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> Ravuconazole [182760-06-1]

Ravuconazole [182760-06-1]

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Référence HY-14272-10mg

Conditionnement : 10mg

Marque : MedChemExpress


Description

Ravuconazole (BMS-207147;ER-30346) is an orally available triazole antifungle agent that potently inhibits a wide range of fungi.

IC50 & Target

Fungal[1]
Cellular Effect
Cell Line Type Value Description References
CHO IC50
10.37 μM
Compound: 5
Inhibition of human ERG expressed in CHO cells by whole-cell patch clamp assay
Inhibition of human ERG expressed in CHO cells by whole-cell patch clamp assay
[PMID: 24564525]
Caco-2 CC50
12.75 μM
Compound: RAVUCONAZOLE
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
10.21203/rs.3.rs-23951/v1
Caco-2 IC50
2.76 μM
Compound: RAVUCONAZOLE
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
10.21203/rs.3.rs-23951/v1
In Vitro

Ravuconazole shows a broad spectrum of activity against a wide range of fungi covering Candida spp., Trichosporon beigelii, C. neoformans and A. fumigatus. The MIC90 ranges from 0.025 to 0.39 mg/mL.Ravuconazoleshows relatively higher levels of activity against three strains of Candida krusei, with MICs ranging from 0.05 to 0.39 mg/mL.Ravuconazoleshows good activity against T. mentagrophytes, T. rubrum, M. gypseum and M. caniswith MICs ranging from 0.05 to 0.39 mg/mL[1]. Ravuconazoleis about two- to four fold more potent than itraconazole and about 40-fold more active than fluconazole against yeasts. Ravuconazoleand itraconazoleare inhibitory to most aspergilli, and against half of the isolates, the activity iscidal. Ravuconazoleand itraconazoleare active, though not cidal, against most hyaline Hyphomycetes, dermatophytes, and the dematiaceous fungi and inactive against Sporothrix schenckii and zygomycetes[2].

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

Ravuconazole Related Antibodies
In Vivo

The maximum concentration of ravuconazole in plasma and the area under the concentration-time curve for ravuconazoleshow good linearity over a range of doses from 2 to 40 mg/kg of body weight. Ravuconazole at a dose of 2.5 mg/kg delays mortality significantly compared with the control treatment.Ravuconazole also shows a substantial therapeutic effect against systemic cryptococcosis[1]. Ravuconazole reduces the numbers of CFU in the lungs significantly compared with the numbers of CFU in the lungs of the controls. In an experimental model of oral candidiasis in rats, ravuconazole reduces the numbers of CFU in oral swabs significantly compared with the numbers of CFU in oral swabs from the controls and is more effective than itraconazole and as effective as fluconazole.[3].

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

437.47

Formule

C22H17F2N5OS
CAS No.
Appearance

Solid

Color

White to yellow

SMILES

FC1=CC(F)=CC=C1[C@](CN2C=NC=N2)(O)[C@@H](C)C3=NC(C4=CC=C(C#N)C=C4)=CS3
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvant et solubilité
In Vitro: 

DMSO : ≥ 50 mg/mL (114.29 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2859 mL 11.4294 mL 22.8587 mL
5 mM 0.4572 mL 2.2859 mL 4.5717 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.71 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.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (5.71 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.
Pureté et documentation
Références