Posaconazole

Catalog #

27639-2

$505 *

Size: 25 mg

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Description

A sterol C14? demethylase inhibitor with an IC50 of 0.25 nM. Anti-fungal used to prevent serious fungal infections in people with a weakened ability to fight infection and to treat yeast infections.

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Synonyms

Noxafil; SCH 56592; 4-[4-[4-[4-[[(3R,5R)-5-(2,4-difluorophenyl)-5-(1,2,4-triazol-1-ylmethyl)oxolan-3-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-2-[(2S,3S)-2-hydroxypentan-3-yl]-1,2,4-triazol-3-one

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Product Data Gallery

Product Info

Storage and Usage

Citations

Purity

≥98% by HPLC

Target(s)

CYP51A1

Formula

C₃₇H₄₂F₂N₈O₄

700.78 Da

Solubility

Soluble in DMSO

Biological Activity

Posaconazole inhibits growth of Candida (C. albicans C43, C. albicans C288, C. albicans C600 and C. albicans C248) and Aspergillus (A. fumigatus ND158 and A. flavus ND134), with IC50 of 0.007 µg/ml, 0.06 µg/ml, 0.2 µg/ml, 0.3 µg/ml, 0.03 µg/ml and 0.03 µg/ml, respectively.

CAS Registry #

171228-49-2

Background

Posaconazole, also known as SCH 56592 or Noxafil, is a novel triazole antifungal compound that potently inhibits 14α-demethylation in a variety of fungi. Posaconzole, an itraconzole derivative with fluorine replacing chlorine in the phenyl ring and hydroxylation in the side chain, binds to the heme cofactor on the active site of 14α-demethylase, which converts lanosterol to 14α-dimethy lanosterol, resulting in the disruption of the integrity and function of the fungal cell membrane and inhibition of fungal growth.

References

1. Hanan K. et al. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY. 2004; 48(10): 3690-3696.
2. Daryl S. et al. Clinical Therapeutics. 2007; 29(9): 1862-1886.

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