己联双辛胍二盐酸盐
中文名称 | 己联双辛胍二盐酸盐 |
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中文同义词 | 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);阿来西定 二盐酸盐;N,N''-双(2-乙基己基)-3,12-二亚氨基-2,4,11,13-四氮杂十四烷二亚胺二盐酸盐;N,N''-双(2-乙基己基)-3,12-二亚氨基-2,4,11,13-四氮杂十四烷二亚胺二盐酸盐 |
英文名称 | N,N''-bis(2-ethylhexyl)-3,12-diimino-2,4,11,13-tetraazatetradecanediamidine dihydrochloride |
英文同义词 | Bisguanidine;N,N''-Bis(2-ethylhexyl)-3,12-diiMino-2,4,11,13-tetraazatetradecanediiMidaMide;Sterwin 904;1,1'-Hexamethylenebis[5-(2-ethylhex-1-yl)]biguanide dihydrochloride;Alexidine dihydrochloride, N,N''''-Hexane-1,6-diylbis[N'-(2-ethylhex-1-yl)(imidodicarbonimidic diamide)] dihydrochloride;N,N''-bis(2-ethylhexyl)-3,12-diimino-2,4,11,13-tetraazatetradecanediamidine dihydrochloride;Bisguadine;Compound-904 |
CAS号 | 1715-30-6 |
分子式 | C26H58Cl2N10 |
分子量 | 581.71172 |
EINECS号 | 216-994-6 |
相关类别 | Aliphatics;Amines;Intermediates & Fine Chemicals;Pharmaceuticals;Isotope Labelled Compounds |
Mol文件 | 1715-30-6.mol |
结构式 |
己联双辛胍二盐酸盐 性质
熔点 | 220.6-223.4°C |
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储存条件 | -20°C |
溶解度 | 二甲基亚砜:≥10mg/mL |
形态 | 粉末 |
颜色 | 白色至类白色 |
稳定性 | 吸湿性 |
EPA化学物质信息 | 2,4,11,13-Tetraazatetradecanediimidamide, N,N''-bis(2-ethylhexyl)-3,12-diimino-, dihydrochloride (1715-30-6) |
PTPMT1
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.
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.