays)[5] |
Dosage: |
0-100 mg/kg approximately |
Administration: |
Intraperitoneal injection or oral administration |
Result: |
Displayed acute and subacute toxic effects with i.p. LD50 ranged between 21.8 mg/kg-40.0 mg/kg, and the oral LD50 varied from 57.6 to 87.0 mg/kg, respectively. |
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性状 | Solid |
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溶解性数据 |
In Vitro:
DMSO : ≥ 100 mg/mL (245.76 mM)
H2O : 0.1 mg/mL (0.25 mM; Need ultrasonic)
* "≥" means soluble, but saturation unknown.
配制储备液
浓度
溶剂体积
质量
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1 mg |
5 mg |
10 mg |
1 mM |
2.4576 mL |
12.2880 mL |
24.5761 mL |
5 mM |
0.4915 mL |
2.4576 mL |
4.9152 mL |
10 mM |
0.2458 mL |
1.2288 mL |
2.4576 mL |
*
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
In Vivo:
请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 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,建议您现用现配,当天使用;
以下溶剂前显示的百 分比是指该溶剂在您配制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
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1.
请依序添加每种溶剂: 10% DMSO 40% PEG300 5% Tween-80 45% saline Solubility: ≥ 2.5 mg/mL (6.14 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.14 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。
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2.
请依序添加每种溶剂: 10% DMSO 90% (20% SBE-β-CD in saline) Solubility: ≥ 2.5 mg/mL (6.14 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.14 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。
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3.
请依序添加每种溶剂: 10% DMSO 90% corn oil Solubility: ≥ 2.5 mg/mL (6.14 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.14 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。
*以上所有助溶剂都可在 西域 网站选购。
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运输条件 |
Room temperature in continental US; may vary elsewhere.
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储存方式 |
Powder |
-20°C |
3 years |
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4°C |
2 years |
In solvent |
-80°C |
6 months |
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-20°C |
1 month |
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参考文献 | |
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