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130773-02-3

中文名称 盐酸奈替康唑
英文名称 Neticonazole Hydrochloride
CAS 130773-02-3
分子式 C17H23ClN2OS
分子量 338.9
MOL 文件 130773-02-3.mol
更新日期 2024/07/08 16:38:18
130773-02-3 结构式 130773-02-3 结构式

基本信息

中文别名
盐酸萘康唑
盐酸奈康唑
盐酸奈替康唑
(E)-1-(2-(甲硫基)-1-(2-(戊氧基)苯基)乙烯基)-1H-咪唑盐酸盐
英文别名
SS-717
Atolant
Neticonazole hydrochloride
1-[2-methylsulfanyl-1-(2-pentoxyphenyl)ethenyl]imidazole hydrochloride
1-[(E)-2-methylsulfanyl-1-(2-pentoxyphenyl)ethenyl]imidazole,hydrochloride
(E)-1-(2-(Methylthio)-1-(2-(pentyloxy)phenyl)vinyl)-1H-imidazole hydrochloride
long-acting,colorectal,Neticonazole,antifungal,Neticonazole Hydrochloride,Imidazole,anti-cancer,nSMase2,Fungal,secretion,Inhibitor,p-ERK,anti-infection,inhibit,exosome
所属类别
有机原料:羧酸类化合物及衍生物

物理化学性质

熔点145-147°
储存条件-20°C储存
溶解度DMSO: 250 mg/mL (737.68 mM)
形态Solid
颜色White to off-white

制备方法

方法1
1-碘戊烷

628-17-1

(E)-1-[2-甲巯基-1-[2-羟基苯基]乙烯基]-1H-咪唑

138206-46-9

盐酸奈替康唑

130773-02-3

以1-碘戊烷和(E)-1-[2-甲巯基-1-[2-羟基苯基]乙烯基]-1H-咪唑为原料,合成(E)-1-(2-(甲硫基)-1-(2-(戊氧基)苯基)乙烯基)-1H-咪唑盐酸盐的一般步骤如下:将式(4)化合物(E)-1-[1-(2-羟基苯基)-2-(甲硫基)乙烯基]-1H-咪唑(15.1 g,65 mmol)、氢氧化钾(5.1 g,91 mmol)和1-碘戊烷(15.55 g,78 mmol)溶于75 mL DMF中,室温搅拌反应3.5小时。反应完成后,将反应液倒入375 mL水中,用乙酸乙酯萃取,有机相依次用水和饱和食盐水洗涤。减压浓缩有机相,得到油状物。将该油状物溶于氯化氢气体饱和的乙酸乙酯中,搅拌10小时。反应液中析出白色固体,经过滤,用乙腈洗涤,真空干燥,得到16.4 g白色固体产物。产率:73.2%。HPLC纯度(面积归一化法):99.61%,单一杂质含量<0.1%。

参考文献:

[1] Patent: CN107556245, 2018, A. Location in patent: Paragraph 0045; 0046

盐酸奈替康唑价格(试剂级)
报价日期产品编号产品名称CAS号包装价格
2025/05/22HY-128365盐酸奈替康唑
Neticonazole hydrochloride
130773-02-325mg650元
2025/05/22HY-128365盐酸奈替康唑
Neticonazole hydrochloride
130773-02-310 mM * 1 mLin DMSO715元
2025/05/22HY-128365盐酸奈替康唑
Neticonazole hydrochloride
130773-02-350mg950元

常见问题列表

生物活性
Neticonazole是咪唑类抗真菌剂,用于治疗皮肤真菌感染。
靶点

Fungal

体外研究

Neticonazole (10 µM; 48 hours; C4-2B cells) treatment decreases the levels of both Alix and Rab27a, and significantly decreases nSMase2 levels. Neticonazole causes a significant inhibition in p-ERK levels.
Neticonazole (0-10 µM) exhibits a potent and dose-dependent inhibition of exosome release from C4-2B cells.
Neticonazole hydrochloride is also an orally active exosome biogenesis and secretion inhibitor.

Western Blot Analysis

Cell Line: C4-2B cells
Concentration: 10 µM
Incubation Time: 48 hours
Result: Decreased the levels of both Alix and Rab27a, and significantly decreased nSMase2 levels.
体内研究

Neticonazole (1-100 ng/kg; oral gavage; daily; for 15 days; male C57BL/6 mice) treatment significantly improves the survival of intestinal dysbacteriosis (IDB) mice with colorectal cancer (CRC) xenograft tumors, likely through increasing apoptosis of CRC xenograft tumor cells.

Animal Model: Male C57BL/6 mice (8 weeks old) given ampicillin, neomycin, metronidazole and vancomycin, and injected with SW480 cells
Dosage: 1 ng/kg, 10 ng/kg and 100 ng/kg
Administration: Oral gavage; daily; for 15 days
Result: Significantly improved the survival of IDB mice with CRC xenograft tumors.
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