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> Quilseconazole [1340593-70-5]

Quilseconazole [1340593-70-5]

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Referência HY-109040-10mg

Tamanho : 10mg

Marca : MedChemExpress


Description

Quilseconazole (VT-1129) is an orally active, highly selective fungal cytochrome P450 enzyme Cyp51 inhibitor that can cross the blood-brain barrier. Quilseconazole prevents the synthesis of ergosterol, an important component of the fungal cell membrane, by inhibiting Cyp51. Quilseconazole has minimal effects on human CYP enzymes. Quilseconazole has antifungal activity and can be used in the study of cryptococcal meningitis and other diseases[1][2][3].

IC50 & Target

CYP51

 

Cellular Effect
Cell Line Type Value Description References
Hepatocyte IC50
79 μM
Compound: 7c
Inhibition of CYP3A4 in human hepatocytes using testosterone as substrate by HPLC/MS/MS method
Inhibition of CYP3A4 in human hepatocytes using testosterone as substrate by HPLC/MS/MS method
[PMID: 24948565]
In Vitro

Quilseconazole exhibits potent antifungal activity against Cryptococcus neoformans and Cryptococcus gattii[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Quilseconazole Related Antibodies

Solvant et solubilité
In Vitro: 

DMSO : 100 mg/mL (194.79 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9479 mL 9.7396 mL 19.4791 mL
5 mM 0.3896 mL 1.9479 mL 3.8958 mL
View the 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.

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (4.87 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (4.87 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Pureté et documentation
Références