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Neticonazole

Names

[ CAS No. ]:
130726-68-0

[ Name ]:
Neticonazole

[Synonym ]:
Neticonazol
Neticonazole HCl
(E)-1-<2-(Methylthio)-1-<2-(pentyloxy)phenyl>ethenyl>-1H-imidazole
Neticonazole
Neticonazole [INN]
Neticonazolum
UNII-KVL61ZF9UO

Biological Activity

[Description]:

Neticonazole is an imidazole derivative and a potent and long-acting antifungal agent. Neticonazole is also an orally active exosome biogenesis and secretion inhibitor. Neticonazole has anti-infection and anti-cancer effects[1][2][3].

[Related Catalog]:

Research Areas >> Cancer
Research Areas >> Infection
Signaling Pathways >> Anti-infection >> Fungal

[Target]

Fungal [1] Exosome secretion[2]


[In Vitro]

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[2]. Neticonazole (0-10 µM) exhibits a potent and dose-dependent inhibition of exosome release from C4-2B cells[2]. Western Blot Analysis[2] 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.

[In Vivo]

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[3]. Animal Model: Male C57BL/6 mice (8 weeks old) given ampicillin, neomycin, metronidazole and vancomycin, and injected with SW480 cells[3] 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.

[References]

[1]. Tsuboi R, et al. Hyperkeratotic chronic tinea pedis treated with neticonazole cream. Neticonazole Study Group. Int J Dermatol. 1996 May;35(5):371-3.

[2]. Datta A, et al. High-throughput screening identified selective inhibitors of exosome biogenesis and secretion: A drug repurposing strategy for advanced cancer. Sci Rep. 2018 May 25;8(1):8161.

[3]. Gu L, et al. The exosome secretion inhibitor neticonazole suppresses intestinal dysbacteriosis-induced tumorigenesis of colorectal cancer. Invest New Drugs. 2020 Apr;38(2):221-228.

Chemical & Physical Properties

[ Density]:
1.06g/cm3

[ Boiling Point ]:
464ºC at 760mmHg

[ Molecular Formula ]:
C17H22N2OS

[ Molecular Weight ]:
302.43400

[ Flash Point ]:
234.4ºC

[ Exact Mass ]:
302.14500

[ PSA ]:
52.35000

[ LogP ]:
4.66180

[ Vapour Pressure ]:
8.66E-09mmHg at 25°C

[ Index of Refraction ]:
1.558

Related Compounds