Deacylketoconazole
Based on 1 Customer Validation
Deacylketoconazole (N-Deacetylketoconazole; R-39519) is an orally active metabolite of Ketoconazole (HY-B0105). Deacylketoconazole exhibits antifungal and antibacterial activity. Deacylketoconazole is cytotoxic in rats hepatocyte.
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- Pureza : 99.60%
- No. CAS: 67914-61-8
- Fòrmula: C24H26Cl2N4O3
- Peso molecular:489.39
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Actividad biológica
Descripciòn
In Vitro
Deacylketoconazole exhibits antifungal and antibacterial efficacy against Staphylococcus aureus, Plasmodium falciparum, Candida albicans and Candida tropicalis with MIC50s of 25 μM, 0.4 μg/mL, 31 μg/mL and 62 μg/mL, respectively[1][2].
Deacylketoconazole (0-60 μM) exhibits cytotoxicity human liver derived HepaRG cells in a dose-dependent manner with EC50 of 22.8 μM[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepaRG
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Concentration:0-60 μM
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Incubation Time:24 h
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Result:Exhibited cytotoxicity in a dose-dependent manner.
Chemical Information
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No. CAS 67914-61-8
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Appearance Solid
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Peso molecular 489.39
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Fòrmula C24H26Cl2N4O3
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Color White to off-white
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SMILES
ClC1=CC=C(C(Cl)=C1)[C@@]2(OC[C@H](O2)COC3=CC=C(C=C3)N4CCNCC4)CN5C=CN=C5
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Synonyms
N-Deacetylketoconazole; R-39519
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvente y solubilidad
In Vitro:
DMSO : 2.5 mg/mL (5.11 mM; ultrasonic and warming and heat to 60°C; 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)
Pureza y Documentación
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Ficha de datos (273 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)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Pfaller MA, et al., Activity of ketoconazole and its deacyl derivative against Plasmodium falciparum and Candida isolates. Antimicrob Agents Chemother. 1982 Nov;22(5):917-9. [Content Brief]
[3]. Fukami T, et al., Human arylacetamide deacetylase hydrolyzes ketoconazole to trigger hepatocellular toxicity. Biochem Pharmacol. 2016 Sep 15;116:153-61. [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 | 2.0434 mL | 10.2168 mL | 20.4336 mL | 51.0840 mL |
| 5 mM | 0.4087 mL | 2.0434 mL | 4.0867 mL | 10.2168 mL |