| Description | Darapladib (SB-480848)(IC50=0.25 nM) is a substituted pyrimidone with inhibitory activity towards lipoprotein-associated phospholipase-A2 (Lp-PLA2). |
| In vitro | During the copper catalysed oxidation of human LDL, Darapladib prevents the production of lyso-PtdCho with IC50 of 4 nM and subsequent monocyte chemotaxis with IC50 of 4 nM. [1] |
| In vivo | In the WHHL rabbits, Darapladib (30 mg/kg p.o.) exhibits excellent inhibition of Lp-PLA2 within the atherosclerotic plaque by 95%. [1] Darapladib, as an inhibitor of Lp-PLA2, reduces development of advanced coronary atherosclerosis in diabetic and hypercholesterolemic (DMHC) pigs. [2] In DMHC pigs, darapladib reduces the amount of IgG-immunopositive material that leaked into the brain and also the density of Aβ42-containing neurons. [3] |
| Target activity | Lp-PLA2:0.25 nM |
| Synonyms | 达拉地, SB-480848 |
| molecular weight | 666.77 |
| Molecular formula | C36H38F4N4O2S |
| CAS | 356057-34-6 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: < 1 mg/mL (insoluble or slightly soluble) DMSO: 45 mg/mL (67.49 mM) Ethanol: 93 mg/mL (139.5 mM) |
| References | 1. Blackie JA, et al. Bioorg Med Chem Lett. 2003, 13(6), 1067-1070. 2. Wilensky RL, et al. Nat Med. 2008, 14(10), 1059-1066. 3. Acharya NK, et al. J Alzheimers Dis. 2013, 35(1), 179-198. |