Bioactivity | 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]. | ||||||||||||
Invitro | PC945 is a triazole antifungal designed for administration via inhalation[1].PC945 exhibits the most potent antifungal activity on azole-susceptible strain NCPF2010 with the MIC value of 0.063 µg/mL[2]. | ||||||||||||
In Vivo | PC945 (0.56-14 μg/mouse; intranasal; daily for 7 days) substantially inhibits the incidence of rolling behavior[1]. Animal Model: | ||||||||||||
Name | PC945 | ||||||||||||
CAS | 1931946-73-4 | ||||||||||||
Formula | C38H37F3N6O3 | ||||||||||||
Molar Mass | 682.73 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. [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. |