PKSI-527 is an inhibitor of plasma kallikrein (K = 0.81 μM). It is selective for plasma kallikrein over glandular kallikrein, plasmin, thrombin, urokinase, and Factor Xa (Ks = >500, 390, >500, 200, and >500 μM, respectively). PKSI-527 reduces bradykinin generation induced by kaolin and λ-carrageenan ex vivo in human plasma. It also prolongs partial thromboplastin and euglobulin clot lysis times. In vivo, PKSI-527 (300 mg/kg per day) reduces hyperplasia, pannus formation, and infiltration of inflammatory cells in the tarsal joint of mice with collagen-induced arthritis.
PKSI-527 is a new, highly selective plasma kallikrein inhibitor. PKSI-527 can suppress collagen-induced arthritis (CIA) by modifying the kallikrein-kinin system[1].
分子式
C25H31N3O4.HCl
分子量
473.99
CAS号
128837-71-8
运输条件
Room temperature in continental US; may vary elsewhere.