| Identification | Back Directory | [Name]
PC945 | [CAS]
1931946-73-4 | [Synonyms]
PC945
PC-945,PC945
D-threo-Pentitol, 2,5-anhydro-1,3,4-trideoxy-2-C-(2,4-difluorophenyl)-4-[[4-[4-[4-[[(4-fluorophenyl)amino]carbonyl]phenyl]-1-piperazinyl]-2-methylphenoxy]methyl]-1-(1H-1,2,4-triazol-1-yl)- | [Molecular Formula]
C38H37F3N6O3 | [MDL Number]
MFCD32858242 | [MOL File]
1931946-73-4.mol | [Molecular Weight]
682.75 |
| Hazard Information | Back Directory | [Uses]
PC945, a potent, long-acting antifungal triazole, possesses activity against a broad range of both azole-susceptible and azole-resistant strains of Aspergillus fumigatus. PC945 is also a potent, tightly binding inhibitor of A. fumigatus sterol 14α-demethylase activity, CYP51A and CYP51B, with IC50s of 0.23 μM and 0.22 μM, respectively[1][2]. | [in vivo]
PC945 (0.56-14 μg/mouse; intranasal; daily for 7 days) substantially inhibits the incidence of rolling behavior[1]. | Animal Model: | Specific-pathogen-free A/J mice (male, 5 weeks old, pulmonary Aspergillus infection)[1] | | Dosage: | 0.56, 2.8, 14 μg/mouse (intranasal application of 0.016-, 0.08-, and 0.4-mg/ml suspensions, respectively) | | Administration: | Intranasal; daily for 7 days | | Result: | Substantially inhibited the incidence of rolling behavior. |
| [IC 50]
fungal; CYP51A: 0.23 μM (IC50); CYP51B: 0.22 μM (IC50) | [References]
[1] Colley T, et al. In Vitro and In Vivo Antifungal Profile of a Novel and Long-Acting Inhaled Azole, PC945, on Aspergillus fumigatus Infection. Antimicrob Agents Chemother. 2017 Apr 24;61(5). pii: e02280-16. DOI:10.1128/AAC.02280-16
[2] Colley T, et al. Antifungal synergy of a topical triazole, PC945, with a systemic triazole against respiratory Aspergillus fumigatus infection. Sci Rep. 2019 Jul 1;9(1):9482. DOI:10.1038/s41598-019-45890-w |
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