Fluconazole (UK 49858) - Moligand™, 10mM in DMSO , Cytochrome P450 51 inhibitor, CAS No.86386-73-4, Cytochrome P450 51 inhibitor

CAS: 86386-73-4 Cat. No.: F408555 Molecular Weight: 306.27 EC Number: 691-089-0

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

2-(2,4-difluorophenyl)-1,3-di(1H-1,2,4-triazol-1-yl)propan-2-ol

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Fluconazole (UK 49858) is a fungallanosterol 14 alpha-demethylaseinhibitor, which thereby prevents the formation of ergosterol,used in the treatment and prevention of superficial and systemic fungal infections.
In vitro

Fluconazole in combination with amphotericin B (AmB) has a synergistic effect on C. albicans planktonic cells but does not alter AmB activity against biofilms. Fluconazole and caspofungin have an antagonistic effect against biofilms but not with planktonic cells. Fluconazole-mediated membrane perturbation (due to inhibition of ergosterol biosynthesis) increases calcineurin inhibitor intracellular concentrations. Fluconazole treatment significantly reduces levels of ergosterol within the cell in C. albicans planktonic cells, leading to cell membrane perturbation. Fluconazole activity is less sensitive to acidic medium than is that of ketoconazole. Fluconazole is approximately 16-fold less active than ketoconazole against 35 representative isolates of C. albicans at physiologic pH. Fluvastatin, a cholesterol-lowering drug, exhibits minimal activity (MICs of 64 to >128 mg/mL) against Candida species and Cryptococcus neoformans. Fluconazole combined with itraconazole exhibits potent activities against C. albicans, C. tropicalis, C. parapsilosis, and C. neoformans, including flucon- azole-resistant strains of C. albicans and C. tropicalis.

In vivo

Fluconazole is very effective in prolonging survival of rats infected with a representative candidal strain. Fluconazole has a dramatic effect on the fungicidal activity of flucytosine in murine cryptococcal meningitis. Fluconazole combined with flucytosine and amphotericin B have significantly improved activity against cryptococcal meningitis compared with the activity of each drug used alone.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥95%

Specifications

Synonyms

2-(2, 4-difluorophenyl)-1, 3-di(1H-1, 2, 4-triazol-1-yl)propan-2-ol

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Fluconazole (UK 49858) is a fungal lanosterol 14 alpha-demethylase inhibitor, which thereby prevents the formation of ergosterol, used in the treatment and prevention of superficial and systemic fungal infections.

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

Names and Identifiers

• Isomeric SMILES: C1=CC(=C(C=C1F)F)C(CN2C=NC=N2)(CN3C=NC=N3)O
• WGK Germany: 3
• RTECS: XZ4810000
• Molecular Weight: 306.27
• Reaxy-Rn: 4269710
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=4269710&ln=

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 56 mg/mL (197.0 mM); Ethanol: 8 mg/mL (28.14 mM); Water: Insoluble
• Melt Point(°C): 138.0-142.0℃

References

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