| Bioactivity | AMG 579 is a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A) with an IC50 of 0.1 nM. | ||||||||||||
| Target | IC50: 0.1 nM (Phosphodiesterase 10A) | ||||||||||||
| 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]. | ||||||||||||
| Name | AMG 579 | ||||||||||||
| CAS | 1227067-61-9 | ||||||||||||
| Formula | C25H23N5O3 | ||||||||||||
| Molar Mass | 441.48 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [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 |