AMG PERK 44 (orally; 3-100 mg/kg) robustly inhibits PERK autophosphorylation in this assay (ED50=3 mg/kg; ED90=60 mg/kg at the 4 hours time point), and >50% target coverage is maintained for 24 h in a time course PD assay when dosed at 100 mg/kg po[1].
AMG PERK 44 (iv; 1 mg/kg) has a CL of 1.6 L/h?kg, a Vss of 3.6 L/kg and MRT of 2.3 hours in Sprague-Dawley rats and male CD-1 mice[1].
| Animal Model: | Four- to six-week old naive athymic nude mice[1] |
| Dosage: | 3, 10, 30, 100 mg/kg |
| Administration: | Orally |
| Result: | Robustly inhibited PERK autophosphorylation in this assay (ED50=3 mg/kg; ED90=60 mg/kg at the 4 hours time point).
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| Animal Model: | Sprague-Dawley rats and male CD-1 mice[1] |
| Dosage: | 1 mg/kg (Pharmacokinetic Analysis) |
| Administration: | Iv |
| Result: | Had a CL of 1.6 L/h?kg, a Vss of 3.6 L/kg and a MRT of 2.3 hours.
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