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 | |
|---|---|
| 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 | |
|---|---|
| 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.
| Related Phospholipase Products |
|---|
| Phospholipase A2
Phospholipase A2 (PLA2) catalyzes the hydrolysis of the sn-2 position of membrane glycerophospholipids to liberate arachidonic acid (AA). |
| Melittin
Melittin is a PLA2 activator that stimulates the activity of low molecular weight PLA2 without increasing the activity of high molecular weight PLA2. |
| trans-4-phenylbut-3-en-2-one
trans-Benzylideneacetone (trans-Benzalacetone), a metabolite of gram-negative entomopathogenic bacterium Xenorhabdus nematophila, is an enzyme inhibitor against phospholipase A2 (PLA2). |
| SYN-020
SYN-020 is an orally active recombinant bovine intestinal alkaline phosphatase (IAP) for studies related to digestive disorders. |
| IIAEK
IIAEK is a novel cholesterol-lowering pentapeptide derived from bovine milk β-lactoglobulin that targets intestinal alkaline phosphatase (IAP) and improves cholesterol metabolism through the specific activation of IAP and down-regulation of ABCA1. Sequence: Ile-Ile-Ala-Glu-Lys |
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