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Alexidine dihydrochloride
目录号: PC10108 纯度: ≥98%
CAS No. :1715-30-6
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中文名称
Alexidine dihydrochloride
中文别名
盐酸阿立西定;己联双辛胍二盐酸盐;N1,N14-二(2-乙基己基)-3,12-二亚胺-2,4,11,13-四氮杂十四烷二脒盐酸盐(1:2)
英文名称
Alexidine dihydrochloride
英文别名
2,4,11,13-Tetraazatetradecanediimidamide,N1,N14-bis(2-ethylhexyl)-3,12-diimino-, hydrochloride (1:2);2,4,11,13-Tetraazatetradecanediimidamide,N1,N14-bis(2-ethylhexyl)-3,12-diimino-, hydrochloride...;Alexidine (hydrochloride);Alexidine dihydrochloride;Alexidine dihydrochloride,N,N\'\'-Bis(2-ethylhexyl)-3,12-diimino-2,4,11,13-tetraazatetradecanediimidamidedihydrochloride;Alexidine dihydrochloride,N,N''-Bis(2-ethylhexyl)-3,12-diimino-2,4,11,13-tetraazatetradecanediimidamidedihydrochloride;1,1'-Hexamethylene-bis(5-[2-ethylhexyl]biguanide);alexidine 2HCl;Bisguadine;Bisguanidine;Compound-904;QR-711;Sterwin 904;1,1′-Hexamethylene-bis(5-[2-ethylhexyl]biguanide);WIN-21904;1,1'-Hexamethylenebis[5-(2-ethylhex-1-yl)]biguanide dihydrochloride;N,N''-Bis(2-ethylhexyl)-3,12-diiMino-2,4,11,13-tetraazatetradecanediiMidaMide;N,N''-bis(2-ethylhexyl)-3,12-diimino-2,4,11,13-tetraazatetradecanediamidine dihydrochloride;N,N''-Bis(2-ethylhexyl)-3,12-diimino-2,4,11,13-tetraazatetradecanediimidamidedihydrochloride
Cas No.
1715-30-6
分子式
C26H58Cl2N10
分子量
581.71
包装储存

-20°C, sealed storage, away from moisture

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

生物活性

Alexidine dihydrochloride is an anticancer agent that targets a mitochondrial tyrosine phosphatase, PTPMT1, in mammalian cells and causes mitochondrial apoptosis. Alexidine dihydrochloride has antifungal and antibiofilm activity against a diverse range of fungal pathogens.

性状

Solid

IC50 & Target[1][2]

PTPMT1

体外研究(In Vitro)

Alexidine dihydrochloride displays activity against most Candida spp.; MIC values of ≤1.5?μg/mL are observed for all isolates tested under planktonic conditions, with the exception of Candida parapsilosis and Candida krusei. Interestingly, Alexidine dihydrochloride also displays striking activity against clinically relevant fluconazole-resistant Candida isolates: C. albicans (CA2, CA6, and CA10), C. glabrata (CG2 and CG5), C. parapsilosis (CP5), and C. auris (CAU-09 and CAU-03).
Inhibition of planktonic growth by Alexidine dihydrochloride reveals a complete inhibition of filamentation or proliferation of the imaged fungi. Alexidine dihydrochloride is able to decimate at low concentrations (1.5 to 6?μg/mL) mature biofilms of Candida, Cryptococcus, and Aspergillus spp. that are known to be resistant to almost all classes of antifungal drugs. In fact, at 10-fold-lower concentrations (150?ng/mL) of planktonic MICs, Alexidine dihydrochloride could inhibit lateral yeast formation and biofilm dispersal in C. albicans.
Alexidine dihydrochloride results in 50% killing of HUVECs and lung epithelial cells, at concentrations 5- to 10-fold higher than the MIC required to kill planktonically growing fungal pathogens.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Chosen to focus on biofilm formation by C. albicans, since a murine biofilm model has been well established in this fungus and used for testing the effects of established and new antifungal agents. The effect of the drugs on the 24-h-old biofilms growing in the jugular vein catheters of mice is visualized microscopically, which reveals significantly lower density of the biofilms in catheters treated with Alexidine dihydrochloride. In fact, fungal CFU determination reveals that Alexidine dihydrochloride inhibits 67% of fungal biofilm growth and viability, compared to the control untreated biofilms.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

-20°C, sealed storage, away from moisture

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

参考文献
溶解度数据
体外研究: 

DMSO : 125 mg/mL (214.88 mM; Need ultrasonic)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7191 mL 8.5953 mL 17.1907 mL
5 mM 0.3438 mL 1.7191 mL 3.4381 mL
10 mM 0.1719 mL 0.8595 mL 1.7191 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,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 (sealed storage, away from moisture)。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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

  • 1.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.58 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 2.

    建议依照次序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.58 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 3.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.58 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.58 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 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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