| Description | Rilapladib (SB 659032) is a selective inhibitor of Lipoprotein-Associated Phospholipase A2(Lp-PLA2, IC50 = 230 pM) and an antagonist of the platelet activating factor receptor. |
| In vitro | Rilapladib reduces the PAF biological activity and levels, thereby reducing Lp-PLA2 biosynthesis and preventing the possible adverse effects of Lp-PLA2 [2]. |
| Target activity | Lp-PLA2:230 pM |
| Synonyms | SB 659032 |
| molecular weight | 735.8 |
| Molecular formula | C40H38F5N3O3S |
| CAS | 412950-08-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 78 mg/mL (106 mM), Sonication is recommended. |
| References | 1. Shaddinger BC, et al. Platelet aggregation unchanged by lipoprotein-associated phospholipase A₂ inhibition: results from an in vitro study and two randomized phase I trials. PLoS One. 2014 Jan 27;9(1):e83094. 2. Athanasios Papakyriakou, et al. Computational Investigation of Darapladib and Rilapladib Binding to Platelet Activating Factor Receptor. A Possible Mechanism of Their Involvement in Atherosclerosis. International Journal of Chemistry; Vol. 6, No. 1; 2014. |