Oxiconazole nitrate
Based on 2 publication(s) in Google Scholar
Oxiconazole (Ro 13-8996) nitrate is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole nitrate is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole nitrate exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest.
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- Purity: 98.0%
- CAS No.: 64211-46-7
- 화학식: C18H14Cl4N4O4
- 분자량:492.14
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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Publications Citing Use of MedChemExpress (MCE) Oxiconazole nitrate
MoreAll Antibiotic Isoforms
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Biological Activity
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CYP3A4 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | CC50 |
26.36 μM
Compound: OXICONAZOLE
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Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay
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10.21203/rs.3.rs-23951/v1 |
| Caco-2 | IC50 |
20.82 μM
Compound: OXICONAZOLE
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Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging
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10.21203/rs.3.rs-23951/v1 |
Oxiconazole (24 h; 0-40 μM) inhibits CRC cell growth[3].
Oxiconazole has antifungal activity against Candida, Aspergillus and Trichophyton[1].
Antifungal Activities of Oxiconazole[1].
| Candidaalbicans | Candidaglabrata | Candidaparapsilosis | Aspergillusfumigatus | Aspergillusflavus | Trichophytonmentagrophytes | Trichophytonrubrum | |
| Oxiconazole | 0.03 μg/mL | 0.01 μg/mL | 0.008 μg/mL | 2 μg/mL | 2 μg/mL | 2 μg/mL | 2 μg/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116, SW480, RKO, DLD-1, SW620, LoVo and NCM460
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Concentration:0-40 μM
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Incubation Time:24 h
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Result:Exhibited inhibitory activity against HCT116, SW480, RKO, DLD-1, SW620, LoVo and NCM460 with IC50s of 25.86 μM, 27.34 μM, 21.01 μM, 25.56 μM, 21.75 μM, 24.87 μM and 126.4 μM.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice (injected subcutaneously with HCT116 cells (1×107/mouse)[3]
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Dosage:50 mg/kg/day
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Administration:IP; for 12 days
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Result:Significantly restrained CRC cell growth and showed no obvious side effects.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 64211-46-7
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Appearance Solid
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분자량 492.14
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화학식 C18H14Cl4N4O4
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Color White to off-white
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SMILES
[O-][N+](O)=O.ClC1=CC=C(/C(CN2C=CN=C2)=N/OCC3=CC=C(Cl)C=C3Cl)C(Cl)=C1
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Synonyms
Ro 13-8996
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (2)
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Journal Impact Factor
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Most Recent
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Int J Biol Sci
2022 May 21;18(9):3747-3761. PMID: 35813474 -
용액&용해도
DMSO : ≥ 100 mg/mL (203.19 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). 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 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.08 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 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.08 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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
순도&문서
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Data Sheet (292 KB)
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SDS (608 KB)
- English - EN (608 KB)
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Handling Instructions (2659 KB)
References
[1]. Rossello A, et al. Synthesis, antifungal activity, and molecular modeling studies of new inverted oxime ethers of oxiconazole. J Med Chem. 2002 Oct 24;45(22):4903-12. [Content Brief]
[2]. Svecova L, et al. Azole antimycotics differentially affect rifampicin-induced pregnane X receptor-mediated CYP3A4 gene expression. Drug Metab Dispos. 2008 Feb;36(2):339-48. [Content Brief]
[3]. Shi J, et al. Repurposing Oxiconazole against Colorectal Cancer via PRDX2-mediated Autophagy Arrest. Int J Biol Sci. 2022 May 21;18(9):3747-3761. [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 (sealed storage, away from moisture). 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 | 2.0319 mL | 10.1597 mL | 20.3194 mL | 50.7986 mL |
| 5 mM | 0.4064 mL | 2.0319 mL | 4.0639 mL | 10.1597 mL | |
| 10 mM | 0.2032 mL | 1.0160 mL | 2.0319 mL | 5.0799 mL | |
| 15 mM | 0.1355 mL | 0.6773 mL | 1.3546 mL | 3.3866 mL | |
| 20 mM | 0.1016 mL | 0.5080 mL | 1.0160 mL | 2.5399 mL | |
| 25 mM | 0.0813 mL | 0.4064 mL | 0.8128 mL | 2.0319 mL | |
| 30 mM | 0.0677 mL | 0.3387 mL | 0.6773 mL | 1.6933 mL | |
| 40 mM | 0.0508 mL | 0.2540 mL | 0.5080 mL | 1.2700 mL | |
| 50 mM | 0.0406 mL | 0.2032 mL | 0.4064 mL | 1.0160 mL | |
| 60 mM | 0.0339 mL | 0.1693 mL | 0.3387 mL | 0.8466 mL | |
| 80 mM | 0.0254 mL | 0.1270 mL | 0.2540 mL | 0.6350 mL | |
| 100 mM | 0.0203 mL | 0.1016 mL | 0.2032 mL | 0.5080 mL |
Oxiconazole nitrate Related Classifications
HY-B1324 Related Classifications
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