Posaconazole

Short Summary : Sterol C14ɑ demethylase inhibitor

Category : Metabolism|C14ɑ demethylase

Purity : 0.9992

CAS Number : 171228-49-2

Formula : C37H42F2N8O4

Molecular Weight : 700.78

SMILE : CCC(C(C)O)N1C(=O)N(C=N1)C2=CC=C(C=C2)N3CCN(CC3)C4=CC=C(C=C4)OCC5CC(OC5)(CN6C=NC=N6)C7=C(C=C(C=C7)F)F

Solubility : >35mg/mL in DMSO

Storage : Store at -20°C

Description : Posaconazole, also known as SCH 56592 or Noxafil, is a novel triazole antifungal compound that potently inhibits 14-demethylation in a variety of fungi, including Candida (C. albicans C43, C. albicans C288, C. albicans C600 and C. albicans C248) and Aspergillus (A. fumigatus ND158 and A. flavus ND134), with half maximal inhibition concentration IC50 of 0.007 g/ml, 0.06 g/ml, 0.2 g/ml, 0.3 g/ml, 0.03 g/ml and 0.03 g/ml respectively [1].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 14-demethylase, which converts lanosterol to 14-dimethy lanosterol, resulting in the disruption of the integrity and function of the fungal cell membrane and inhibition of fungal growth [2].References:[1] Hanan K. Munayyer, Paul A. Mann, Andrew S. Chau, Taisa Yarosh-Tomaine, Jonathan R. Greene, Roberta S. Hare, Larry Heimark, Robert E. Palermo, David Loebenberg and Paul M. McNicholas. Posaconazole is a potent inhibitor of sterol 14-demethylation in yeasts and molds. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY. 2004; 48(10): 3690-3696[2] Daryl S. Schiller and Horatio B. Fung. Posaconazole: an extended-spectrum triazole antifungal agent. Clinical Therapeutics. 2007; 29(9): 1862-1886

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