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product name Econazole nitrate


Description: Econazole Nitrate (also known as 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. 

References: Eur J Pharmacol. 2006 Feb 15;531(1-3):1-8; Iran J Pharm Res. 2014 Fall;13(4):1327-34.



Molecular Weight (MW)

444.7 
Formula

C18H15Cl3N2O.HNO3 
CAS No.

24169-02-6 
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 89 mg/mL (200.1 mM) 
Water: <1 mg/mL
Ethanol: 5 mg/mL (11.2 mM) 
Solubility (In vivo)

 
Synonyms

NSC 243115 

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/19403638

In Vitro

In vitro activity: 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.


Kinase Assay:


Cell Assay

In Vivo  
Animal model  
Formulation & Dosage  
References Eur J Pharmacol. 2006 Feb 15;531(1-3):1-8; Iran J Pharm Res. 2014 Fall;13(4):1327-34. 

CHIR-99021

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Author: Sodium channel

Share this post on:

product name Econazole nitrate


Description: Econazole Nitrate (also known as 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. 

References: Eur J Pharmacol. 2006 Feb 15;531(1-3):1-8; Iran J Pharm Res. 2014 Fall;13(4):1327-34.



Molecular Weight (MW)

444.7 
Formula

C18H15Cl3N2O.HNO3 
CAS No.

24169-02-6 
Storage

-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)

DMSO: 89 mg/mL (200.1 mM) 
Water: <1 mg/mL
Ethanol: 5 mg/mL (11.2 mM) 
Solubility (In vivo)

 
Synonyms

NSC 243115 

other peoduct :References PubMed ID::http://www.ncbi.nlm.nih.gov/pubmed/19403638

In Vitro

In vitro activity: 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.


Kinase Assay:


Cell Assay

In Vivo  
Animal model  
Formulation & Dosage  
References Eur J Pharmacol. 2006 Feb 15;531(1-3):1-8; Iran J Pharm Res. 2014 Fall;13(4):1327-34. 

CHIR-99021

Share this post on:

Author: Sodium channel