PMX-53 TFA

PMX-53, a macrocyclic complement 5a (C5a) peptidomimetic and C5a receptor antagonist (IC50 = 0.3 µM), effectively inhibits the C5a-induced secretion of myeloperoxidase (MPO) in isolated human polymorphonuclear leukocytes (PMNs) . Administered orally at 10 mg/kg, PMX-53 mitigates vascular leakage, PMN infiltration, and the production of TNF-? and IL-6 in a rat peritoneal Arthus reaction model. Additionally, in a 3-nitropropionic acid (3-NP) -induced Huntington's disease rat model, it alleviates body weight loss, anorexia, and striatal degeneration. Furthermore, at a dose of 3 mg/kg, PMX-53 decreases atherosclerotic lesion size and lipid content in ApoE-/- mice.

O=C([C@H](NC([C@@]1([H])N(CCC1)C([C@H](CCCNC([C@@H](NC2=O)CCCNC(N)=N)=O)NC([C@@H](NC(C)=O)CC3=CC=CC=C3)=O)=O)=O)CC4CCCCC4)N[C@H]2CC5=CNC6=CC=CC=C56.OC(C(F)(F)F)=O