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AMG 580

Names

[ CAS No. ]:
1227067-71-1

[ Name ]:
AMG 580

[Synonym ]:
1-(4-{3-[4-(1H-Benzimidazol-2-ylcarbonyl)phenoxy]-2-pyrazinyl}-1-piperidinyl)-2-fluoro-1-propanone
1-Propanone, 1-[4-[3-[4-(1H-benzimidazol-2-ylcarbonyl)phenoxy]-2-pyrazinyl]-1-piperidinyl]-2-fluoro-
MFCD30470997

Biological Activity

[Description]:

AMG 580 (AMG580) is a novel potent, selective phosphodiesterase 10A (PDE10A) inhibitor with IC50 of 0.13 nM; displays no activity against PED isoforms at 30 uM; is suitable as a tracer for lead optimization to determine target coverage by novel PDE10A inhibitors, shows potential imaging biomarker for mapping PDE10A distribution and ensuring target coverage by therapeutic PDE10A inhibitors in clinical studies.

[References]

References 1. Chen H, et al. J Pharmacol Exp Ther. 2015 Feb;352(2):327-37. 2. Hu E, et al. ACS Med Chem Lett. 2016 May 19;7(7):719-23. 3. Hwang DR, et al. Nucl Med Biol. 2015 Aug;42(8):654-63. View Related Products by Target Phosphodiesterase (PDE)

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
712.1±70.0 °C at 760 mmHg

[ Molecular Formula ]:
C26H24FN5O3

[ Molecular Weight ]:
473.499

[ Flash Point ]:
384.5±35.7 °C

[ Exact Mass ]:
473.186310

[ LogP ]:
3.25

[ Vapour Pressure ]:
0.0±2.3 mmHg at 25°C

[ Index of Refraction ]:
1.637

Related Compounds