Oteseconazole [1340593-59-0]
Référence T16412-10mg
Conditionnement : 10mg
Marque : TargetMol
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Oteseconazole
(Synonyms: VT-1161) Copy Product Info
Oteseconazole (VT-1161) is an orally active anti-fungal agent. Oteseconazole displays no obvious effect on human CYP51. It also potently binds to and inhibits Candida albicans CYP51 (Kd, <39 nM).
Cas No. 1340593-59-0
For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:99.95%
Appearance:Solid
Color:White
COA LCMS HNMR
Product Introduction
Oteseconazole AI Summary
Oteseconazole exhibits potent antifungal activity against Candida albicans, Trichophyton rubrum, and Cryptococcus neoformans with MIC50 values of <= 0.001 ug/mL, 0.001 ug/mL, and 625.0 nM respectively. It demonstrates a high selectivity index (>65000.0) for inhibiting CYP3A4 in human hepatocytes and has a strong binding affinity (Kd <= 39.0 nM) for Candida albicans CYP51, with a selectivity ratio (>2200.0) for yeast CYP51 over human CYP51. The compound shows considerable metabolic stability (>99.0 %) in human liver microsomes after 2 hours and has a long half-life (>24.0 hr) after oral administration. In vivo, Oteseconazole effectively reduces kidney fungal burden by 99.0% in a mouse candidiasis model and shows 86.0% mycological efficacy in a guinea pig dermatophytosis model at an oral dose of 10 mg/kg. While Oteseconazole has low haemolytic activity (HC10 > 20.0 uM) and non-cytotoxicity to HEK293 cells (CC50 > 20000.0 nM), it does not exhibit significant antibacterial activity against several tested bacterial strains at MIC values above 20000.0 nM..
Note: Summary generated by AI. Data source: ChEMBL 
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | Oteseconazole (VT-1161) is an orally active anti-fungal agent. Oteseconazole displays no obvious effect on human CYP51. It also potently binds to and inhibits Candida albicans CYP51 (Kd, <39 nM). |
| Targets & IC50 | CYP2C19:72 μM, CYP2C9:99 μM |
| Synonyms | VT-1161 |
| Molecular Weight | 527.39 |
| Formula | C23H16F7N5O2 |
| Cas No. | 1340593-59-0 |
| Smiles | O[C@@](Cn1cnnn1)(c1ccc(F)cc1F)C(F)(F)c1ccc(cn1)-c1ccc(OCC(F)(F)F)cc1 |
| Relative Density. | 1.47 g/cm3 (Predicted) |
| Storage | Store at low temperature Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 250 mg/mL (474.03 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 5 mg/mL (9.48 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density. | ||||||||||||||||||||||||||||||||||||