| Description | Lp-PLA2-IN-3 is a potent and orally bioactive lipoprotein-associated phospholipase A2 (Lp-PLA2) inhibitor that inhibits recombinant human Lp-PLA2 with an IC50 value of 14 nM. |
| In vivo | Lp-PLA2-IN-3 (1 mg/kg; i.v.) treatment shows the CL, Vss, and t1/2 were 3.1mL/min/kg, 0.3 L/kg, 4 hours, respectively.[1] Lp-PLA2-IN-3 (3 mg/kg; p.o.) treatment shows the Cmax, AUC0-24h, t1/2, and F were 0.27 μg/mL, 3.4 μg h/mL, 7.7 hours, and 35.5%, respectively.[1] |
| Target activity | Lp-PLA2:14 nM |
| molecular weight | 467.85 |
| Molecular formula | C20H13ClF3N3O3S |
| CAS | 2196245-16-4 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 250 mg/mL (534.36 mM) |
| References | 1. Liu Q, et al. Structure-Guided Discovery of Novel, Potent, and Orally Bioavailable Inhibitors of Lipoprotein-Associated Phospholipase A2. J Med Chem. 2017 Dec 28;60(24):10231-10244. |