Voriconazole (UK-109496) - Moligand™, 10mM in DMSO , Cytochrome P450 51 inhibitor, CAS No.137234-62-9, Cytochrome P450 51 inhibitor

CAS: 137234-62-9 Cat. No.: V409051 Molecular Weight: 349.31 EC Number: 629-701-5 PubChem CID: 71616

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

(2R,3S)-2-(2,4-difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1H-1,2,4-triazol-1-yl)butan-2-ol

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Voriconazole (UK-109496) is a new triazole derivative similar to fluconazole and itraconazole that acts by inhibiting fungalcytochrome P-450-dependent,14-alpha-sterol demethylase-mediated synthesis of ergosterol.
In vitro

Voriconazole is active against certain opportunistic filamentous and dimorphic fungi (molds) and yeasts. Voriconazole in vitro activities are higher than or similar to those of itraconazole and amphotericin B for most of the molds tested, with the exceptions of R. arrhizus and S. schenckii. Voriconazole inhibits 95% of isolates at ≤1 μg/ml against 448 recent clinical mold isolates.

In vivo

Voriconazole is significantly more effective than itraconazole in reducing Aspergillus content in the lungs of immunocompromised guinea pig with pulmonary aspergillosis. Voriconazole also has been shown to be effective in guinea pigs with experimental pulmonary or intracranial infections caused by C. neoformans. Voriconazole (5 mg/kg/day, i.p.) combined with Amphotericin B (1.25 mg/kg/day, i.p.) significantly reduces the colony counts in the tissues of selected Guinea pigs compared with those in the tissues of the controls. Voriconazole (5 mg/kg/day, i.p.) combined with Amphotericin B (1.25 mg/kg/day, i.p.) also results in reductions in colony counts in tissues compared with those in the tissues of Guinea pigs treated with caspofungin acetate (the difference is not statistically significant) and improves the survival times but does not sterilize tissues. Voriconazole (5 mg/kg/day, i.p.) combined with caspofungin acetate (CAS) at either dose reduces colony counts in tissues 1,000-fold over those for the controls and are the only regimens that significantly reduces the numbers of positive cultures.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

(2R, 3S)-2-(2, 4-difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1H-1, 2, 4-triazol-1-yl)butan-2-ol

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Voriconazole (UK-109496) is a new triazole derivative similar to fluconazole and itraconazole that acts by inhibiting fungal cytochrome P-450-dependent, 14-alpha-sterol demethylase-mediated synthesis of ergosterol.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Cytochrome P450 51 inhibitor

Product Properties

• ALogP: 1.5

Names and Identifiers

• Isomeric SMILES: C[C@@H](C1=NC=NC=C1F)[C@](CN2C=NC=N2)(C3=C(C=C(C=C3)F)F)O
• WGK Germany: 3
• RTECS: UV9145000
• PubChem CID: 71616
• Molecular Weight: 349.31
• Reaxy-Rn: 7694998

Associated Targets(Human)

CYP2B6 Tchem Cytochrome P450 2B6 (3 Activities)

Discover Target: CYP2B6

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

CYP46A1 Tchem Cholesterol 24-hydroxylase (8 Activities)

Discover Target: CYP46A1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 87 mg/mL (307.04 mM); Ethanol: 3 mg/mL (10.58 mM); Water: Insoluble
• Specific Rotation[α]: -58.0 to -62.0 deg(C=1, MeOH)
• Boil Point(°C): ~508.6° C at 760 mmHg
• Melt Point(°C): 128-134°C

References

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