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1227067-61-9

1227067-61-9 structure
1227067-61-9 structure
  • Name: AMG-579
  • Chemical Name: AMG 579
  • CAS Number: 1227067-61-9
  • Molecular Formula: C25H23N5O3
  • Molecular Weight: 441.48
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphodiesterase (PDE)
  • Create Date: 2019-02-08 18:30:18
  • Modify Date: 2024-01-28 15:53:24
  • AMG 579 is a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A) with an IC50 of 0.1 nM.

Name AMG 579
Description AMG 579 is a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A) with an IC50 of 0.1 nM.
Related Catalog
Target

IC50: 0.1 nM (Phosphodiesterase 10A)[1]

In Vivo AMG 579 shows statistically significant reduction of PCP induced behavior in rats over the 2 h period. Minimum effective doses for efficacy in PCP-LMA model is determined to be 0.3 mg/kg for AMG 579. In dog, 5 exhibits superior oral bioavailability of 72%[1].
Animal Admin Rats[1] Adult male Sprague−Dawley rats (250−280 g) are dosed at 0.1, 0.3, 1, and 3 mg/kg PO 1 h prior to administration of PCP. The magnitude of rat locomotor activity is quantified as number of beam breaks over a 2 h period[1].
References

[1]. Hu E,et al. Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A). J Med Chem. 2014 Aug 14;57(15):6632-41.

Molecular Formula C25H23N5O3
Molecular Weight 441.48