PMX 53
PMX 53
CAS: 219639-75-5
Molecular Formula: C47H65N11O7
PMX 53 - Names and Identifiers
| Name | PMX 53 |
| Synonyms | PMX 53 Ac-Phe-cyclo(Orn-Pro-D-Cha-Trp-Arg) L-Arginine, N-acetyl-L-phenylalanyl-L-ornithyl-L-prolyl-3-cyclohexyl-D-alanyl-L-tryptophyl-, (6→2)-lactam |
| CAS | 219639-75-5 |
PMX 53 - Physico-chemical Properties
| Molecular Formula | C47H65N11O7 |
| Molar Mass | 896.11 |
| Density | 1.40±0.1 g/cm3(Predicted) |
| pKa | 13.23±0.70(Predicted) |
| In vitro study | PMX-53 is a potent CD88 antagonist and inhibits C5a-induced neutrophil myeloperoxidase release and chemotaxis with IC 50 values of 22 nM and 75 nM, respectively. PMX-53 (10 nM) inhibits C5a-induced Ca 2+ mobilization in HMC-1 cells, but at higher concentrations( ≥30 nM) it causes degranulation in LAD2 mast cells, CD34 + cell-derived mast cells, and RBL-2H3 cells stably expressing MrgX2. Replacement of Trp with Ala and Arg with dArg abolishes the ability of PMX-53 to inhibit C5a-induced Ca 2+ mobilization in HMC-1 cells and to cause degranulation in RBL-2H3 cells expressing MrgX2. |
PMX 53 - References
| biological activity | PMX-53 (3D53) is a synthetic peptide that is also a potent, an orally active complement C5a receptor (CD88) antagonist with an IC50 of 20 nM. 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, anti-cancer and anti-atherosclerotic effects. |
| Target | IC50: 20 nM (Complement C5a receptor) MrgX2 |
| Animal Model: | Adult male Wistar rats (weighing 180-200 g) injected with zymosan |
| Dosage: | 0.3 mg/kg, 1 mg/kg or 3 mg/kg |
| Administration: | Subcutaneous injection; once |
| Result: | Inhibited the hypernociception induced by zymosan-activated serum and C5a. |
Last Update：2024-04-09 02:00:19
