Econazole
Based on 6 publication(s) in Google Scholar
Econazole ((±)-Econazol) is an orally active imidazole antifungal agent, as well as a cytochrome P-450 inhibitor and a blocker of calcium and manganese ion uptake. Econazole is active against a variety of fungi and some Gram-positive bacteria, but has no significant activity against Gram-negative bacteria. Econazole can inhibit the synthesis of prostaglandins and can also induce liver damage.
For research use only. We do not sell to patients.
- Purity: 99.93%
- CAS No.: 27220-47-9
- Formula: C18H15Cl3N2O
- Molecular Weight:381.68
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) Econazole
MoreAll Calcium Channel Isoforms
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | IC50 |
11.2 μM
Compound: Econazole
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Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
Inhibition of mouse Ido1 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
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[PMID: 23122865] |
| HEK-293T | IC50 |
7.6 μM
Compound: Econazole
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Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis
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[PMID: 23122865] |
| K562 | CC50 |
54.7 μM
Compound: 3
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Cytotoxicity to reduce chronic myeloid leukemia K 562 cells
Cytotoxicity to reduce chronic myeloid leukemia K 562 cells
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[PMID: 15267229] |
| K562 | CC50 |
70 μM
Compound: 3, econazole
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Cytotoxicity against human K562 cells after assessed as reduction of cell viability 24 hrs by MTT assay
Cytotoxicity against human K562 cells after assessed as reduction of cell viability 24 hrs by MTT assay
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[PMID: 18529046] |
| MDA-MB-231 | IC50 |
17 μM
Compound: 5
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Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction in BAPTA-induced Ca2+ depletion-stimulated SOCE activity preincubated for 15 mins followed by BAPTA addition in presence of extracellular Ca2+ by PBX-ba
Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction in BAPTA-induced Ca2+ depletion-stimulated SOCE activity preincubated for 15 mins followed by BAPTA addition in presence of extracellular Ca2+ by PBX-ba
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[PMID: 27856238] |
| MDA-MB-231 | IC50 |
94 μM
Compound: 5
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Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction of SERCA inhibition-induced ER release preincubated for 15 mins followed by CPA addition by PBX-based FLIPR assay
Inhibition of Orai1-mediated store operated Ca2+ entry in human MDA-MB-231 cells assessed as reduction of SERCA inhibition-induced ER release preincubated for 15 mins followed by CPA addition by PBX-based FLIPR assay
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[PMID: 27856238] |
| U-937 | CC50 |
108 μM
Compound: 3, econazole
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Cytotoxicity against human U937 cells assessed as reduction of cell viability after 24 hrs by MTT assay
Cytotoxicity against human U937 cells assessed as reduction of cell viability after 24 hrs by MTT assay
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[PMID: 18529046] |
| U-937 | CC50 |
60 μM
Compound: 3
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Cytotoxicity to reduce human histolytic lymphoma U937 cells
Cytotoxicity to reduce human histolytic lymphoma U937 cells
|
[PMID: 15267229] |
Econazole (0-30 μM; 40 min) can inhibit the production of PGE2 (HY-101952) induced by multiple stimulants in MC3T3-E1 cells[1].
Econazole (25 μM; 2-3 min) can effectively inhibit the calcium ion influx and manganese ion uptake induced by Thapsigargin (HY-13433) in rat thymic lymphocytes[2].
Econazole (3-30 μM) can inhibit TRPM2-mediated currents in HEK-293 cells expressing hTRPM2[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Econazole (100-300 mg/kg; oral administration; single dose) can induce liver injury in rats[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Wistar strain rats (110-130 g)[5]
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Dosage:100, 200 and 300 mg/kg
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Administration:Oral administration (p.o.); single dose
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Result:Significantly and dose-dependently increased the concentration of serum transaminases (SGOT, SGPT).
Caused different degrees of hepatic tissue changes, including coagulative necrosis, lytic change, cloudy swelling or hydropic degeneration, microvesicular (fatty) degeneration, focal necrosis, inflammatory cell infiltration, and an increase in mitotic figures in the liver.
