1883548-84-2

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 V_ss of 3.6 L/kg and MRT of 2.3 hours in Sprague-Dawley rats and male CD-1 mice^[1].