Darapladib (CAS 356057-34-6) is a selective inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2), an enzyme strongly implicated in the progression and instability of atherosclerotic plaques. In vitro, Darapladib shows high potency toward Lp-PLA2 (IC50 approximately 270 pM) with minimal inhibition of other secretory PLA2 isoforms (e.g., III, V, X). Preclinical studies in ApoE-deficient mouse models demonstrate that inhibition of Lp-PLA2 attenuates vascular inflammatory processes and markedly reduces atherosclerotic lesion formation. Clinically, Darapladib administration in statin-treated patients significantly decreases plasma Lp-PLA2 activity and inflammatory markers, indicating potential applications in cardiovascular research related to atherosclerosis and associated inflammation.
Chemical Properties
Physical Appearance
A solid
Storage
Store at -20°C
M.Wt
666.77
Cas No.
356057-34-6
Formula
C36H38F4N4O2S
Synonyms
SB-480848;SB480848;SB 480848
Solubility
≥32.95 mg/mL in DMSO; insoluble in H2O; ≥891 mg/mL in EtOH
