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Econazole

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Chemical Structure| 27220-47-9 同义名 : (±)-Econazol
CAS号 : 27220-47-9
货号 : A103065
分子式 : C18H15Cl3N2O
纯度 : 99%+
分子量 : 381.683
MDL号 : MFCD00800993
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(275.1 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Calcium Channel
描述 Econazole is an antifungal agent and a new PI3K (phosphatidylinositol-3-kinase) inhibitor and a potential drug that can be used in lung cancer treatment alone or in combination with cisplatin. Econazole significantly suppressed A549 tumor growth in nude mice[3]. Guinea-pigs infected with T. mentagrophytes, M. canis or C. albicans and treated topically or orally with econazole, were cured. In each of these tests the activity of econazole was compared with that of different reference drugs. Vaginal candidiasis in rats was cured after oral administration of econazole. Toxicity and teratogenicity studies in different laboratory animals indicate that econazole is well tolerated[4]. The econazole-bound TRPV5 (transient receptor potential vanilloid 5) structure adopts a closed conformation with a distinct lower gate that occludes Ca2+ permeation through the channel[5]. Moreover, econazole nitrate loaded transethosomes are effective to deliver econazole nitrate transdermally in a controlled fashion for effective elimination of cutaneous candidiasis[6].
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00385502 Onychomycosis Phase 2 Unknown June 2008 United States, Arizona ... 展开 >> Tucson, Arizona, United States, 85741 United States, New York New York, New York, United States, 10032 United States, Oregon Portland, Oregon, United States, 97210 收起 <<
NCT03129321 Tinea Pedis Phase 3 Completed - -
NCT03129321 - Completed - -
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.62mL

0.52mL

0.26mL

13.10mL

2.62mL

1.31mL

26.20mL

5.24mL

2.62mL
参考文献

[1]Ge S, Lin Y, et al. Percutaneous delivery of econazole using microemulsion as vehicle: formulation, evaluation and vesicle-skin interaction. Int J Pharm. 2014 Apr 25;465(1-2):120-31.

[2]Rubio B, Gonzalez R, Karoussos K. Vulvo-vaginal candidosis and its treatment with the new fungicidal substance econazole. J Int Med Res. 1980;8(6):436-8.

[3]Dong C, Yang R, Li H, et al. Econazole nitrate inhibits PI3K activity and promotes apoptosis in lung cancer cells. Sci Rep. 2017;7(1):17987. Published 2017 Dec 21

[4]Thienpont D, Van Cutsem J, Van Nueten JM, Niemegeers CJ, Marsboom R. Bilogical and toxicological properties of econazole, a broad-spectrum antimycotic. Arzneimittelforschung. 1975;25 (2):224 ‐230

[5]Hughes TET, Lodowski DT, Huynh KW, et al. Structural basis of TRPV5 channel inhibition by econazole revealed by cryo-EM. Nat Struct Mol Biol. 2018;25(1):53‐60

[6]Verma S, Utreja P. Transethosomes of Econazole Nitrate for Transdermal Delivery: Development, In-vitro Characterization, and Ex-vivo Assessment. Pharm Nanotechnol. 2018;6(3):171‐179