Biological ActivityPMX 205 is a potent C5a receptor peptide antagonist (IC50 = 31 nM). Ameliorates experimentally-induced colon inflammation in mice. Reduces fibrillar amyloid deposits, decreases hyperphosphorylated tau levels and rescues cognitive function in a mouse model of Alzheimer's disease. Also improves hindlimb grip strength and slows disease progression in the hSOD1G93A mouse model of amyotrophic lateral sclerosis. Orally active and brain penetrant.
(Modifications: X-1 = N2-(1-Oxo-3-phenylpropyl)-Orn, X-3 = D-Cha, Lactam bridge: Orn-1 to Arg-5)
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Pharmacological inhibition of complement C5a-C5a1 receptor signalling ameliorates disease pathology in the hSOD1G93A mouse model of amyotrophic lateral sclerosis.
Lee et al.
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.
Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activity.
March et al.
Treatment with a C5aR antagonist decreases pathology and enhances behavioral performance in murine models of Alzheimer's disease.
Fonseca et al.
The C5a receptor antagonist PMX205 ameliorates experimentally induced colitis associated with increased IL-4 and IL-10.
Jain et al.
Citation for PMX 205
The citations listed below are publications that use Tocris products. Selected citations for PMX 205 include:
1 Citation: Showing 1 - 1
Complement Receptor C5aR1 Plays an Evolutionarily Conserved Role in Successful Cardiac Regeneration.
Authors: Natarajan Et al.
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