For research use only.
Catalog No.S2535 Synonyms: NSC 243115
CAS No. 24169-02-6
Econazole Nitrate (NSC 243115) is a Ca2+ channel blocker, used as an antifungal medicine that fights infections caused by fungus.
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|Description||Econazole Nitrate (NSC 243115) is a Ca2+ channel blocker, used as an antifungal medicine that fights infections caused by fungus.|
Econazole nitrate is an effective inducer of micronuclei over a narrow dose range in cell lines V79, XEM2 and XEMd-MZ (expresses CYP1A2).  Econazole nitrate inhibits the proliferation of MCF-7 cells in a time- and dose-dependent manner by MTT method and colony forming assay. Econazole nitrate results in typical characteristics of apoptosis including the morphological changes and DNA fragmentation in MCF-7 cells. Econazole nitrate results in the decrease expression of procaspase-3, procaspase-9 and bcl-2.  Econazole inhibits ADP-ribose-activated currents in HEK-293 cells expressing recombinant human TRPM2 (hTRPM2). Econazole produces an essentially complete inhibition of the TRPM2-mediated current.  Econazole (25-50 mM) partially inhibits capacitative Ca2+ entry induced by cyclopiazonic acid, another endoplasmic reticulum Ca2+ pump inhibitor. Econazole induces Ca2+ influx via two separate pathways: one is sensitive to La3+, the other is not.  Econazole reversibly inhibits (Bu)(2)cAMP-stimulated progesterone production in a dose- and time-dependent manner in MA-10 cells without affecting total protein synthesis or P450(scc) and 3beta-hydroxysteroid dehydrogenase (3beta-HSD) enzyme expression or activity.  Econazole is a store-operated Ca2+ channel antagonist which induces cytotoxic cell death of leukemia. Econazole (5-20 mM) arrests human colon cancer cells at the G0/G1 phase of the cell cycle. Econazole induces COLO 205 cells apoptosis evidenced by ladder formation in DNA fragmentation assay and sub-G1 peak. 
-  Ferrer-Villada T, et al. Eur J Pharmacol,?006, 531(1-3), 1-8.
-  Sun J, et al. Iran J Pharm Res,?014, 13(4), 1327-1334.
-  Hill K, et al. Naunyn Schmiedebergs Arch Pharmacol,?004, 370(4), 227-237.
|In vitro||DMSO||89 mg/mL (200.13 mM)|
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|% DMSO % % Tween 80 % ddH2O|
Working concentration： mg/ml；
Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01696799||Completed||Drug: Econazole Nitrate|Drug: placebo||Interdigital Tinea Pedis||AmDerma|AmDerma Pharmaceuticals LLC||September 2011||Phase 2|
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