In Vitro: Darapladib (5 μM; 6, 12 h) induces cell cycle arrest in glioma cells (C6 glioma cells and U251MG cells). Darapladib (5 μM; 3, 6 h) triggers cell apoptosis in glioma cells. Darapladib (5 μM; 5, 15, 30, 60 and 90 min) induces an increase in phosphorylation of ERK1/2 proteins in glioma cells.
In Vivo: Darapladib (50 mg/kg; p.o.; once daily for 6 weeks) significantly inhibits serum Lp-PLA2 activity in LDLR-deficient mice. Darapladib (50 mg/kg; p.o.; once daily for 6 weeks) decreases serum hs-CRP and IL-6 levels.