Bromoenol lactone ((6E)-Bromoenol lactone) is a suicide-based irreversible, selective, potent inhibitor of calcium-independent phospholipase A2 (iPLA2β) with an IC50 value of approximately 7 μM, which inhibits antigen-stimulated mast cell exocytosis without blocking Ca2+ influx.
| Molecular Weight | 317.18 |
| Formula | C16H13BrO2 |
| CAS Number | 88070-98-8 |
| Form | Solid |
| Solubility (25°C) | DMSO 50 mg/mL (ultrasonic) |
| 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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