Size | Price | Stock | Qty |
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500mg |
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1g |
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5g |
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Purity: ≥98%
Econazole Nitrate (formerly also known as NSC-243115; SQ-13050; Spectazole) is a potent calcium channel blocker/CCB used as an imidazole-based antifungal medicine against infections caused by fungus. It was approved in 1974 for treating a variety of fungal skin infections such as athlete's foot, jock itch, and ringworm. 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.
ln Vitro |
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.
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ln Vivo |
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Animal Protocol |
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References |
Molecular Formula |
C18H15CL3N2O.HNO3
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Molecular Weight |
444.7
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Elemental Analysis |
C, 48.62; H, 3.63; Cl, 23.92; N, 9.45; O, 14.39
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CAS # |
24169-02-6
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Related CAS # |
Econazole;27220-47-9
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Appearance |
White to off-white solid powder.
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SMILES |
C1=CC(=CC=C1COC(CN2C=CN=C2)C3=C(C=C(C=C3)Cl)Cl)Cl.[N+](=O)(O)[O-]
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InChi Key |
DDXORDQKGIZAME-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C18H15Cl3N2O.HNO3/c19-14-3-1-13(2-4-14)11-24-18(10-23-8-7-22-12-23)16-6-5-15(20)9-17(16)21;2-1(3)4/h1-9,12,18H,10-11H2;(H,2,3,4)
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Chemical Name |
1-[2-[(4-chlorophenyl)methoxy]-2-(2,4-dichlorophenyl)ethyl]imidazole;nitric acid
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Synonyms |
Econazole Nitrate; R 14,827; R 14827; Spectazole; SQ 13050; SQ13050; SQ-13050; Ecoza; epi-Pevaryl; Gyno-pevaryl; Ifenec.
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
DMSO : 50~89 mg/mL ( 112.44~200.13 mM )
H2O : 0.67 mg/mL (1.51 mM) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.62 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 2.5 mg/mL (5.62 mM) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2487 mL | 11.2435 mL | 22.4871 mL | |
5 mM | 0.4497 mL | 2.2487 mL | 4.4974 mL | |
10 mM | 0.2249 mL | 1.1244 mL | 2.2487 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT01358240 | Completed | Drug: Econazole Nitrate Foam 1% Drug: Vehicle Foam |
Tinea Pedis Athlete's Foot |
AmDerma | June 2011 | Phase 3 |
NCT01353976 | Completed Has Results | Drug: Econazole Nitrate Foam 1% Other: Vehicle Foam |
Tinea Pedis Athlete's Foot |
AmDerma | May 2011 | Phase 3 |
NCT01696799 | Completed | Drug: Econazole Nitrate Drug: placebo |
Interdigital Tinea Pedis | AmDerma | September 2011 | Phase 2 |
NCT03129321 | Completed Has Results | Drug: Econazole Nitrate Cream, 1% Drug: Placebo |
Tinea Pedis | Mylan Inc. | March 15, 2016 | Phase 3 |