130773-02-3
130773-02-3 結(jié)構(gòu)式
基本信息
鹽酸奈康唑
鹽酸奈替康唑
(E)-1-(2-(甲硫基)-1-(2-(戊氧基)苯基)乙烯基)-1H-咪唑鹽酸鹽
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
物理化學(xué)性質(zhì)
制備方法
628-17-1
![(E)-1-[2-甲巰基-1-[2-羥基苯基]乙烯基]-1H-咪唑](/CAS/20180629/GIF/138206-46-9.gif)
138206-46-9
130773-02-3
以1-碘戊烷和(E)-1-[2-甲巰基-1-[2-羥基苯基]乙烯基]-1H-咪唑?yàn)樵?，合?E)-1-(2-(甲硫基)-1-(2-(戊氧基)苯基)乙烯基)-1H-咪唑鹽酸鹽的一般步驟如下：將式（4）化合物(E)-1-[1-(2-羥基苯基)-2-(甲硫基)乙烯基]-1H-咪唑（15.1 g，65 mmol）、氫氧化鉀（5.1 g，91 mmol）和1-碘戊烷（15.55 g，78 mmol）溶于75 mL DMF中，室溫?cái)嚢璺磻?yīng)3.5小時(shí)。反應(yīng)完成后，將反應(yīng)液倒入375 mL水中，用乙酸乙酯萃取，有機(jī)相依次用水和飽和食鹽水洗滌。減壓濃縮有機(jī)相，得到油狀物。將該油狀物溶于氯化氫氣體飽和的乙酸乙酯中，攪拌10小時(shí)。反應(yīng)液中析出白色固體，經(jīng)過濾，用乙腈洗滌，真空干燥，得到16.4 g白色固體產(chǎn)物。產(chǎn)率：73.2%。HPLC純度（面積歸一化法）：99.61%，單一雜質(zhì)含量<0.1%。
參考文獻(xiàn)：
[1] Patent: CN107556245, 2018, A. Location in patent: Paragraph 0045; 0046
| 報(bào)價(jià)日期 | 產(chǎn)品編號(hào) | 產(chǎn)品名稱 | CAS號(hào) | 包裝 | 價(jià)格 |
| 2026/06/05 | HY-128365 | 鹽酸奈替康唑 Neticonazole hydrochloride | 130773-02-3 | 25mg | 650元 |
| 2026/06/05 | HY-128365 | 鹽酸奈替康唑 Neticonazole hydrochloride | 130773-02-3 | 10 mM * 1 mLin DMSO | 715元 |
| 2026/06/05 | HY-128365 | 鹽酸奈替康唑 Neticonazole hydrochloride | 130773-02-3 | 50mg | 950元 |
常見問題列表
Fungal
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. |
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. |