APX001

Names

[ Name ]:
APX001

[Synonym ]:
7B1P18ID9L
E1210
E-1210
3-(3-{4-[(2-Pyridinyloxy)methyl]benzyl}-1,2-oxazol-5-yl)-2-pyridinamine
2-Pyridinamine, 3-[3-[[4-[(2-pyridinyloxy)methyl]phenyl]methyl]-5-isoxazolyl]-

Biological Activity

[Description]:

APX001 (APX 001A;E1210) is a novel broad-spectrum antifungal agent that inhibits the fungal protein Gwt1, demonstrates significantly acitive MIC50 and MIC90 values of 0.004 and 0.031 ug/ml (16 strains of C. auris); inhibits the inositol acylation activity of C. albicans Gwt1p and A. fumigatus Gwt1p with IC50 of 0.3 to 0.6 uM but has no inhibitory activity against human Pig-Wp; shows significant efficacy in murine model of disseminated C. auris infection, and log reduction in CFU counts in kidney, lung, and brain tissue. Fungal Infection Phase 1 Clinical

[References]

References 1. Hager CL, et al. Antimicrob Agents Chemother. 2018 Feb 23;62(3). pii: e02319-17. 2. Zhao M, et al. Antimicrob Agents Chemother. 2018 Jan 29. pii: AAC.02542-17. 3. Watanabe NA, et al. Antimicrob Agents Chemother. 2012 Feb;56(2):960-71. 4. Miyazaki M, et al. Antimicrob Agents Chemother. 2011 Oct;55(10):4652-8. View Related Products by Target Fungal Fungal Infection

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
569.4±45.0 °C at 760 mmHg

[ Molecular Formula ]:
C₂₁H₁₈N₄O₂

[ Molecular Weight ]:
358.393

[ Flash Point ]:
298.1±28.7 °C

[ Exact Mass ]:
358.142975

[ LogP ]:
3.75

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.640

Related Compounds

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