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Oteseconazole

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Catalog No. T16412Cas No. 1340593-59-0
Alias VT-1161

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).

Oteseconazole

Oteseconazole

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Purity: 99.95%
Catalog No. T16412Alias VT-1161Cas No. 1340593-59-0
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).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$93In StockIn Stock
2 mg$137In StockIn Stock
5 mg$228In StockIn Stock
10 mg$372In StockIn Stock
25 mg$569In StockIn Stock
50 mg$787In StockIn Stock
100 mg$1,070-In Stock
200 mg$1,430-In Stock
1 mL x 10 mM (in DMSO)$268In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.95%
Appearance:Solid
Color:White
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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
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
CYP2C9:99 μM, CYP2C19:72 μM
SynonymsVT-1161
Chemical Properties
Molecular Weight527.39
FormulaC23H16F7N5O2
Cas No.1340593-59-0
SmilesO[C@@](Cn1cnnn1)(c1ccc(F)cc1F)C(F)(F)c1ccc(cn1)-c1ccc(OCC(F)(F)F)cc1
Relative Density.1.47 g/cm3 (Predicted)
Storage & Solubility Information
Storagestore 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
1mg5mg10mg50mg
1 mM1.8961 mL9.4806 mL18.9613 mL94.8065 mL
5 mM0.3792 mL1.8961 mL3.7923 mL18.9613 mL
10 mM0.1896 mL0.9481 mL1.8961 mL9.4806 mL
20 mM0.0948 mL0.4740 mL0.9481 mL4.7403 mL
50 mM0.0379 mL0.1896 mL0.3792 mL1.8961 mL
100 mM0.0190 mL0.0948 mL0.1896 mL0.9481 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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