Rilapladib (SB 659032) is a selective Lp-PLA2 (lipoprotein-associated phospholipase A2) inhibitor with an IC50 of 230 pM. Rilapladib (SB 659032) is also a PAFR (Platelet Activating Factor Receptor) antagonist.
Cell Experiment | |
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Cell lines | Platelet-rich plasma samples |
Preparation method | Lp-PLA2 activity was measured in parallel using plasma samples that were derived from PRP that had been treated either with vehicle or rilapladib (100 nM) for 5 minutes using [3H]-PAF as the substrate as previously described. |
Concentrations | 100 nM |
Incubation time | 5 minutes |
Animal Experiment | |
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Animal models | |
Formulation | |
Dosages | |
Administration |
Molecular Weight | 735.8 |
Formula | C40H38F5N3O3S |
CAS Number | 412950-08-4 |
Solubility (25°C) | DMSO 78 mg/mL |
Storage | Powder -20°C |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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