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PMX-53 is a potent CD88 (C5aR) antagonist with an IC50 of 20 nM, it inhibits C5a-induced neutrophil myeloperoxidase release and chemotaxis with IC50 values of 22 nM and 75 nM, respectively. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 specifically binds to C5aR1 and does not bind to the second C5aR (C5L2) and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects.
| Molecular Weight | 896.09 |
| Formula | C47H65N11O7 |
| CAS Number | 219639-75-5 |
| Form | Solid |
| Solubility (25°C) | DMSO 100 mg/mL Water 5 mg/mL (ultrasonic and warming) |
| Storage | Store at ≤ -20°C, protect from light, dry, sealed |
[6] Jrg Khl. Curr Opin Mol Ther. Drug evaluation: the C5a receptor antagonist PMX-53
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