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PMX 53 and PMX 205 are cyclic hexapeptide inhibitors of complement C5a receptors (C5aR1), that are widely used to study C5aR1 pathobiology in mouse models of disease. PMX 205 is a cyclic hexapeptide. It is a potent antagonist of the C5a receptor (C5aR). It is orally active. PMX 205 is also brain penetrant and reduces fibrillar amyloid deposits, decreases hyperphosphorylated tau levels, and rescues cognitive function. PMX205 entered the intact CNS at pharmacologically active concentrations, with increased entry observed in hSOD1G93A mice. PMX53 inhibits C5a-induced hypernociception in rats, inhibits lung metastasis in a mouse breast cancer model and reduces atherosclerotic lesions in a mouse model of atherosclerosis. |
