| Identification | Back Directory | [Name]
L-Arginine, N-acetyl-L-phenylalanyl-L-ornithyl-L-prolyl-3-cyclohexyl-D-alanyl-L-tryptophyl-, (6→2)-lactam, trifluoroacetate (9CI) | [CAS]
514814-99-4 | [Synonyms]
PMX-53 (trifluoroacetate salt)
L-Arginine, N-acetyl-L-phenylalanyl-L-ornithyl-L-prolyl-3-cyclohexyl-D-alanyl-L-tryptophyl-, (6→2)-lactam, trifluoroacetate (9CI) | [Molecular Formula]
C49H66F3N11O9 | [MOL File]
514814-99-4.mol | [Molecular Weight]
1010.13 |
| Hazard Information | Back Directory | [Description]
PMX-53 is a macrocyclic complement 5a (C5a) peptidomimetic and an antagonist of the C5a receptor (IC50 = 0.3 µM).1 It inhibits C5a-induced secretion of myeloperoxidase (MPO) in isolated human polymorphonuclear leukocytes (PMNs). PMX-53 (10 mg/kg, p.o.) inhibits vascular leakage, PMN infiltration, and peritoneal TNF-α and IL-6 production in a rat model of the peritoneal Arthus reaction.1 It reduces body weight loss and anorexia and inhibits striatal degeneration in a rat model of Huntington’s disease induced by 3-nitropropionic acid (3-NP; Item No. 14684).2 PMX-53 (3 mg/kg) also reduces atherosclerotic lesion size and lipid content in ApoE-/- mice.3WARNING This product is not for human or veterinary use. | [References]
[1] ANGELA M. FINCH. Low-Molecular-Weight Peptidic and Cyclic Antagonists of the Receptor for the Complement Factor C5a[J]. Journal of Medicinal Chemistry, 1999, 42 11: 1965-1974. DOI: 10.1021/jm9806594
[2] TRENT M. WOODRUFF. Therapeutic activity of C5a receptor antagonists in a rat model of neurodegeneration[J]. FASEB Journal, 2006, 20 9: 1407-1417. DOI: 10.1096/fj.05-5814com
[3] HELGA D. MANTHEY. Complement C5a inhibition reduces atherosclerosis in ApoE–/– mice[J]. FASEB Journal, 2011, 25 7: 2447-2455. DOI: 10.1096/fj.10-174284 |
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