1. Anti-infection
  2. Fungal
  3. Ravuconazole

Ravuconazole (Synonyms: BMS-207147; ER-30346)

Cat. No.: HY-14272 Purity: 99.63%
Handling Instructions

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

For research use only. We do not sell to patients.

Ravuconazole Chemical Structure

Ravuconazole Chemical Structure

CAS No. : 182760-06-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 92 In-stock
Estimated Time of Arrival: December 31
2 mg USD 60 In-stock
Estimated Time of Arrival: December 31
5 mg USD 96 In-stock
Estimated Time of Arrival: December 31
10 mg USD 168 In-stock
Estimated Time of Arrival: December 31
25 mg USD 354 In-stock
Estimated Time of Arrival: December 31
50 mg USD 636 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

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

IC50 & Target

Fungal[1]

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].

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].

Clinical Trial
Molecular Weight

437.47

Formula

C₂₂H₁₇F₂N₅OS

CAS No.

182760-06-1

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (114.29 mM)

H2O : < 0.1 mg/mL (insoluble)

*"≥" 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
10 mM 0.2286 mL 1.1429 mL 2.2859 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.71 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1][3]

Mouse[1]
Ravuconazole is prepared in 10% DMSO in 0.5% CMC.C. neoformans No. 3 is grown on an SDA plate at 30°Cfor 48 h, and challenge organisms are prepared in sterile saline. Mice (age, 5 weeks; n 5 10) are infected via the tail vein. Ravuconazole are orally administered, in a volume of 0.2 mL per dose, twice daily for 5 consecutive days starting 1 h after infection. Controls receive 10% DMSO in 0.5% CMC. Ravuconazole are administered at doses of 8 and 32 mg/kg. Mortality is recorded daily for 21 days of infection. Drug efficacy is assessed by determining the delay in mortality.
Rats[3]
The rats are orally infected three times at 48-h intervals with 0.1 mL of a saline suspension containing cells of C. albicansE81022. Ravuconazoleis orally administered, in a volume of 0.5 mL per dose, once daily for 3 consecutive days starting 2 days after the last infection. Control groups receive 10% DMSO in 0.5% CMC. Drugs are administered at doses of 1 and 4 mg/kg. Drug efficacy is assessed 5 days after the last infection by measuring the number of C. albicansorganisms in oral swabs.

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

References
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Keywords:

RavuconazoleBMS-207147ER-30346BMS207147BMS 207147ER30346ER 30346FungalInhibitorinhibitorinhibit

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