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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)
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solubility||Soluble to 1 mg/ml in water with sonication|
References are publications that support the biological activity of the product.
March et al (2004) Potent cyclic antagonists of the complement C5a receptor on human polymorphonuclear leukocytes. Relationships between structures and activity. Mol.Pharmacol. 65 868 PMID: 15044616
Fonseca et al (2009) Treatment with a C5aR antagonist decreases pathology and enhances behavioral performance in murine models of Alzheimer's disease. J.Immunol. 183 1375 PMID: 19561098
Jain et al (2013) The C5a receptor antagonist PMX205 ameliorates experimentally induced colitis associated with increased IL-4 and IL-10. Br.J.Pharmacol. 168 488 PMID: 22924972
Lee et al (2017) Pharmacological inhibition of complement C5a-C5a1 receptor signalling ameliorates disease pathology in the hSOD1G93A mouse model of amyotrophic lateral sclerosis. Br.J.Pharmacol. 174 689 PMID: 28128456
Kumar et al (2018) Development and validation of a LC-MS/MS assay for pharmacokinetic studies of complement C5a receptor antagonists PMX53 and PMX205 in mice. Sci.Rep. 8 8101 PMID: 29802264
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Keywords: PMX 205, PMX 205 supplier, PMX205, potent, c5a, receptor, peptide, antagonist, alzheimer's, disease, alzheimers, antialzheimers, antiinflammatory, Complement, 5196, Tocris Bioscience
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