Chemical Information
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CAS No. 27220-47-9
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Appearance Solid
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Molecular Weight 381.68
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Formula C18H15Cl3N2O
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Color White to off-white
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SMILES
ClC1=CC=C(C(OCC2=CC=C(Cl)C=C2)CN3C=CN=C3)C(Cl)=C1
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Synonyms
(±)-Econazol
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (6)
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Journal Impact Factor
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Most Recent
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Adv Sci (Weinh)
Targeting Transient Receptor Potential Melastatin-2 (TRPM2) Enhances Therapeutic Efficacy of Third Generation EGFR Inhibitors against EGFR Mutant Lung Cancer. [Abstract]2024 Jul 23:e2310126. PMID: 39044361 -
Anal Chem
Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]2025 Jun 3;97(21):11099-11109. PMID: 40401576 -
BMC Cancer
TRPM2 channels mediate ROS-induced actin remodeling and cell migration of prostate cancer cells. [Abstract]2025 May 28;25(1):956. PMID: 40437388 -
Anal Biochem
Inhibitor screening assay for neurexin-LRRTM adhesion protein interaction involved in synaptic maintenance and neurological disorders. [Abstract]2019 Dec 15;587:113463. PMID: 31574254 -
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Oxid Med Cell Longev
Competing Endogenous RNA and Coexpression Network Analysis for Identification of Potential Biomarkers and Therapeutics in association with Metastasis Risk and Progression of Prostate Cancer. [Abstract]2019 Aug 5:2019:8265958. PMID: 31467637
Solvent & Solubility
DMSO : 100 mg/mL (262.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.55 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Köfeler HC, et al. Effect of cytochrome P-450 inhibitors econazole, bifonazole and clotrimazole on prostanoid formation. Br J Pharmacol. 2000 Jul;130(6):1241-6. [Content Brief]
[2]. Mason MJ, et al. Inhibition of Ca2+ transport pathways in thymic lymphocytes by econazole, miconazole, and SKF 96365. Am J Physiol. 1993 Mar;264(3 Pt 1):C654-62. [Content Brief]
[3]. Hill K, et al. Inhibition of TRPM2 channels by the antifungal agents clotrimazole and econazole. Naunyn Schmiedebergs Arch Pharmacol. 2004 Oct;370(4):227-37. [Content Brief]
[4]. Heel RC, et al. Econazole: a review of its antifungal activity and therapeutic efficacy. Drugs. 1978 Sep;16(3):177-201. [Content Brief]
[5]. Liu CF, et al. Antioxidative natural product protect against econazole-induced liver injuries. Toxicology. 2004 Mar 1;196(1-2):87-93. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6200 mL | 13.1000 mL | 26.2000 mL | 65.4999 mL |
| 5 mM | 0.5240 mL | 2.6200 mL | 5.2400 mL | 13.1000 mL | |
| 10 mM | 0.2620 mL | 1.3100 mL | 2.6200 mL | 6.5500 mL | |
| 15 mM | 0.1747 mL | 0.8733 mL | 1.7467 mL | 4.3667 mL | |
| 20 mM | 0.1310 mL | 0.6550 mL | 1.3100 mL | 3.2750 mL | |
| 25 mM | 0.1048 mL | 0.5240 mL | 1.0480 mL | 2.6200 mL | |
| 30 mM | 0.0873 mL | 0.4367 mL | 0.8733 mL | 2.1833 mL | |
| 40 mM | 0.0655 mL | 0.3275 mL | 0.6550 mL | 1.6375 mL | |
| 50 mM | 0.0524 mL | 0.2620 mL | 0.5240 mL | 1.3100 mL | |
| 60 mM | 0.0437 mL | 0.2183 mL | 0.4367 mL | 1.0917 mL | |
| 80 mM | 0.0327 mL | 0.1637 mL | 0.3275 mL | 0.8187 mL | |
| 100 mM | 0.0262 mL | 0.1310 mL | 0.2620 mL | 0.6550 mL |