| CAS | 219639-75-5 |
| Sequence | Ac-Phe-Orn-Pro-D-Cha-Trp-Arg-OH(Lactam bridge: Orn-2 to Arg-6 ) |
| Sequence Single | Ac-F-Orn-P-D-Cha-WR(Lactam bridge: Orn-2 to Arg-6 ) |
| Molecular Formula | C47H65N11O7 |
| Molecular Weight | 896.1 |
| Technology | Synthetic |
| Storage | -20°C, avoid light, cool and dry place |
| Description | PMX-53 (3D53) is a synthetic peptidic and a potent and 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, anticancer and antiatherosclerotic effects. |
| References | 1. Role of complement C5a in mechanical inflammatory hypernociception: potential use of C5a receptor antagonists to control inflammatory pain. Ting et al (2008). Br.J.Pharmacol. 153 1043 PMID: 18084313 2. PMX-53 as a dual CD88 antagonist and an agonist for Mas-related gene 2 (MrgX2) in human mast cells. Subramanian et al (2011). Mol.Pharmacol. 79 1005 PMID: 21441599 3. Low-molecular-weight peptidic and cyclic antagonists of the receptor for the complement factor C5a. Finch et al (1999). J.Med.Chem. 42 1965 PMID: 10354404 4. Complement c5a receptor facilitates cancer metastasis by altering T-cell responses in the metastatic niche. Vadrevu et al (2014). Cancer Res. 74 3454 PMID: 24786787 5. Complement C5a inhibition reduces atherosclerosis in ApoE-/- mice. Manthey et al (2011). FASEB J 25 2447 PMID: 21490292 6. Development and validation of a LC-MS/MS assay for pharmacokinetic studies of complement C5a receptor antagonists PMX53 and PMX205 in mice. Kumar et al (2018). Sci.Rep. 8 8101 PMID: 29802264 |