Name: Posaconazole
Price: 259.00 USD

- Overview
  - Posaconazole is a synthetic, broad-spectrum, second generation triazole with antifungal activity. It has potent in vitro and in vivo trypanocidal activity. It was discovered by Schering-Plough and it is a structural analog of itraconazole. It has promising anti-cancer properties. Posaconazole is slightly soluble in DMSO but is practically insoluble in water.
    
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    Background
    
    Posaconazole blocks ergosterol synthesis, by inhibiting the enzyme lanosterol 14 α-demethylase. The result is an accumulation of methylated sterol precursors. It also inhibits CYP3A4, but does not inhibit the activity of other CYP enzymes thus it may have the potential for fewer drug interactions.
- Properties
  - CAS Number
    
    171228-49-2
    
    Molecular Formula
    
    C37H42F2N8O4
    
    Molecular Weight
    
    700.78
    
    Appearance
    
    White to off-white crystalline powder
    
    Solubility
    
    Slightly soluble in DMSO. Practically insoluble in water.
    
    Other Properties
    
    Source: Synthetic
    Purity Level: 98-102% (anhydrous basis)
    
    Storage
    
    -20°C
    
    * For research use only
- Applications
  - Application Description
    
    Spectrum: Broad-spectrum antifungal activity including yeast (Candida) and fungi (Aspergillus spp. Scedosporium, Fusarium spp. Zygomycetes spp). It is effective against a parasitological cure in a murine model of Chagas disease caused by Trypanosoma cruzi. Triazole resistance is increasing among fungal pathogens including Candida spp. due to multiple molecular mechanisms.
    
    Microbiology Applications: Posaconazole was involved in a 10-year study of 19,000 clinically important strains of yeast and mold with 200 medical centers participating. Strains were tested using CLSI broth microdilution methods with RPMI 1640 medium, with MIC50 (0.063 µg/ml) and MIC90 (1 µg/ml) for all fungal isolates in the database. For both yeasts and molds, MIC90 was 1 µg/ml. The compound was active against Candida and Aspergillus isolates that are resistant to Fluconazole, Voriconazole, and Amphotericin B (Sabatelli et al, 2006).
    The in vivo efficacy of Poscanazole was studied in a murine model against four Aspergillus fumigatus isolates with MICs of 0.03-16 mg/L. Resistance mechanisms included substitutions in the cyp51A gene (Mavridou et al, 2010).
    As a trypanocidal agent, it can act synergistically with Amiodarone. It disrupts Ca2+ homeostasis in T. cruzi (Benaim et al, 2006). The antiproliferative synergism of the compounds was characterized using electron microscopy (Veiga-Santos et al, 2012) and this association is promising against T. cruzi.
    
    Cancer Applications: Deregulation of the Hedgehog (Hh) pathway signaling pathway, a highly conserved developmental pathway, leads to disorders and cancers such as basal cell carcinoma. Under normal conditions, binding of a Hh ligand, relieves its inhibition of Smoothened (SMO), a transmembranae protein. Posaconazole inhibits the Hh pathway by a similar mechanism to itraconazole. It is a promising compound for Hh-dependent cancers (Chen B et al, 2016).